Table 1 (in 10 parts) summarizes... | American Society of Hematology

Table 1

(in 10 parts) summarizes observed or potential drug interactions between TKIs and commonly concomitantly prescribed drugs or classical interacting agents (lines) sorted according to the ATC classification. The arrows ↑ and ↓ indicate an increase or decrease of drug concentration, respectively. Boldface text outlines interactions reported in the literature (reference number), whereas standard characters represent potential interactions predicted from theoretical considerations (but not yet reported in the literature). “Absence of interaction” means that a clinical study concluded to the absence of interaction (reference number), and “—” means that no interaction is either reported or theoretically expected.

Part 1. Alimentary tract and metabolism
	Imatinib	Dasatinib	Nilotinib
PPI
Omeprazole	• Inhibition of Pgp by omeprazole: ↑ imatinib exposure^9,18,64	• ↓ dasatinib absorption⁹ (↓ dasatinib solubility) • Inhibition of Pgp by omeprazole: ↑ dasatinib exposure^9,18,64	—
Esomeprazole	• Inhibition of Pgp by esomeprazole: ↑ imatinib exposure^9,18,64	• ↓ dasatinib absorption⁹ (↓ dasatinib solubility) • Inhibition of Pgp by esomeprazole: ↑ dasatinib exposure^9,18,64	—
Pantoprazole	• Inhibition of Pgp by pantoprazole: ↑ imatinib exposure^9,18,64	• ↓ dasatinib absorption⁹ (↓ dasatinib solubility) • Inhibition of Pgp by pantoprazole: ↑ dasatinib exposure^9,18,64	—
H2-antagonists
Cimetidine	• Inhibition of CYP 3A4 and Pgp by cimetidine: ↑ imatinib exposure^18,65 • Inhibition of hOCT1 by cimetidine: ↓ imatinib intracellular exposure^18,64,65	• ↓ dasatinib absorption⁹ (↓ dasatinib solubility) • Inhibition of CYP 3A4 and Pgp by cimetidine: ↑ dasatinib exposure^18,65	• Inhibition of CYP 3A4 by cimetidine: ↑ nilotinib exposure^18,65
Ranitidine	• Inhibition of Pgp by ranitidine: ↑ imatinib exposure^18,65 • Inhibition of hOCT1 by ranitidine: ↓ imatinib intracellular exposure^9,18,64,65	• ↓ dasatinib absorption⁹ (↓ dasatinib solubility) • Inhibition of Pgp by ranitidine: ↑ dasatinib exposure^18,65	—
Antiemetics
Metoclopramide	—	• ↑ QT interval¹⁹ (additive effect) → monitor ECG	• ↑ QT interval¹⁹ (additive effect) → monitor ECG
Antidiabetic drugs
Insulin	—	—	—
Metformin	• Inhibition of hOCT1 by metformin: ↓ imatinib intracellular exposure^9,18,64	—	—
Glibenclamide	• Inhibition of CYP 3A4 and 2C9 by imatinib: ↑ glibenclamide exposure^9,18,19 • Inhibition of Pgp by glibenclamide: ↑ imatinib exposure^9,18,64	• Inhibition of CYP 3A4 by dasatinib: ↑ glibenclamide exposure^9,18,19 • Inhibition of Pgp by glibenclamide: ↑ dasatinib exposure^9,18,64	• Inhibition of CYP 3A4 and 2C9 by nilotinib: ↑ glibenclamide exposure^9,18,19
Acarbose	—	—	—
Rosiglitazone	• Inhibition of CYP 2C9 by imatinib: ↑ rosiglitazone exposure^9,18,19	—	• Inhibition of CYP 2C9 by nilotinib: ↑ rosiglitazone exposure^9,18,19
Pioglitazone	• Inhibition of CYP 3A4 and 2C9 by imatinib: ↑ pioglitazone exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ pioglitazone exposure^9,18,19	• Inhibition of CYP 3A4 and 2C9 by nilotinib: ↑ pioglitazone exposure^9,18,19
Nateglinide	• Inhibition of CYP 3A4 and 2C9 by imatinib: ↑ nateglinide exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ nateglinide exposure^9,18,19	• Inhibition of CYP 3A4 and 2C9 by nilotinib: ↑ nateglinide exposure^9,18,19
Repaglinide	• Inhibition of CYP 3A4 by imatinib: ↑ repaglinide exposure^9,18,19	• Inhibition of CYP 3A4 and 2C8 by dasatinib: ↑ repaglinide exposure^9,18,19	• Inhibition of CYP 3A4 and 2C8 by nilotinib: ↑ repaglinide exposure^9,18,19

Part 1. Alimentary tract and metabolism
	Imatinib	Dasatinib	Nilotinib
PPI
Omeprazole	• Inhibition of Pgp by omeprazole: ↑ imatinib exposure^9,18,64	• ↓ dasatinib absorption⁹ (↓ dasatinib solubility) • Inhibition of Pgp by omeprazole: ↑ dasatinib exposure^9,18,64	—
Esomeprazole	• Inhibition of Pgp by esomeprazole: ↑ imatinib exposure^9,18,64	• ↓ dasatinib absorption⁹ (↓ dasatinib solubility) • Inhibition of Pgp by esomeprazole: ↑ dasatinib exposure^9,18,64	—
Pantoprazole	• Inhibition of Pgp by pantoprazole: ↑ imatinib exposure^9,18,64	• ↓ dasatinib absorption⁹ (↓ dasatinib solubility) • Inhibition of Pgp by pantoprazole: ↑ dasatinib exposure^9,18,64	—
H2-antagonists
Cimetidine	• Inhibition of CYP 3A4 and Pgp by cimetidine: ↑ imatinib exposure^18,65 • Inhibition of hOCT1 by cimetidine: ↓ imatinib intracellular exposure^18,64,65	• ↓ dasatinib absorption⁹ (↓ dasatinib solubility) • Inhibition of CYP 3A4 and Pgp by cimetidine: ↑ dasatinib exposure^18,65	• Inhibition of CYP 3A4 by cimetidine: ↑ nilotinib exposure^18,65
Ranitidine	• Inhibition of Pgp by ranitidine: ↑ imatinib exposure^18,65 • Inhibition of hOCT1 by ranitidine: ↓ imatinib intracellular exposure^9,18,64,65	• ↓ dasatinib absorption⁹ (↓ dasatinib solubility) • Inhibition of Pgp by ranitidine: ↑ dasatinib exposure^18,65	—
Antiemetics
Metoclopramide	—	• ↑ QT interval¹⁹ (additive effect) → monitor ECG	• ↑ QT interval¹⁹ (additive effect) → monitor ECG
Antidiabetic drugs
Insulin	—	—	—
Metformin	• Inhibition of hOCT1 by metformin: ↓ imatinib intracellular exposure^9,18,64	—	—
Glibenclamide	• Inhibition of CYP 3A4 and 2C9 by imatinib: ↑ glibenclamide exposure^9,18,19 • Inhibition of Pgp by glibenclamide: ↑ imatinib exposure^9,18,64	• Inhibition of CYP 3A4 by dasatinib: ↑ glibenclamide exposure^9,18,19 • Inhibition of Pgp by glibenclamide: ↑ dasatinib exposure^9,18,64	• Inhibition of CYP 3A4 and 2C9 by nilotinib: ↑ glibenclamide exposure^9,18,19
Acarbose	—	—	—
Rosiglitazone	• Inhibition of CYP 2C9 by imatinib: ↑ rosiglitazone exposure^9,18,19	—	• Inhibition of CYP 2C9 by nilotinib: ↑ rosiglitazone exposure^9,18,19
Pioglitazone	• Inhibition of CYP 3A4 and 2C9 by imatinib: ↑ pioglitazone exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ pioglitazone exposure^9,18,19	• Inhibition of CYP 3A4 and 2C9 by nilotinib: ↑ pioglitazone exposure^9,18,19
Nateglinide	• Inhibition of CYP 3A4 and 2C9 by imatinib: ↑ nateglinide exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ nateglinide exposure^9,18,19	• Inhibition of CYP 3A4 and 2C9 by nilotinib: ↑ nateglinide exposure^9,18,19
Repaglinide	• Inhibition of CYP 3A4 by imatinib: ↑ repaglinide exposure^9,18,19	• Inhibition of CYP 3A4 and 2C8 by dasatinib: ↑ repaglinide exposure^9,18,19	• Inhibition of CYP 3A4 and 2C8 by nilotinib: ↑ repaglinide exposure^9,18,19

Part 2. Blood and blood-forming organs
	Imatinib	Dasatinib	Nilotinib
Antiplatelet drug*
Clopidogrel	• Inhibition of CYP 3A4 and 2C19 by imatinib: ↑clopidogrel exposure^9,18,19 ↓ clopidogrel bioactivation^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ clopidogrel exposure^9,18,19 ↓ clopidogrel bioactivation^9,18,19 • Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ clopidogrel exposure^9,18,19 ↓ clopidogrel bioactivation^9,18,19
Anticoagulants*
Acenocoumarol	• Inhibition of CYP 2C9 by imatinib: ↑ anticoagulation → monitor PT/INR⁹	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	• Inhibition of CYP 2C9 by nilotinib: ↑ anticoagulation → monitor PT/INR⁹
Phenprocoumon	• Inhibition of CYP 2C9 by imatinib: ↑ anticoagulation → monitor PT/INR⁹	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	• Inhibition of CYP 2C9 by nilotinib: ↑ anticoagulation → monitor PT/INR⁹
Warfarin	• Inhibition of CYP 2C9 by imatinib: ↑ anticoagulation → monitor PT/INR⁹	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	• Inhibition of CYP 2C9 by nilotinib: ↑ anticoagulation → monitor PT/INR⁹
Heparin	• Inhibition of Pgp by heparin: ↑ imatinib exposure⁶⁶	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19 • Inhibition of Pgp by heparin: ↑ dasatinib exposure^{9,10,52,66–68}	—
Enoxaparin	—	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	—
Nadroparin	—	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	—
Dalteparin	—	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	—

Part 2. Blood and blood-forming organs
	Imatinib	Dasatinib	Nilotinib
Antiplatelet drug*
Clopidogrel	• Inhibition of CYP 3A4 and 2C19 by imatinib: ↑clopidogrel exposure^9,18,19 ↓ clopidogrel bioactivation^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ clopidogrel exposure^9,18,19 ↓ clopidogrel bioactivation^9,18,19 • Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ clopidogrel exposure^9,18,19 ↓ clopidogrel bioactivation^9,18,19
Anticoagulants*
Acenocoumarol	• Inhibition of CYP 2C9 by imatinib: ↑ anticoagulation → monitor PT/INR⁹	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	• Inhibition of CYP 2C9 by nilotinib: ↑ anticoagulation → monitor PT/INR⁹
Phenprocoumon	• Inhibition of CYP 2C9 by imatinib: ↑ anticoagulation → monitor PT/INR⁹	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	• Inhibition of CYP 2C9 by nilotinib: ↑ anticoagulation → monitor PT/INR⁹
Warfarin	• Inhibition of CYP 2C9 by imatinib: ↑ anticoagulation → monitor PT/INR⁹	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	• Inhibition of CYP 2C9 by nilotinib: ↑ anticoagulation → monitor PT/INR⁹
Heparin	• Inhibition of Pgp by heparin: ↑ imatinib exposure⁶⁶	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19 • Inhibition of Pgp by heparin: ↑ dasatinib exposure^{9,10,52,66–68}	—
Enoxaparin	—	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	—
Nadroparin	—	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	—
Dalteparin	—	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	—

Part 3. Cardiovascular system
	Imatinib	Dasatinib	Nilotinib
Calcium channel blockers
Verapamil	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ verapamil exposure^{9,23,24,55,69–72} • Inhibition of CYP 3A4 and Pgp by verapamil: ↑ imatinib exposure^24,69,70,72	• Inhibition of CYP 3A4 by dasatinib: ↑ verapamil exposure^9,18 • Inhibition of CYP 3A4 and Pgp by verapamil: ↑ dasatinib exposure^{9,10,52,67,68}	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ verapamil exposure^{9,18,19,25,73} • Inhibition of CYP 3A4 by verapamil: ↑ nilotinib exposure^9,18,19
Diltiazem	• Inhibition of CYP 3A4 by imatinib: ↑ diltiazem exposure^9,18 • Inhibition of CYP 3A4 and Pgp by diltiazem: ↑ imatinib exposure^{9,23,24,55,69–72}	• Inhibition of CYP 3A4 by dasatinib: ↑ diltiazem exposure^9,18 • Inhibition of CYP 3A4 and Pgp by diltiazem: ↑ dasatinib exposure^{9,10,52,67,68}	• Inhibition of CYP 3A4 by nilotinib: ↑ diltiazem exposure^9,18 • Inhibition of CYP 3A4 by diltiazem: ↑ nilotinib exposure^9,18,19
Nifedipine	• Inhibition of CYP 3A4 by imatinib: ↑ nifedipine exposure^9,18,74	• Inhibition of CYP 3A4 by dasatinib: ↑ nifedipine exposure^9,18,74	• Inhibition of CYP3A4 by nilotinib: ↑ nifedipine exposure^9,18,74
Amlodipine	• Inhibition of CYP 3A4 by imatinib: ↑ amlodipine exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ amlodipine exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ amlodipine exposure^9,18,19
NO precursors
Molsidomine	—	—	—
Isosorbid mononitrate (ISMN)	• Inhibition of CYP 3A4 by imatinib: ↑ ISMN exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ ISMN exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ ISMN exposure^9,18,19
Isosorbid dinitrate (ISDN)	• Inhibition of CYP 3A4 by imatinib: ↑ ISDN exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ ISDN exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ ISDN exposure^9,18,19
Nitroglycerine	—	—	—
HMG-CoA reductase inhibitors
Simvastatin	• Inhibition of CYP 3A4 by imatinib: ↑ simvastatin exposure^9,18,19,48 • Inhibition of Pgp by simvastatin: ↑ imatinib exposure^{9,23,24,55,69–72}	• Inhibition of CYP 3A4 by dasatinib: ↑ simvastatin exposure^9,18,19,48 • Inhibition of Pgp by simvastatin: ↑ dasatinib exposure^{9,10,52,67,68}	• Inhibition of CYP 3A4 by nilotinib: ↑ simvastatin exposure^9,18,19
Pravastatin	—	—	—
Atorvastatin	• Inhibition of CYP 3A4 by imatinib: ↑ atorvastatin exposure^9,18,19 • Inhibition of Pgp by atorvastatin: ↑ imatinib exposure^{9,23,24,55,69–72}	• Inhibition of CYP 3A4 by dasatinib: ↑ atorvastatin exposure^9,18,19 • Inhibition of Pgp by atorvastatin: ↑ dasatinib exposure^9,10,67,68	• Inhibition of CYP 3A4 by nilotinib: ↑ atorvastatin exposure^9,18,19
Rosuvastatin	—	—	—
Antiarrhythmic drugs
Amiodarone	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ amiodarone exposure^{9,23,24,69,70,72,75} • Inhibition of CYP3A4 and Pgp by amiodarone: ↑ imatinib exposure^{9,23,24,69,70,72,75} • Inhibition of hOCT1 by amiodarone: ↓ imatinib intracellular exposure^9,18,64	• Inhibition of CYP 3A4 by dasatinib: ↑ amiodarone exposure^{9,23,24,69,70,72,75} • Inhibition of CYP 3A4 and Pgp by amiodarone: ↑ dasatinib exposure^{9,10,67,68,75} • ↑ QT interval¹⁹ (additive effect) → monitor ECG	• Inhibition of Pgp and CYP 3A4 by nilotinib: ↑ amiodarone exposure^{9,18,19,25,73} • Inhibition of CYP 3A4 by amiodarone: ↑ nilotinib exposure^9,18,19 • ↑ QT interval¹⁹ (additive effect) → monitor ECG
Quinidine	• Inhibition of CYP 3A4 by imatinib: ↑ quinidine exposure^9,18,19 • Inhibition of Pgp by quinidine: ↑ imatinib exposure^{9,23,24,55,69–72} • Inhibition of hOCT1 by quinidine: ↓ imatinib intracellular exposure^9,18,65	• Inhibition of CYP 3A4 by dasatinib: ↑ quinidine exposure^9,18,19 • Inhibition of Pgp by quinidine: ↑ dasatinib exposure^9,18,19 • ↑ QT interval¹⁹ (additive effect) → monitor ECG	• Inhibition of CYP 3A4 by nilotinib: ↑ quinidine exposure^9,18,19 • ↑ QT interval¹⁹ (additive effect) → monitor ECG
Diuretics
Furosemide	• Absence of interaction⁷⁶	—	—
Torasemide	• Inhibition of CYP 2C9 by imatinib: ↑ torasemide exposure^9,18	—	• Inhibition of CYP 2C9 by nilotinib: ↑ torasemide exposure^9,18
Hydrochlorothiazide	—	—	—
Spironolactone	• Inhibition of Pgp by spironolactone: ↑ imatinib exposure^9,64	• Inhibition of Pgp by spironolactone: ↑ dasatinib exposure^{9,10,52,64,67}	—
Beta blockers
Metoprolol	• Inhibition of CYP 2D6 by imatinib: ↑ metoprolol exposure¹⁸	• Inhibition of Pgp by metoprolol: ↑ dasatinib exposure^9,10,52,67	• Inhibition of CYP 2D6 by nilotinib: ↑ metoprolol exposure^9,18,19
Bisoprolol	• Inhibition of CYP 2D6 by imatinib: ↑ bisoprolol exposure¹⁸	• Inhibition of CYP 3A4 by dasatinib: ↑ bisoprolol exposure^9,18	• Inhibition of CYP 2D6 by nilotinib: ↑ bisoprolol exposure^9,18,19
Carvedilol	• Inhibition of CYP 2C9 and 2D6 by imatinib: ↑ carvedilol exposure¹⁸ • Inhibition of Pgp by carvedilol: ↑ imatinib exposure^64,71,77	• Inhibition of Pgp by carvedilol: ↑ dasatinib exposure^{9,10,52,67,68,77}	• Inhibition of CYP 2C9 and 2D6 by nilotinib: ↑ carvedilol exposure^9,18,19
Atenolol	• Absence of interaction⁹	—	—
ACE inhibitors
Captopril	• Inhibition of CYP 2D6 by imatinib: ↑ captopril exposure¹⁸ • Inhibition of Pgp by captopril: ↑ imatinib exposure^{9,18,23,64,70,72}	• Inhibition of Pgp by captopril: ↑ dasatinib exposure^9,10,52,67	• Inhibition of CYP 2D6 by nilotinib: ↑ captopril exposure^9,18,19
Enalapril	• Inhibition of CYP 3A4 by imatinib: ↑ enalapril exposure¹⁸ • Inhibition of Pgp by enalapril: ↑ imatinib exposure^{9,18,23,64,70,72}	• Inhibition of Pgp by enalapril: ↑ dasatinib exposure^9,10,52,67	• Inhibition of CYP 3A4 by nilotinib: ↑ enalapril exposure^9,18,19
Ramipril	—	—	—
Lisinopril	• Inhibition of Pgp by imatinib: ↑ lisinopril exposure^{9,18,23,64,70,72} • Inhibition of Pgp by lisinopril: ↑ imatinib exposure⁹	• Inhibition of Pgp by lisinopril: ↑ dasatinib exposure^9,10,52,67	—
AT II receptor blockers
Losartan	• Inhibition of CYP 2C9 and 3A4 by imatinib: losartan exposure and ↓ losartan bioactivation^9,18,19 • Inhibition of Pgp by losartan: ↑ imatinib exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ losartan exposure^9,18 • Inhibition of Pgp by losartan: ↑ dasatinib exposure^9,10,52,67	• Inhibition of CYP 2C9 and 3A4 by nilotinib: ↑ losartan exposure and ↓ losartan bioactivation^9,18,19
Candesartan	—	—	—
Cardiac glycosides
Digoxin	• ↓ digoxin absorption^9,18,19 (unknown mechanism)	• ↑ QT interval¹⁹ (additive effect) → monitor ECG	• ↑ QT interval¹⁹ (additive effect) → monitor ECG • Inhibition of Pgp by nilotinib: ↑ digoxin exposure^9,18,19

Part 3. Cardiovascular system
	Imatinib	Dasatinib	Nilotinib
Calcium channel blockers
Verapamil	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ verapamil exposure^{9,23,24,55,69–72} • Inhibition of CYP 3A4 and Pgp by verapamil: ↑ imatinib exposure^24,69,70,72	• Inhibition of CYP 3A4 by dasatinib: ↑ verapamil exposure^9,18 • Inhibition of CYP 3A4 and Pgp by verapamil: ↑ dasatinib exposure^{9,10,52,67,68}	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ verapamil exposure^{9,18,19,25,73} • Inhibition of CYP 3A4 by verapamil: ↑ nilotinib exposure^9,18,19
Diltiazem	• Inhibition of CYP 3A4 by imatinib: ↑ diltiazem exposure^9,18 • Inhibition of CYP 3A4 and Pgp by diltiazem: ↑ imatinib exposure^{9,23,24,55,69–72}	• Inhibition of CYP 3A4 by dasatinib: ↑ diltiazem exposure^9,18 • Inhibition of CYP 3A4 and Pgp by diltiazem: ↑ dasatinib exposure^{9,10,52,67,68}	• Inhibition of CYP 3A4 by nilotinib: ↑ diltiazem exposure^9,18 • Inhibition of CYP 3A4 by diltiazem: ↑ nilotinib exposure^9,18,19
Nifedipine	• Inhibition of CYP 3A4 by imatinib: ↑ nifedipine exposure^9,18,74	• Inhibition of CYP 3A4 by dasatinib: ↑ nifedipine exposure^9,18,74	• Inhibition of CYP3A4 by nilotinib: ↑ nifedipine exposure^9,18,74
Amlodipine	• Inhibition of CYP 3A4 by imatinib: ↑ amlodipine exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ amlodipine exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ amlodipine exposure^9,18,19
NO precursors
Molsidomine	—	—	—
Isosorbid mononitrate (ISMN)	• Inhibition of CYP 3A4 by imatinib: ↑ ISMN exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ ISMN exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ ISMN exposure^9,18,19
Isosorbid dinitrate (ISDN)	• Inhibition of CYP 3A4 by imatinib: ↑ ISDN exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ ISDN exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ ISDN exposure^9,18,19
Nitroglycerine	—	—	—
HMG-CoA reductase inhibitors
Simvastatin	• Inhibition of CYP 3A4 by imatinib: ↑ simvastatin exposure^9,18,19,48 • Inhibition of Pgp by simvastatin: ↑ imatinib exposure^{9,23,24,55,69–72}	• Inhibition of CYP 3A4 by dasatinib: ↑ simvastatin exposure^9,18,19,48 • Inhibition of Pgp by simvastatin: ↑ dasatinib exposure^{9,10,52,67,68}	• Inhibition of CYP 3A4 by nilotinib: ↑ simvastatin exposure^9,18,19
Pravastatin	—	—	—
Atorvastatin	• Inhibition of CYP 3A4 by imatinib: ↑ atorvastatin exposure^9,18,19 • Inhibition of Pgp by atorvastatin: ↑ imatinib exposure^{9,23,24,55,69–72}	• Inhibition of CYP 3A4 by dasatinib: ↑ atorvastatin exposure^9,18,19 • Inhibition of Pgp by atorvastatin: ↑ dasatinib exposure^9,10,67,68	• Inhibition of CYP 3A4 by nilotinib: ↑ atorvastatin exposure^9,18,19
Rosuvastatin	—	—	—
Antiarrhythmic drugs
Amiodarone	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ amiodarone exposure^{9,23,24,69,70,72,75} • Inhibition of CYP3A4 and Pgp by amiodarone: ↑ imatinib exposure^{9,23,24,69,70,72,75} • Inhibition of hOCT1 by amiodarone: ↓ imatinib intracellular exposure^9,18,64	• Inhibition of CYP 3A4 by dasatinib: ↑ amiodarone exposure^{9,23,24,69,70,72,75} • Inhibition of CYP 3A4 and Pgp by amiodarone: ↑ dasatinib exposure^{9,10,67,68,75} • ↑ QT interval¹⁹ (additive effect) → monitor ECG	• Inhibition of Pgp and CYP 3A4 by nilotinib: ↑ amiodarone exposure^{9,18,19,25,73} • Inhibition of CYP 3A4 by amiodarone: ↑ nilotinib exposure^9,18,19 • ↑ QT interval¹⁹ (additive effect) → monitor ECG
Quinidine	• Inhibition of CYP 3A4 by imatinib: ↑ quinidine exposure^9,18,19 • Inhibition of Pgp by quinidine: ↑ imatinib exposure^{9,23,24,55,69–72} • Inhibition of hOCT1 by quinidine: ↓ imatinib intracellular exposure^9,18,65	• Inhibition of CYP 3A4 by dasatinib: ↑ quinidine exposure^9,18,19 • Inhibition of Pgp by quinidine: ↑ dasatinib exposure^9,18,19 • ↑ QT interval¹⁹ (additive effect) → monitor ECG	• Inhibition of CYP 3A4 by nilotinib: ↑ quinidine exposure^9,18,19 • ↑ QT interval¹⁹ (additive effect) → monitor ECG
Diuretics
Furosemide	• Absence of interaction⁷⁶	—	—
Torasemide	• Inhibition of CYP 2C9 by imatinib: ↑ torasemide exposure^9,18	—	• Inhibition of CYP 2C9 by nilotinib: ↑ torasemide exposure^9,18
Hydrochlorothiazide	—	—	—
Spironolactone	• Inhibition of Pgp by spironolactone: ↑ imatinib exposure^9,64	• Inhibition of Pgp by spironolactone: ↑ dasatinib exposure^{9,10,52,64,67}	—
Beta blockers
Metoprolol	• Inhibition of CYP 2D6 by imatinib: ↑ metoprolol exposure¹⁸	• Inhibition of Pgp by metoprolol: ↑ dasatinib exposure^9,10,52,67	• Inhibition of CYP 2D6 by nilotinib: ↑ metoprolol exposure^9,18,19
Bisoprolol	• Inhibition of CYP 2D6 by imatinib: ↑ bisoprolol exposure¹⁸	• Inhibition of CYP 3A4 by dasatinib: ↑ bisoprolol exposure^9,18	• Inhibition of CYP 2D6 by nilotinib: ↑ bisoprolol exposure^9,18,19
Carvedilol	• Inhibition of CYP 2C9 and 2D6 by imatinib: ↑ carvedilol exposure¹⁸ • Inhibition of Pgp by carvedilol: ↑ imatinib exposure^64,71,77	• Inhibition of Pgp by carvedilol: ↑ dasatinib exposure^{9,10,52,67,68,77}	• Inhibition of CYP 2C9 and 2D6 by nilotinib: ↑ carvedilol exposure^9,18,19
Atenolol	• Absence of interaction⁹	—	—
ACE inhibitors
Captopril	• Inhibition of CYP 2D6 by imatinib: ↑ captopril exposure¹⁸ • Inhibition of Pgp by captopril: ↑ imatinib exposure^{9,18,23,64,70,72}	• Inhibition of Pgp by captopril: ↑ dasatinib exposure^9,10,52,67	• Inhibition of CYP 2D6 by nilotinib: ↑ captopril exposure^9,18,19
Enalapril	• Inhibition of CYP 3A4 by imatinib: ↑ enalapril exposure¹⁸ • Inhibition of Pgp by enalapril: ↑ imatinib exposure^{9,18,23,64,70,72}	• Inhibition of Pgp by enalapril: ↑ dasatinib exposure^9,10,52,67	• Inhibition of CYP 3A4 by nilotinib: ↑ enalapril exposure^9,18,19
Ramipril	—	—	—
Lisinopril	• Inhibition of Pgp by imatinib: ↑ lisinopril exposure^{9,18,23,64,70,72} • Inhibition of Pgp by lisinopril: ↑ imatinib exposure⁹	• Inhibition of Pgp by lisinopril: ↑ dasatinib exposure^9,10,52,67	—
AT II receptor blockers
Losartan	• Inhibition of CYP 2C9 and 3A4 by imatinib: losartan exposure and ↓ losartan bioactivation^9,18,19 • Inhibition of Pgp by losartan: ↑ imatinib exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ losartan exposure^9,18 • Inhibition of Pgp by losartan: ↑ dasatinib exposure^9,10,52,67	• Inhibition of CYP 2C9 and 3A4 by nilotinib: ↑ losartan exposure and ↓ losartan bioactivation^9,18,19
Candesartan	—	—	—
Cardiac glycosides
Digoxin	• ↓ digoxin absorption^9,18,19 (unknown mechanism)	• ↑ QT interval¹⁹ (additive effect) → monitor ECG	• ↑ QT interval¹⁹ (additive effect) → monitor ECG • Inhibition of Pgp by nilotinib: ↑ digoxin exposure^9,18,19

Part 4. Hormonal preparations
	Imatinib	Dasatinib	Nilotinib
Corticosteroids
Prednisone	—	—	—
Dexamethasone	• Induction of CYP 3A4 by dexamethasone: ↓ imatinib exposure¹⁹	• Induction of CYP 3A4 by dexamethasone: ↓ dasatinib exposure¹⁹	• Induction of CYP 3A4 by dexamethasone: ↓ nilotinib exposure^9,18,19
Betamethasone	—	—	—
Thyroid therapy
Levothyroxine	• Induction of UGTs by imatinib: ↓ levothyroxine^31,32 • Inhibition of CYP 3A4 by levothyroxine: ↑ imatinib exposure^31,32	• Inhibition of CYP 3A4 by levothyroxine: ↑ dasatinib exposure^9,19	• Inhibition of CYP 3A4 by levothyroxine: ↑ nilotinib exposure^9,19
Carbimazole	—	—	—
Antineoplastic agents
Cyclophosphamide	• Inhibition of CYP 2D6 and 3A4 by imatinib: ↑ cyclophosphamide exposure ↓ cyclophosphamide bioactivation^9,19	• Inhibition of CYP 3A4 by dasatinib: ↑ cyclophosphamide exposure ↓ cyclophosphamide bioactivation^9,19	• Induction of CYP 2B6 by nilotinib: ↓ cyclophosphamide exposure ↑ cyclophosphamide bioactivation¹⁹ • Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ cyclophosphamide exposure^9,19 ↓ cyclophosphamide bioactivation¹⁹
Antiestrogen agent
Tamoxifen	• Inhibition of CYP 2D6 and 3A4 by imatinib: ↑ tamoxifen exposure ↓ tamoxifen bioactivation^18,78	• Inhibition of CYP 3A4 by dasatinib: ↑ tamoxifen exposure ↓ tamoxifen bioactivation^18,78	• Inhibition of CYP 2D6 and 3A4 by nilotinib: ↑ tamoxifen exposure ↓ tamoxifen bioactivation^18,78

Part 4. Hormonal preparations
	Imatinib	Dasatinib	Nilotinib
Corticosteroids
Prednisone	—	—	—
Dexamethasone	• Induction of CYP 3A4 by dexamethasone: ↓ imatinib exposure¹⁹	• Induction of CYP 3A4 by dexamethasone: ↓ dasatinib exposure¹⁹	• Induction of CYP 3A4 by dexamethasone: ↓ nilotinib exposure^9,18,19
Betamethasone	—	—	—
Thyroid therapy
Levothyroxine	• Induction of UGTs by imatinib: ↓ levothyroxine^31,32 • Inhibition of CYP 3A4 by levothyroxine: ↑ imatinib exposure^31,32	• Inhibition of CYP 3A4 by levothyroxine: ↑ dasatinib exposure^9,19	• Inhibition of CYP 3A4 by levothyroxine: ↑ nilotinib exposure^9,19
Carbimazole	—	—	—
Antineoplastic agents
Cyclophosphamide	• Inhibition of CYP 2D6 and 3A4 by imatinib: ↑ cyclophosphamide exposure ↓ cyclophosphamide bioactivation^9,19	• Inhibition of CYP 3A4 by dasatinib: ↑ cyclophosphamide exposure ↓ cyclophosphamide bioactivation^9,19	• Induction of CYP 2B6 by nilotinib: ↓ cyclophosphamide exposure ↑ cyclophosphamide bioactivation¹⁹ • Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ cyclophosphamide exposure^9,19 ↓ cyclophosphamide bioactivation¹⁹
Antiestrogen agent
Tamoxifen	• Inhibition of CYP 2D6 and 3A4 by imatinib: ↑ tamoxifen exposure ↓ tamoxifen bioactivation^18,78	• Inhibition of CYP 3A4 by dasatinib: ↑ tamoxifen exposure ↓ tamoxifen bioactivation^18,78	• Inhibition of CYP 2D6 and 3A4 by nilotinib: ↑ tamoxifen exposure ↓ tamoxifen bioactivation^18,78

Part 5. Anti-infectives
	Imatinib	Dasatinib	Nilotinib
Penicillins
Amoxicillin	—	—	—
Flucloxacillin	—	—	—
Cephalosporins
Céfuroxime	—	—	—
Cefpodoxime	—	—	—
Ceftriaxone	—	—	—
Macrolides
Clarithromycin	• Inhibition of CYP 3A4 and Pgp by clarithromycin: ↑ imatinib exposure^9,18,19,36	• Inhibition of CYP 3A4 and Pgp by clarithromycin: ↑ dasatinib exposure^9,18,19	• Inhibition of CYP 3A4 by clarithromycin: ↑ nilotinib exposure^9,18,19
Azithromycin	—	—	—
Erythromycin	• Inhibition of CYP 3A4 and Pgp by erythromycin: ↑ imatinib exposure^9,18,19,36	• Inhibition of CYP 3A4 and Pgp by erythromycin: ↑ dasatinib exposure^9,18,19	• Inhibition of CYP 3A4 by erythromycin: ↑ nilotinib exposure^9,18,19
Tetracyclines
Doxycyclin	—	—	—
Quinolones
Ciprofloxacin	• Inhibition of Pgp by ciprofloxacin: ↑ imatinib exposure^{9,18,23,64,70,72}	• ↑ QT interval^18,19 (additive effect) → monitor ECG • Inhibition of Pgp by ciprofloxacin: ↑ dasatinib exposure^{9,10,52,67,68}	• ↑ QT interval^18,19 (additive effect) → monitor ECG
Levofloxacin	• Inhibition of Pgp by levofloxacin: ↑ imatinib exposure^{9,18,23,64,70,72} • Inhibition of hOCT1 by levofloxacine: ↓ imatinib intracellular exposure^9,18,64	• ↑ QT interval^18,19 (additive effect) → monitor ECG • Inhibition of Pgp by levofloxacin: ↑ dasatinib exposure^{9,10,52,67,68}	• ↑ QT interval^18,19 (additive effect) → monitor ECG
Norfloxacin	—	• ↑ QT interval^18,19 (additive effect) → monitor ECG	• ↑ QT interval^18,19 (additive effect) → monitor ECG
Sulfonamides
Co-trimoxazole	• Inhibition of CYP 2C9 by imatinib: ↑ co-trimoxazole^9,18,19	—	• Inhibition of CYP 2C9 by nilotinib: ↑ co-trimoxazole^9,18,19
Azoles
Itraconazole	• Inhibition of CYP 3A4 and Pgp by itraconazole: ↑ imatinib exposure^9,18,19	• Inhibition of CYP 3A4 and Pgp by itraconazole: ↑ dasatinib exposure^9,18,19	• Inhibition of CYP 3A4 by itraconazole: ↑ nilotinib exposure^9,18,19
Fluconazole	• Inhibition of CYP 3A4 and Pgp by fluconazole: ↑ imatinib exposure^9,18,19	• Inhibition of CYP 3A4 and Pgp by fluconazole: ↑ dasatinib exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• Inhibition of CYP 3A4 by fluconazole: ↑ nilotinib exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG
Voriconazole	• Inhibition of CYP 3A4 by voriconazole: ↑ imatinib exposure^9,18,19,33	• Inhibition of CYP 3A4 by voriconazole: ↑ dasatinib exposure^9,18,19 • ↑ QT interval (additive effect) → monitor ECG	• Inhibition of CYP 3A4 by voriconazole: ↑ nilotinib exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG
Ketoconazole	• Inhibition of CYP 3A4 and Pgp by ketoconazole: ↑ imatinib exposure^9,18,19,30	• Inhibition of CYP 3A4 and Pgp by ketoconazole: ↑ dasatinib exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• Inhibition of CYP 3A4 by ketoconazole: ↑ nilotinib exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG
Allylamine
Terbinafine	• Inhibition of CYP 3A4 and 2C9 by imatinib: ↑ terbinafine exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ terbinafine exposure^9,18,19	• Inhibition of CYP 3A4 and 2C9 by nilotinib: ↑ terbinafine exposure^9,18,19
Nitroimidazole
Metronidazole	—	—	—
Antiviral/nucleoside analog
Aciclovir	• Absence of interaction⁷⁹	—	—
Valaciclovir	• Absence of interaction⁷⁹	—	—
Ganciclovir	• Inhibition of hOCT1 by ganciclovir: ↓ imatinib intracellular exposure^9,18,19	—	—
Valganciclovir	• Inhibition of hOCT1 by ganciclovir: ↓ imatinib intracellular exposure^9,18,19	—	—
Antimycobacterials
Rifampicine	• Induction of CYP 3A4 by rifampicine: ↓ imatinib exposure^9,18,80	• Induction of CYP 3A4 by rifampicine: ↓ dasatinib exposure^9,18,19	• Induction of CYP 3A4 by rifampicine: ↓ nilotinib exposure^9,18,19
Isoniazide	—	—	—
Ethambutol	—	—	—
Protease inhibitors
Ritonavir	• Inhibition of CYP 3A4 and Pgp by ritonavir: ↑ imatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 and Pgp by ritonavir: ↑ dasatinib exposure^9,18,19,81 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• Inhibition of CYP 3A4 by ritonavir: ↑ nilotinib exposure^9,18,19,81 • ↑ QT interval^18,19 (additive effect) → monitor ECG
Saquinavir	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ saquinavir exposure^9,18,19,81 • Inhibition of hOCT1 by saquinavir: ↓ imatinib intracellular exposure^9,18,64	• Inhibition of CYP 3A4 by dasatinib: ↑ saquinavir exposure^9,18,19,81	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ saquinavir exposure^9,18,19,81
Darunavir	• Inhibition of CYP 3A4 by darunavir: ↑ imatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by darunavir: ↑ dasatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by darunavir: ↑ nilotinib exposure^9,18,19,81
Atazanavir	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ atazanavir exposure^9,18,19,81	• Inhibition of CYP 3A4 by dasatinib: ↑ atazanavir exposure^9,18,19,81	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ atazanavir exposure^9,18,19,81
Lopinavir	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ lopinavir exposure^9,18,19,81 • Inhibition of CYP 3A4 and Pgp by lopinavir/ritonavir*: ↑ imatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by dasatinib: ↑ lopinavir exposure^9,18,19,81 • Inhibition of CYP 3A4 and Pgp by lopinavir/ritonavir*: ↑ dasatinib exposure^9.18.19.81	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ lopinavir exposure^9,18,19,81 • Inhibition of CYP 3A4 by lopinavir/ritonavir*: ↑ nilotinib exposure^9,18,19,81
Indinavir	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ indinavir exposure^9,18,19,81 • Inhibition of hOCT1 by indinavir: ↓ imatinib intracellular exposure^9,18,64	• Inhibition of CYP 3A4 by dasatinib: ↑ indinavir exposure^9,18,19,81	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ indinavir exposure^9,18,19,81
Nucleoside and nucleotide reverse transcriptase inhibitors
Lamivudine	• Inhibition of hOCT1 by lamivudine: ↓ imatinib intracellular exposure^9,18,64	—	—
Emtricitabine	—	—	—
Zidovudine	—	—	—
Non-nucleoside reverse transcriptase inhibitors
Efavirenz	• Inhibition of CYP 3A4 by imatinib: ↑ efavirenz exposure^9,18,19,81 • Induction of CYP 3A4 by efavirenz: ↓ imatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by dasatinib: ↑ efavirenz exposure^9,18,19,81 • Induction of CYP 3A4 by efavirenz: ↓ dasatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by nilotinib: ↑ efavirenz exposure^9,18,19,81 • Induction of CYP 3A4 by efavirenz: ↓ nilotinib exposure^9,18,19,81
Nevirapine	• Inhibition of CYP 3A4 by imatinib: ↑ nevirapine exposure^9,18,19,81 • Induction of CYP 3A4 by nevirapine: ↓ imatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by dasatinib: ↑ nevirapine exposure^9,18,19,81 • Induction of CYP 3A4 by nevirapine: ↓ dasatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by nilotinib: ↑ nevirapine exposure^9,18,19,81 • Induction of CYP 3A4 by nevirapine: ↓ nilotinib exposure^9,18,19,81
Etravirine	• Inhibition of CYP 2C9 and 3A4 by imatinib: ↑ etravirine exposure^9,18,19,81 • Induction of CYP 3A4 by etravirine: ↓ imatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by dasatinib: ↑ etravirine exposure^9,18,19,81 • Induction of CYP 3A4 by etravirine: ↓ dasatinib exposure^9,18,19,81	• Inhibition of CYP 2C9 and 3A4 by nilotinib: ↑ etravirine exposure^9,18,19,81 • Induction of CYP 3A4 by etravirine: ↓ nilotinib exposure^9,18,19,81
Antimalarial drugs
Quinine	• Inhibition of CYP 3A4 by imatinib: ↑ quinine exposure^9,18,19 • Inhibition of CYP 2D6 and Pgp by quinine: ↑ imatinib exposure^9,18,19 • Inhibition of hOCT1 by quinine: ↓ imatinib intracellular exposure^9,18,64	• Inhibition of CYP 3A4 by dasatinib: ↑ quinine exposure^9,18,19 • Inhibition of CYP 3A4 by dasatinib: ↑ quinine exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• Inhibition of CYP 3A4 by nilotinib: ↑ quinine exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG
Chloroquine	• Inhibition of Pgp by chloroquine: ↑ imatinib exposure^9,18,19 • Inhibition of hOCT1 by chloroquine: ↓ imatinib intracellular exposure^9,18,64	• Inhibition of Pgp by chloroquine: ↑ dasatinib exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• ↑ QT interval^18,19 (additive effect) → monitor ECG
Mefloquine	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ mefloquine exposure^9,18,19 • Inhibition of Pgp by mefloquine: ↑ imatinib exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ mefloquine exposure^9,18,19 • Inhibition of Pgp by mefloquine: ↑ dasatinib exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• Inhibition of CYP 3A4 and Ppg by nilotinib: ↑ mefloquine exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG
Proguanil	• Inhibition of CYP 2C19 and Pgp by imatinib: ↑ proguanil exposure ↓ proguanil bioactivation^9,18,19	—	—
Atovaquone	—	—	—
Doxycycline	—	—	—

Part 5. Anti-infectives
	Imatinib	Dasatinib	Nilotinib
Penicillins
Amoxicillin	—	—	—
Flucloxacillin	—	—	—
Cephalosporins
Céfuroxime	—	—	—
Cefpodoxime	—	—	—
Ceftriaxone	—	—	—
Macrolides
Clarithromycin	• Inhibition of CYP 3A4 and Pgp by clarithromycin: ↑ imatinib exposure^9,18,19,36	• Inhibition of CYP 3A4 and Pgp by clarithromycin: ↑ dasatinib exposure^9,18,19	• Inhibition of CYP 3A4 by clarithromycin: ↑ nilotinib exposure^9,18,19
Azithromycin	—	—	—
Erythromycin	• Inhibition of CYP 3A4 and Pgp by erythromycin: ↑ imatinib exposure^9,18,19,36	• Inhibition of CYP 3A4 and Pgp by erythromycin: ↑ dasatinib exposure^9,18,19	• Inhibition of CYP 3A4 by erythromycin: ↑ nilotinib exposure^9,18,19
Tetracyclines
Doxycyclin	—	—	—
Quinolones
Ciprofloxacin	• Inhibition of Pgp by ciprofloxacin: ↑ imatinib exposure^{9,18,23,64,70,72}	• ↑ QT interval^18,19 (additive effect) → monitor ECG • Inhibition of Pgp by ciprofloxacin: ↑ dasatinib exposure^{9,10,52,67,68}	• ↑ QT interval^18,19 (additive effect) → monitor ECG
Levofloxacin	• Inhibition of Pgp by levofloxacin: ↑ imatinib exposure^{9,18,23,64,70,72} • Inhibition of hOCT1 by levofloxacine: ↓ imatinib intracellular exposure^9,18,64	• ↑ QT interval^18,19 (additive effect) → monitor ECG • Inhibition of Pgp by levofloxacin: ↑ dasatinib exposure^{9,10,52,67,68}	• ↑ QT interval^18,19 (additive effect) → monitor ECG
Norfloxacin	—	• ↑ QT interval^18,19 (additive effect) → monitor ECG	• ↑ QT interval^18,19 (additive effect) → monitor ECG
Sulfonamides
Co-trimoxazole	• Inhibition of CYP 2C9 by imatinib: ↑ co-trimoxazole^9,18,19	—	• Inhibition of CYP 2C9 by nilotinib: ↑ co-trimoxazole^9,18,19
Azoles
Itraconazole	• Inhibition of CYP 3A4 and Pgp by itraconazole: ↑ imatinib exposure^9,18,19	• Inhibition of CYP 3A4 and Pgp by itraconazole: ↑ dasatinib exposure^9,18,19	• Inhibition of CYP 3A4 by itraconazole: ↑ nilotinib exposure^9,18,19
Fluconazole	• Inhibition of CYP 3A4 and Pgp by fluconazole: ↑ imatinib exposure^9,18,19	• Inhibition of CYP 3A4 and Pgp by fluconazole: ↑ dasatinib exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• Inhibition of CYP 3A4 by fluconazole: ↑ nilotinib exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG
Voriconazole	• Inhibition of CYP 3A4 by voriconazole: ↑ imatinib exposure^9,18,19,33	• Inhibition of CYP 3A4 by voriconazole: ↑ dasatinib exposure^9,18,19 • ↑ QT interval (additive effect) → monitor ECG	• Inhibition of CYP 3A4 by voriconazole: ↑ nilotinib exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG
Ketoconazole	• Inhibition of CYP 3A4 and Pgp by ketoconazole: ↑ imatinib exposure^9,18,19,30	• Inhibition of CYP 3A4 and Pgp by ketoconazole: ↑ dasatinib exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• Inhibition of CYP 3A4 by ketoconazole: ↑ nilotinib exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG
Allylamine
Terbinafine	• Inhibition of CYP 3A4 and 2C9 by imatinib: ↑ terbinafine exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ terbinafine exposure^9,18,19	• Inhibition of CYP 3A4 and 2C9 by nilotinib: ↑ terbinafine exposure^9,18,19
Nitroimidazole
Metronidazole	—	—	—
Antiviral/nucleoside analog
Aciclovir	• Absence of interaction⁷⁹	—	—
Valaciclovir	• Absence of interaction⁷⁹	—	—
Ganciclovir	• Inhibition of hOCT1 by ganciclovir: ↓ imatinib intracellular exposure^9,18,19	—	—
Valganciclovir	• Inhibition of hOCT1 by ganciclovir: ↓ imatinib intracellular exposure^9,18,19	—	—
Antimycobacterials
Rifampicine	• Induction of CYP 3A4 by rifampicine: ↓ imatinib exposure^9,18,80	• Induction of CYP 3A4 by rifampicine: ↓ dasatinib exposure^9,18,19	• Induction of CYP 3A4 by rifampicine: ↓ nilotinib exposure^9,18,19
Isoniazide	—	—	—
Ethambutol	—	—	—
Protease inhibitors
Ritonavir	• Inhibition of CYP 3A4 and Pgp by ritonavir: ↑ imatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 and Pgp by ritonavir: ↑ dasatinib exposure^9,18,19,81 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• Inhibition of CYP 3A4 by ritonavir: ↑ nilotinib exposure^9,18,19,81 • ↑ QT interval^18,19 (additive effect) → monitor ECG
Saquinavir	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ saquinavir exposure^9,18,19,81 • Inhibition of hOCT1 by saquinavir: ↓ imatinib intracellular exposure^9,18,64	• Inhibition of CYP 3A4 by dasatinib: ↑ saquinavir exposure^9,18,19,81	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ saquinavir exposure^9,18,19,81
Darunavir	• Inhibition of CYP 3A4 by darunavir: ↑ imatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by darunavir: ↑ dasatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by darunavir: ↑ nilotinib exposure^9,18,19,81
Atazanavir	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ atazanavir exposure^9,18,19,81	• Inhibition of CYP 3A4 by dasatinib: ↑ atazanavir exposure^9,18,19,81	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ atazanavir exposure^9,18,19,81
Lopinavir	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ lopinavir exposure^9,18,19,81 • Inhibition of CYP 3A4 and Pgp by lopinavir/ritonavir*: ↑ imatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by dasatinib: ↑ lopinavir exposure^9,18,19,81 • Inhibition of CYP 3A4 and Pgp by lopinavir/ritonavir*: ↑ dasatinib exposure^9.18.19.81	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ lopinavir exposure^9,18,19,81 • Inhibition of CYP 3A4 by lopinavir/ritonavir*: ↑ nilotinib exposure^9,18,19,81
Indinavir	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ indinavir exposure^9,18,19,81 • Inhibition of hOCT1 by indinavir: ↓ imatinib intracellular exposure^9,18,64	• Inhibition of CYP 3A4 by dasatinib: ↑ indinavir exposure^9,18,19,81	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ indinavir exposure^9,18,19,81
Nucleoside and nucleotide reverse transcriptase inhibitors
Lamivudine	• Inhibition of hOCT1 by lamivudine: ↓ imatinib intracellular exposure^9,18,64	—	—
Emtricitabine	—	—	—
Zidovudine	—	—	—
Non-nucleoside reverse transcriptase inhibitors
Efavirenz	• Inhibition of CYP 3A4 by imatinib: ↑ efavirenz exposure^9,18,19,81 • Induction of CYP 3A4 by efavirenz: ↓ imatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by dasatinib: ↑ efavirenz exposure^9,18,19,81 • Induction of CYP 3A4 by efavirenz: ↓ dasatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by nilotinib: ↑ efavirenz exposure^9,18,19,81 • Induction of CYP 3A4 by efavirenz: ↓ nilotinib exposure^9,18,19,81
Nevirapine	• Inhibition of CYP 3A4 by imatinib: ↑ nevirapine exposure^9,18,19,81 • Induction of CYP 3A4 by nevirapine: ↓ imatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by dasatinib: ↑ nevirapine exposure^9,18,19,81 • Induction of CYP 3A4 by nevirapine: ↓ dasatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by nilotinib: ↑ nevirapine exposure^9,18,19,81 • Induction of CYP 3A4 by nevirapine: ↓ nilotinib exposure^9,18,19,81
Etravirine	• Inhibition of CYP 2C9 and 3A4 by imatinib: ↑ etravirine exposure^9,18,19,81 • Induction of CYP 3A4 by etravirine: ↓ imatinib exposure^9,18,19,81	• Inhibition of CYP 3A4 by dasatinib: ↑ etravirine exposure^9,18,19,81 • Induction of CYP 3A4 by etravirine: ↓ dasatinib exposure^9,18,19,81	• Inhibition of CYP 2C9 and 3A4 by nilotinib: ↑ etravirine exposure^9,18,19,81 • Induction of CYP 3A4 by etravirine: ↓ nilotinib exposure^9,18,19,81
Antimalarial drugs
Quinine	• Inhibition of CYP 3A4 by imatinib: ↑ quinine exposure^9,18,19 • Inhibition of CYP 2D6 and Pgp by quinine: ↑ imatinib exposure^9,18,19 • Inhibition of hOCT1 by quinine: ↓ imatinib intracellular exposure^9,18,64	• Inhibition of CYP 3A4 by dasatinib: ↑ quinine exposure^9,18,19 • Inhibition of CYP 3A4 by dasatinib: ↑ quinine exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• Inhibition of CYP 3A4 by nilotinib: ↑ quinine exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG
Chloroquine	• Inhibition of Pgp by chloroquine: ↑ imatinib exposure^9,18,19 • Inhibition of hOCT1 by chloroquine: ↓ imatinib intracellular exposure^9,18,64	• Inhibition of Pgp by chloroquine: ↑ dasatinib exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• ↑ QT interval^18,19 (additive effect) → monitor ECG
Mefloquine	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ mefloquine exposure^9,18,19 • Inhibition of Pgp by mefloquine: ↑ imatinib exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ mefloquine exposure^9,18,19 • Inhibition of Pgp by mefloquine: ↑ dasatinib exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• Inhibition of CYP 3A4 and Ppg by nilotinib: ↑ mefloquine exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG
Proguanil	• Inhibition of CYP 2C19 and Pgp by imatinib: ↑ proguanil exposure ↓ proguanil bioactivation^9,18,19	—	—
Atovaquone	—	—	—
Doxycycline	—	—	—

Part 6. Immunomodulating agents
	Imatinib	Dasatinib	Nilotinib
Immunosuppressants
Ciclosporin	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ ciclosporin exposure^37,38 • Inhibition of Pgp and CYP 3A4 by ciclosporin: ↑ imatinib exposure^37,38	• Inhibition of CYP 3A4 by dasatinib: ↑ ciclosporin exposure^9,18,19,82 • Inhibition of CYP3A4 and Pgp by ciclosporin: ↑ dasatinib exposure^9,18,19,82	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ ciclosporin exposure^9,18,19,82 • Inhibition of CYP3A4 by ciclosporin: ↑ nilotinib exposure^9,18,19,82
Tacrolimus	• Inhibition of CYP 3A4 by imatinib: ↑ tacrolimus exposure^9,18,19,82 • Inhibition of Pgp by tacrolimus: ↑ imatinib exposure^9,18,19,82	• Inhibition of CYP 3A4 by dasatinib: ↑ tacrolimus exposure^9,18,19,82 • Inhibition of Pgp by tacrolimus: ↑ dasatinib exposure^9,18,19,82	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ tacrolimus exposure^9,18,19,82
Sirolimus	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ sirolimus exposure^9,18,19,82	• Inhibition of CYP 3A4 by dasatinib: ↑ sirolimus exposure^9,18,19,82	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ sirolimus exposure^9,18,19,82
Everolimus	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ everolimus exposure^9,18,19,82	• Inhibition of CYP 3A4 by dasatinib: ↑ everolimus exposure^9,18,19,82	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ everolimus exposure^9,18,19,82
Mycophenolate mofetil	—	—	—
Methotrexate	—	—	—
Azathioprine	—	—	—

Part 6. Immunomodulating agents
	Imatinib	Dasatinib	Nilotinib
Immunosuppressants
Ciclosporin	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ ciclosporin exposure^37,38 • Inhibition of Pgp and CYP 3A4 by ciclosporin: ↑ imatinib exposure^37,38	• Inhibition of CYP 3A4 by dasatinib: ↑ ciclosporin exposure^9,18,19,82 • Inhibition of CYP3A4 and Pgp by ciclosporin: ↑ dasatinib exposure^9,18,19,82	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ ciclosporin exposure^9,18,19,82 • Inhibition of CYP3A4 by ciclosporin: ↑ nilotinib exposure^9,18,19,82
Tacrolimus	• Inhibition of CYP 3A4 by imatinib: ↑ tacrolimus exposure^9,18,19,82 • Inhibition of Pgp by tacrolimus: ↑ imatinib exposure^9,18,19,82	• Inhibition of CYP 3A4 by dasatinib: ↑ tacrolimus exposure^9,18,19,82 • Inhibition of Pgp by tacrolimus: ↑ dasatinib exposure^9,18,19,82	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ tacrolimus exposure^9,18,19,82
Sirolimus	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ sirolimus exposure^9,18,19,82	• Inhibition of CYP 3A4 by dasatinib: ↑ sirolimus exposure^9,18,19,82	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ sirolimus exposure^9,18,19,82
Everolimus	• Inhibition of CYP 3A4 and Pgp by imatinib: ↑ everolimus exposure^9,18,19,82	• Inhibition of CYP 3A4 by dasatinib: ↑ everolimus exposure^9,18,19,82	• Inhibition of CYP 3A4 and Pgp by nilotinib: ↑ everolimus exposure^9,18,19,82
Mycophenolate mofetil	—	—	—
Methotrexate	—	—	—
Azathioprine	—	—	—

Part 7. Musculoskeletal system
	Imatinib	Dasatinib	Nilotinib
NSAIDs
Aspirin	—	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	—
Ibuprofen	• Inhibition of CYP 2C9 by imatinib: ↑ ibuprofen exposure^9,18,83,84	• Inhibition of CYP 2C8 by dasatinib: ↑ ibuprofen exposure^9,18,83,84	• Inhibition of CYP 2C8 and 2C9 by nilotinib: ↑ ibuprofen exposure^9,18,83,84
Mefenacid	• Inhibition of CYP 2C9 by imatinib: ↑ mefenacid exposure^9,18,19	• Inhibition of CYP 2C8 by dasatinib: ↑ mefenacid exposure^9,18,19	• Inhibition of CYP 2C8 and 2C9 by nilotinib: ↑ mefenacid exposure^9,18,19
Metamizole	• Induction of CYP 3A4 by metamizole: ↓ imatinib exposure^9,18,85	• Induction of CYP 3A4 by metamizole: ↓ dasatinib exposure^9,18,85	• Induction of CYP 3A4 by metamizole: ↓ nilotinib exposure^9,18,85
Diclofenac	• Inhibition of CYP 2C9 by imatinib: ↑ diclofenac exposure^9,18,86 • Inhibition of Pgp by diclofenac: ↑ imatinib exposure^9,18,86	• Inhibition of CYP 2C8 by dasatinib: ↑ diclofenac exposure^9,18,86 • Inhibition of Pgp by diclofenac: ↑ dasatinib exposure^9,18,86	• Inhibition of CYP 2C8 and 2C9 by nilotinib: ↑ diclofenac exposure^9,18,86
Antigout preparations
Allopurinol	—	—	—

Part 7. Musculoskeletal system
	Imatinib	Dasatinib	Nilotinib
NSAIDs
Aspirin	—	• Thrombocytopenic effect of dasatinib: ↑ risk of bleeding^9,18,19	—
Ibuprofen	• Inhibition of CYP 2C9 by imatinib: ↑ ibuprofen exposure^9,18,83,84	• Inhibition of CYP 2C8 by dasatinib: ↑ ibuprofen exposure^9,18,83,84	• Inhibition of CYP 2C8 and 2C9 by nilotinib: ↑ ibuprofen exposure^9,18,83,84
Mefenacid	• Inhibition of CYP 2C9 by imatinib: ↑ mefenacid exposure^9,18,19	• Inhibition of CYP 2C8 by dasatinib: ↑ mefenacid exposure^9,18,19	• Inhibition of CYP 2C8 and 2C9 by nilotinib: ↑ mefenacid exposure^9,18,19
Metamizole	• Induction of CYP 3A4 by metamizole: ↓ imatinib exposure^9,18,85	• Induction of CYP 3A4 by metamizole: ↓ dasatinib exposure^9,18,85	• Induction of CYP 3A4 by metamizole: ↓ nilotinib exposure^9,18,85
Diclofenac	• Inhibition of CYP 2C9 by imatinib: ↑ diclofenac exposure^9,18,86 • Inhibition of Pgp by diclofenac: ↑ imatinib exposure^9,18,86	• Inhibition of CYP 2C8 by dasatinib: ↑ diclofenac exposure^9,18,86 • Inhibition of Pgp by diclofenac: ↑ dasatinib exposure^9,18,86	• Inhibition of CYP 2C8 and 2C9 by nilotinib: ↑ diclofenac exposure^9,18,86
Antigout preparations
Allopurinol	—	—	—

Part 8. Nervous system
	Imatinib	Dasatinib	Nilotinib
SSRI
Fluoxetine	• Inhibition of CYP 2D6 by imatinib: ↑ fluoxetine exposure^{9,18,19,87,88}	• ↑ QT interval^{9,18,19,87,88} (additive effect) → monitor ECG	• ↑ QT interval^{9,18,19,87,88} (additive effect) → monitor ECG
Fluvoxamine	• Inhibition of CYP 2D6 by imatinib: ↑ fluvoxamine exposure^9,18,19	—	• Inhibition of CYP 2D6 by nilotinib: ↑ fluvoxamine exposure^9,18,19
Paroxetine	• Inhibition of CYP 2D6 by imatinib: ↑ paroxetine exposure^9,18,19	—	• Inhibition of CYP 2D6 by nilotinib: ↑ paroxetine exposure^9,18,19
Citalopram	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ citalopram exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ citalopram exposure^9,18,19	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ citalopram exposure^9,18,19
Sertraline	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ sertraline exposure^9,18,19,87	• Inhibition of CYP 3A4 by dasatinib: ↑ sertraline exposure^9,18,19,87	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ sertraline exposure^9,18,19,87
SSNRI
Venlafaxine	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ venlafaxine exposure^9,18,19,87	• Inhibition of CYP 3A4 by dasatinib: ↑ venlafaxine exposure^9,18,19,87 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ venlafaxine exposure^9,18,19,87 • ↑ QT interval^18,19 (additive effect) → monitor ECG
Duloxetine	• Inhibition of CYP 2D6 by imatinib: ↑ duloxetine exposure^9,18,19	—	• Inhibition of CYP 2D6 by nilotinib: ↑ duloxetine exposure^9,18,19
Tetracyclic agent
Mirtazapine	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ mirtazapine exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ mirtazapine exposure^9,18,19	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ mirtazapine exposure^9,18,19
Tricyclic agents
Trimipramine	• Inhibition of CYP 2D6 by imatinib: ↑ trimipramine exposure^9,18,19	• ↑ QT interval^18,19 (additive effect) → monitor ECG	• ↑ QT interval^18,19 (additive effect) → monitor ECG • Inhibition of CYP 2D6 by nilotinib: ↑ trimipramine exposure^9,18,19
Amitriptyline	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ amitriptyline exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ amitriptyline exposure^9,18,19 • ↑ QT interval^18,19(additive effect) → monitor ECG	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ amitriptyline exposure^9,18,19 • ↑ QT interval^18,19(additive effect) → monitor ECG
Phenothiazines
Levomepromazine	• Inhibition of CYP 2D6 by imatinib: ↑ levomepromazine exposure^9,18,19	—	• Inhibition of CYP 2D6 by nilotinib: ↑ levomepromazine exposure^9,18,19
Z-drugs
Zolpidem	• Inhibition of CYP 3A4 by imatinib: ↑ zolpidem exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ zolpidem exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ zolpidem exposure^9,18,19
Zaleplon	• Inhibition of CYP 3A4 by imatinib: ↑ zaleplon exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ zaleplon exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ zaleplon exposure^9,18,19
Zopiclon	• Inhibition of CYP 3A4 by imatinib: ↑ zopiclon exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ zopiclon exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ zopiclon exposure^9,18,19
Benzodiazepines
Alprazolam	• Inhibition of CYP 3A4 by imatinib: ↑ alprazolam exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ alprazolam exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ alprazolam exposure^9,18,19
Bromazepam	• Inhibition of CYP 3A4 by imatinib: ↑ bromazepam exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ bromazepam exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ bromazepam exposure^9,18,19
Clonazepam	• Inhibition of CYP 3A4 by imatinib: ↑ clonazepam exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ clonazepam exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ clonazepam exposure^9,18,19
Oxazepam	—	—	—
Lorazepam	—	—	—
Diazepam	• Inhibition of CYP 3A4 by imatinib: ↑ diazepam exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ diazepam exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ diazepam exposure^9,18,19
Midazolam	• Inhibition of CYP 3A4 by imatinib: ↑ midazolam exposure^9,18,19 • Inhibition of Pgp by midazolam: ↑ imatinib exposure^9,18,19 • Inhibition of hOCT1 by midazolam: ↓ imatinib intracellular exposure^9,18,64	• Inhibition of CYP 3A4 by dasatinib: ↑ midazolam exposure^9,18,19 • Inhibition of Pgp by midazolam: ↑ dasatinib exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ midazolam exposure^9,18,19
Barbiturates
Phenobarbital	• Inhibition of CYP 2C9 and 2C19 by imatinib: ↑ phenobarbital exposure^9,18,19 • Induction of CYP 3A4 by phenobarbital: ↓ imatinib exposure^9,18,19	• Induction of CYP 3A4 by phenobarbital: ↓ dasatinib exposure^9,18,19	• Inhibition of CYP 2C9 by nilotinib: ↑ phenobarbital exposure^9,18,19 • Induction of CYP 3A4 by phenobarbital: ↓ nilotinib exposure^9,18,19
Antipsychotic agents
Haloperidol	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ haloperidol exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ haloperidol exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• ↑ QT interval^18,19 (additive effect) → monitor ECG
Clozapine	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ clozapine exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ clozapine exposure^9,18,19	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ clozapine exposure^9,18,19
Olanzapine	—	—	—
Risperidone	• Inhibition of CYP 2D6 by imatinib: ↑ risperidone exposure^9,18,19	• ↑ QT interval^18,19 (additive effect) → monitor ECG	• ↑ QT interval^18,19 (additive effect) → monitor ECG
Antiseizure drugs
Phenytoin	• Induction of CYP 3A4 by phenytoin: ↓ imatinib exposure^9,18,19	• Induction of CYP 3A4 by phenytoin: ↓ dasatinib exposure^9,18,19	• Induction of CYP 3A4 by phenytoin: ↓ nilotinib exposure^9,18,19
Valproic acid	• Inhibition of CYP 2C9 and 2C19 by imatinib: ↑ valproic acid exposure • Inhibition of CYP 3A4 by valproic acid: ↑ imatinib exposure^9,18,19	• Inhibition of CYP 3A4 by valproic acid: ↑ dasatinib exposure^9,18,19	• Inhibition of CYP 2C9 by nilotinib: ↑ valproic acid exposure •Inhibition of CYP 3A4 by valproic acid: ↑ nilotinib exposure^9,18,19
Carbamazepine	• Induction of CYP 3A4 and Pgp by carbamazepine: ↓ imatinib exposure^9,18,19	• Induction of CYP 3A4 and Pgp by carbamazepine: ↓ dasatinib exposure^9,18,19	• Induction of CYP 3A4 by carbamazepine: ↓ nilotinib exposure^9,18,19
Lamotrigine	—	—	—
Gabapentin	—	—	—
Topiramate	• Induction of CYP 3A4 by topiramate: ↓ imatinib exposure^9,18,19	• Induction of CYP 3A4 by topiramate: ↓ dasatinib exposure^9,18,19	• Induction of CYP 3A4 by topiramate: ↓ nilotinib exposure^9,18,19
Levetiracetam	—	—	—
Antimaniac drug
Lithium	—	—	—
Aminoketone
Bupropion	—	—	• Induction of CYP 2B6 by nilotinib: ↓ bupropion exposure ↑ bupropion bioactivation^9,18,19
Opioids
Morphine	—	—	—
Tramadol	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ tramadol exposure^9,18,19 ↓ tramadol bioactivation^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ tramadol exposure^9,18,19	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ tramadol exposure^9,18,19 ↓ tramadol bioactivation^9,18,19
Methadone	• Inhibition of CYP 3A4 by imatinib: ↑ methadone exposure^9,18,19 • Inhibition of Pgp by methadone: ↑ imatinib exposure^9,18,19	• ↑QT interval^18,19 (additive effect) → monitor ECG • Inhibition of CYP 3A4 by dasatinib: ↑ methadone exposure^9,18,19 • Inhibition of Pgp by methadone: ↑ dasatinib exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ methadone exposure^9,18,19 • Induction of CYP 2B6 by nilotinib: ↓ methadone exposure¹⁹ • ↑ QT interval^18,19 (additive effect) → monitor ECG
Hydromorphone	—	—	—
Oxycodone	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ oxycodone exposure ↓ oxycodone bioactivation^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ oxycodone exposure^9,18,19	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ oxycodone exposure ↓ oxycodone bioactivation^9,18,19
Buprenorphine	• Inhibition of CYP 3A4 by imatinib: ↑ buprenorphine exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ buprenorphine exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ buprenorphine exposure^9,18,19
Other
Acetaminophen	• Inhibition of O-glucuronidation by imatinib: ↑ acetaminophen exposure^9,18,19,50	—	—
Antimigraine preparations
Dihydroergotamine	• Inhibition of CYP 3A4 by imatinib: ↑ dihydroergotamine exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ dihydroergotamine exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ dihydroergotamine exposure^9,18,19
Sumatriptan	—	—	—

Part 8. Nervous system
	Imatinib	Dasatinib	Nilotinib
SSRI
Fluoxetine	• Inhibition of CYP 2D6 by imatinib: ↑ fluoxetine exposure^{9,18,19,87,88}	• ↑ QT interval^{9,18,19,87,88} (additive effect) → monitor ECG	• ↑ QT interval^{9,18,19,87,88} (additive effect) → monitor ECG
Fluvoxamine	• Inhibition of CYP 2D6 by imatinib: ↑ fluvoxamine exposure^9,18,19	—	• Inhibition of CYP 2D6 by nilotinib: ↑ fluvoxamine exposure^9,18,19
Paroxetine	• Inhibition of CYP 2D6 by imatinib: ↑ paroxetine exposure^9,18,19	—	• Inhibition of CYP 2D6 by nilotinib: ↑ paroxetine exposure^9,18,19
Citalopram	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ citalopram exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ citalopram exposure^9,18,19	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ citalopram exposure^9,18,19
Sertraline	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ sertraline exposure^9,18,19,87	• Inhibition of CYP 3A4 by dasatinib: ↑ sertraline exposure^9,18,19,87	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ sertraline exposure^9,18,19,87
SSNRI
Venlafaxine	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ venlafaxine exposure^9,18,19,87	• Inhibition of CYP 3A4 by dasatinib: ↑ venlafaxine exposure^9,18,19,87 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ venlafaxine exposure^9,18,19,87 • ↑ QT interval^18,19 (additive effect) → monitor ECG
Duloxetine	• Inhibition of CYP 2D6 by imatinib: ↑ duloxetine exposure^9,18,19	—	• Inhibition of CYP 2D6 by nilotinib: ↑ duloxetine exposure^9,18,19
Tetracyclic agent
Mirtazapine	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ mirtazapine exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ mirtazapine exposure^9,18,19	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ mirtazapine exposure^9,18,19
Tricyclic agents
Trimipramine	• Inhibition of CYP 2D6 by imatinib: ↑ trimipramine exposure^9,18,19	• ↑ QT interval^18,19 (additive effect) → monitor ECG	• ↑ QT interval^18,19 (additive effect) → monitor ECG • Inhibition of CYP 2D6 by nilotinib: ↑ trimipramine exposure^9,18,19
Amitriptyline	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ amitriptyline exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ amitriptyline exposure^9,18,19 • ↑ QT interval^18,19(additive effect) → monitor ECG	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ amitriptyline exposure^9,18,19 • ↑ QT interval^18,19(additive effect) → monitor ECG
Phenothiazines
Levomepromazine	• Inhibition of CYP 2D6 by imatinib: ↑ levomepromazine exposure^9,18,19	—	• Inhibition of CYP 2D6 by nilotinib: ↑ levomepromazine exposure^9,18,19
Z-drugs
Zolpidem	• Inhibition of CYP 3A4 by imatinib: ↑ zolpidem exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ zolpidem exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ zolpidem exposure^9,18,19
Zaleplon	• Inhibition of CYP 3A4 by imatinib: ↑ zaleplon exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ zaleplon exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ zaleplon exposure^9,18,19
Zopiclon	• Inhibition of CYP 3A4 by imatinib: ↑ zopiclon exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ zopiclon exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ zopiclon exposure^9,18,19
Benzodiazepines
Alprazolam	• Inhibition of CYP 3A4 by imatinib: ↑ alprazolam exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ alprazolam exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ alprazolam exposure^9,18,19
Bromazepam	• Inhibition of CYP 3A4 by imatinib: ↑ bromazepam exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ bromazepam exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ bromazepam exposure^9,18,19
Clonazepam	• Inhibition of CYP 3A4 by imatinib: ↑ clonazepam exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ clonazepam exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ clonazepam exposure^9,18,19
Oxazepam	—	—	—
Lorazepam	—	—	—
Diazepam	• Inhibition of CYP 3A4 by imatinib: ↑ diazepam exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ diazepam exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ diazepam exposure^9,18,19
Midazolam	• Inhibition of CYP 3A4 by imatinib: ↑ midazolam exposure^9,18,19 • Inhibition of Pgp by midazolam: ↑ imatinib exposure^9,18,19 • Inhibition of hOCT1 by midazolam: ↓ imatinib intracellular exposure^9,18,64	• Inhibition of CYP 3A4 by dasatinib: ↑ midazolam exposure^9,18,19 • Inhibition of Pgp by midazolam: ↑ dasatinib exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ midazolam exposure^9,18,19
Barbiturates
Phenobarbital	• Inhibition of CYP 2C9 and 2C19 by imatinib: ↑ phenobarbital exposure^9,18,19 • Induction of CYP 3A4 by phenobarbital: ↓ imatinib exposure^9,18,19	• Induction of CYP 3A4 by phenobarbital: ↓ dasatinib exposure^9,18,19	• Inhibition of CYP 2C9 by nilotinib: ↑ phenobarbital exposure^9,18,19 • Induction of CYP 3A4 by phenobarbital: ↓ nilotinib exposure^9,18,19
Antipsychotic agents
Haloperidol	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ haloperidol exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ haloperidol exposure^9,18,19 • ↑ QT interval^18,19 (additive effect) → monitor ECG	• ↑ QT interval^18,19 (additive effect) → monitor ECG
Clozapine	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ clozapine exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ clozapine exposure^9,18,19	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ clozapine exposure^9,18,19
Olanzapine	—	—	—
Risperidone	• Inhibition of CYP 2D6 by imatinib: ↑ risperidone exposure^9,18,19	• ↑ QT interval^18,19 (additive effect) → monitor ECG	• ↑ QT interval^18,19 (additive effect) → monitor ECG
Antiseizure drugs
Phenytoin	• Induction of CYP 3A4 by phenytoin: ↓ imatinib exposure^9,18,19	• Induction of CYP 3A4 by phenytoin: ↓ dasatinib exposure^9,18,19	• Induction of CYP 3A4 by phenytoin: ↓ nilotinib exposure^9,18,19
Valproic acid	• Inhibition of CYP 2C9 and 2C19 by imatinib: ↑ valproic acid exposure • Inhibition of CYP 3A4 by valproic acid: ↑ imatinib exposure^9,18,19	• Inhibition of CYP 3A4 by valproic acid: ↑ dasatinib exposure^9,18,19	• Inhibition of CYP 2C9 by nilotinib: ↑ valproic acid exposure •Inhibition of CYP 3A4 by valproic acid: ↑ nilotinib exposure^9,18,19
Carbamazepine	• Induction of CYP 3A4 and Pgp by carbamazepine: ↓ imatinib exposure^9,18,19	• Induction of CYP 3A4 and Pgp by carbamazepine: ↓ dasatinib exposure^9,18,19	• Induction of CYP 3A4 by carbamazepine: ↓ nilotinib exposure^9,18,19
Lamotrigine	—	—	—
Gabapentin	—	—	—
Topiramate	• Induction of CYP 3A4 by topiramate: ↓ imatinib exposure^9,18,19	• Induction of CYP 3A4 by topiramate: ↓ dasatinib exposure^9,18,19	• Induction of CYP 3A4 by topiramate: ↓ nilotinib exposure^9,18,19
Levetiracetam	—	—	—
Antimaniac drug
Lithium	—	—	—
Aminoketone
Bupropion	—	—	• Induction of CYP 2B6 by nilotinib: ↓ bupropion exposure ↑ bupropion bioactivation^9,18,19
Opioids
Morphine	—	—	—
Tramadol	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ tramadol exposure^9,18,19 ↓ tramadol bioactivation^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ tramadol exposure^9,18,19	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ tramadol exposure^9,18,19 ↓ tramadol bioactivation^9,18,19
Methadone	• Inhibition of CYP 3A4 by imatinib: ↑ methadone exposure^9,18,19 • Inhibition of Pgp by methadone: ↑ imatinib exposure^9,18,19	• ↑QT interval^18,19 (additive effect) → monitor ECG • Inhibition of CYP 3A4 by dasatinib: ↑ methadone exposure^9,18,19 • Inhibition of Pgp by methadone: ↑ dasatinib exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ methadone exposure^9,18,19 • Induction of CYP 2B6 by nilotinib: ↓ methadone exposure¹⁹ • ↑ QT interval^18,19 (additive effect) → monitor ECG
Hydromorphone	—	—	—
Oxycodone	• Inhibition of CYP 3A4 and 2D6 by imatinib: ↑ oxycodone exposure ↓ oxycodone bioactivation^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ oxycodone exposure^9,18,19	• Inhibition of CYP 3A4 and 2D6 by nilotinib: ↑ oxycodone exposure ↓ oxycodone bioactivation^9,18,19
Buprenorphine	• Inhibition of CYP 3A4 by imatinib: ↑ buprenorphine exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ buprenorphine exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ buprenorphine exposure^9,18,19
Other
Acetaminophen	• Inhibition of O-glucuronidation by imatinib: ↑ acetaminophen exposure^9,18,19,50	—	—
Antimigraine preparations
Dihydroergotamine	• Inhibition of CYP 3A4 by imatinib: ↑ dihydroergotamine exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ dihydroergotamine exposure^9,18,19	• Inhibition of CYP 3A4 by nilotinib: ↑ dihydroergotamine exposure^9,18,19
Sumatriptan	—	—	—

Part 9. Respiratory system
	Imatinib	Dasatinib	Nilotinib
H1-antagonists
Cetirizin	—	—	• Inhibition of Pgp by nilotinib: ↑ cetirizin exposure^9,18,19
Levocetirizin	—	—	• Inhibition of Pgp by nilotinib: ↑ levocetirizin exposure^9,17,18
Loratadin	• Inhibition of CYP 3A4 by imatinib: ↑ loratadin exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ loratadin exposure^9,18,19	• Inhibition of Pgp by nilotinib: ↑ loratadin exposure^9,18,19
Fexofenadin	• Inhibition of Pgp by fexofenadin: ↑ imatinib exposure⁶⁴	• Inhibition of Pgp by fexofenadin: ↑ dasatinib exposure⁶⁴	• Inhibition of Pgp by nilotinib: ↑ fexofenadin exposure⁶⁴
	• Inhibition of Pgp by imatinib: ↑ fexofenadin exposure⁶⁴
Anti-asthma drugs
Salbutamol	—	—	—
Theophylline	—	—	—

Part 9. Respiratory system
	Imatinib	Dasatinib	Nilotinib
H1-antagonists
Cetirizin	—	—	• Inhibition of Pgp by nilotinib: ↑ cetirizin exposure^9,18,19
Levocetirizin	—	—	• Inhibition of Pgp by nilotinib: ↑ levocetirizin exposure^9,17,18
Loratadin	• Inhibition of CYP 3A4 by imatinib: ↑ loratadin exposure^9,18,19	• Inhibition of CYP 3A4 by dasatinib: ↑ loratadin exposure^9,18,19	• Inhibition of Pgp by nilotinib: ↑ loratadin exposure^9,18,19
Fexofenadin	• Inhibition of Pgp by fexofenadin: ↑ imatinib exposure⁶⁴	• Inhibition of Pgp by fexofenadin: ↑ dasatinib exposure⁶⁴	• Inhibition of Pgp by nilotinib: ↑ fexofenadin exposure⁶⁴
	• Inhibition of Pgp by imatinib: ↑ fexofenadin exposure⁶⁴
Anti-asthma drugs
Salbutamol	—	—	—
Theophylline	—	—	—

Part 10. Miscellaneous
	Imatinib	Dasatinib	Nilotinib
St John's wort	• Induction of CYP 3A4 by St John's wort: ↓ imatinib exposure^43,44	• Induction of CYP 3A4 by St John's wort: ↓ dasatinib exposure⁵⁶	• Induction of CYP 3A4 by St John's wort: ↓ nilotinib exposure^9,18
Grapefruit	• Inhibition of CYP 3A4 and Pgp by grapefruit: ↑ imatinib exposure ^9,18	• Inhibition of CYP 3A4 and Pgp by grapefruit: ↑ dasatinib exposure ^9,18	• Inhibition of CYP 3A4 by grapefruit: ↑ nilotinib exposure⁶²
Licorice	• Inhibition of CYP 3A4 by licorice: ↑ imatinib exposure^9,18,89	• Inhibition of CYP 3A4 by licorice: ↑ dasatinib exposure^9,18,89	• Inhibition of CYP 3A4 by licorice: ↑ nilotinib exposure^9,18,89

Part 10. Miscellaneous
	Imatinib	Dasatinib	Nilotinib
St John's wort	• Induction of CYP 3A4 by St John's wort: ↓ imatinib exposure^43,44	• Induction of CYP 3A4 by St John's wort: ↓ dasatinib exposure⁵⁶	• Induction of CYP 3A4 by St John's wort: ↓ nilotinib exposure^9,18
Grapefruit	• Inhibition of CYP 3A4 and Pgp by grapefruit: ↑ imatinib exposure ^9,18	• Inhibition of CYP 3A4 and Pgp by grapefruit: ↑ dasatinib exposure ^9,18	• Inhibition of CYP 3A4 by grapefruit: ↑ nilotinib exposure⁶²
Licorice	• Inhibition of CYP 3A4 by licorice: ↑ imatinib exposure^9,18,89	• Inhibition of CYP 3A4 by licorice: ↑ dasatinib exposure^9,18,89	• Inhibition of CYP 3A4 by licorice: ↑ nilotinib exposure^9,18,89

TKIs in general can cause thrombocytopenia, which is usually of no clinical relevance. Please take that into consideration when coadministrating with anticoagulant medication.

PT indicates prothrombin time; INR, international normalized ratio.

As lopinavir is co-administered with ritonavir, the net clinical effect observed is inhibition of CYP 3A4 and Pgp by ritonavir, and therefore increase of TKI exposure.

View Large

This Feature Is Available To Subscribers Only