Table 4.

FTase inhibitors in clinical trials

  CompoundPhaseMalignancyStatusProtocol ID
R115777 Solid advanced tumors Completed NCI-97-C-0086B* 
R115777 Refractory solid tumors (children) Active NCI-98-C-0141* 
R115777 Refractory or recurrent acute leukemia or Active MSGCC-9802  
   accelerated or blastic phase chronic   NCI-T99-0030* 
   myeloid leukemia  MSGCC-0398115  
    URCC-980300 
R115777 Advanced cancer Active UTHSC-9785011335  
    NCI-V98-1501 
    JRF-R115777  
    SACI-IDD-98-03 
L-778,123 Refractory or recurrent solid tumors or Active MSKCC-98116 
   lymphomas  NCI-G99-1572* 
    MERCK-003-04  
SCH66336 Advanced cancer Active MSKCC-99020  
    NCI-G99-1540* 
    SPRI-C98-564-01  
SCH66336 II Metastatic adenocarcinoma of the Active MSKCC-98115 
   pancreas  NCI-G99-1571* 
    SPRI-C98-545-12  
SCH66336 II Metastatic adenocarcinoma of the Active CWRU-SCH-1298 
   pancreas  NCI-G99-1534* 
    SPRI-C98-545-18  
SCH66336 II Metastatic adenocarcinoma of Not yet active UCLA-9906030  
   the pancreas refractory to  NCI-G99-1610* 
   gemcitabine  SPRI-P00346 
SCH66336 II Previously treated, inoperable, locally Not yet active CAN-NCIC-IND128  
   advanced, or metastatic transitional  SPRI-CAN-NCIC-IND128  
   cell carcinoma of the bladder    
  CompoundPhaseMalignancyStatusProtocol ID
R115777 Solid advanced tumors Completed NCI-97-C-0086B* 
R115777 Refractory solid tumors (children) Active NCI-98-C-0141* 
R115777 Refractory or recurrent acute leukemia or Active MSGCC-9802  
   accelerated or blastic phase chronic   NCI-T99-0030* 
   myeloid leukemia  MSGCC-0398115  
    URCC-980300 
R115777 Advanced cancer Active UTHSC-9785011335  
    NCI-V98-1501 
    JRF-R115777  
    SACI-IDD-98-03 
L-778,123 Refractory or recurrent solid tumors or Active MSKCC-98116 
   lymphomas  NCI-G99-1572* 
    MERCK-003-04  
SCH66336 Advanced cancer Active MSKCC-99020  
    NCI-G99-1540* 
    SPRI-C98-564-01  
SCH66336 II Metastatic adenocarcinoma of the Active MSKCC-98115 
   pancreas  NCI-G99-1571* 
    SPRI-C98-545-12  
SCH66336 II Metastatic adenocarcinoma of the Active CWRU-SCH-1298 
   pancreas  NCI-G99-1534* 
    SPRI-C98-545-18  
SCH66336 II Metastatic adenocarcinoma of Not yet active UCLA-9906030  
   the pancreas refractory to  NCI-G99-1610* 
   gemcitabine  SPRI-P00346 
SCH66336 II Previously treated, inoperable, locally Not yet active CAN-NCIC-IND128  
   advanced, or metastatic transitional  SPRI-CAN-NCIC-IND128  
   cell carcinoma of the bladder    

Three orally bioavailable FTase inhibitors have entered several phase I/II clinical trials. Most of these trials are National Cancer Institute–sponsored (*). The malignancies comprise a wide variety of human solid tumors (eg, primary brain tumors such as gliomas, neurofibromas, neurofibrosarcomas and malignant schwannomas, neuroblastomas, Wilms tumors, germ cell tumors, adenocarcinomas of the pancreas) and hematopoietic diseases such as acute leukemias and chronic myeloid leukemia in acceleration and blastic phase.

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