BTK inhibitors currently approved and under development
| Compound . | Indication . | Stage of development . | Clinical study . | Mechanism . | TEC family kinase inhibition half-maximal inhibitory concentration (nm) . | ||
|---|---|---|---|---|---|---|---|
| BTK . | ITK . | TEC . | |||||
| Ibrutinib22 | Newly diagnosed and R/R | Approved | RESONATE25 | Irreversible C481 binding | 0.5 | 10.7 | 78 |
| RESONATE4 | |||||||
| Acalabrutinib9 | Newly diagnosed and R/R | Approved | ELEVATE-TN10 | Irreversible C481 binding | 5.1 | >1,000 | 93 |
| ASCEND12 | |||||||
| Zanubrutinib13 (BGB-3111) | In development | 3 (approved in mantle cell lymphoma) | SEQUOIA14 ALPINE15 | Irreversible C481 binding | 0.22 | 30 | 1.9 |
| Vecabrutinib17 (SNS-062) | Early development | 1b (CLL/B-NHL) | NCT03037645 | Noncovalent reversible | 3 | 4 | 14 |
| Halted in CLL | |||||||
| LOXO-30519 | Early development | 1/2 (CLL/B-NHL) | NCT03740529 | Noncovalent reversible | 3.15 | >5,000 | 1,234 |
| Fenebrutinib18 (GDC-0853) | Early development | 1 (CLL/B-NHL) | NCT01991184 | Noncovalent reversible | 0.91 | >1,000 | >1,000 |
| ARQ-53120 | Early development | 1 (CLL/B-NHL) | NCT03162536 | Noncovalent reversible | 4.23 | >10,000 | 5.8 |
| Compound . | Indication . | Stage of development . | Clinical study . | Mechanism . | TEC family kinase inhibition half-maximal inhibitory concentration (nm) . | ||
|---|---|---|---|---|---|---|---|
| BTK . | ITK . | TEC . | |||||
| Ibrutinib22 | Newly diagnosed and R/R | Approved | RESONATE25 | Irreversible C481 binding | 0.5 | 10.7 | 78 |
| RESONATE4 | |||||||
| Acalabrutinib9 | Newly diagnosed and R/R | Approved | ELEVATE-TN10 | Irreversible C481 binding | 5.1 | >1,000 | 93 |
| ASCEND12 | |||||||
| Zanubrutinib13 (BGB-3111) | In development | 3 (approved in mantle cell lymphoma) | SEQUOIA14 ALPINE15 | Irreversible C481 binding | 0.22 | 30 | 1.9 |
| Vecabrutinib17 (SNS-062) | Early development | 1b (CLL/B-NHL) | NCT03037645 | Noncovalent reversible | 3 | 4 | 14 |
| Halted in CLL | |||||||
| LOXO-30519 | Early development | 1/2 (CLL/B-NHL) | NCT03740529 | Noncovalent reversible | 3.15 | >5,000 | 1,234 |
| Fenebrutinib18 (GDC-0853) | Early development | 1 (CLL/B-NHL) | NCT01991184 | Noncovalent reversible | 0.91 | >1,000 | >1,000 |
| ARQ-53120 | Early development | 1 (CLL/B-NHL) | NCT03162536 | Noncovalent reversible | 4.23 | >10,000 | 5.8 |
NHL, non-Hodgkin lymphoma.