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BMS-690514 + FOLFIRI
- Development stage
- Unknown
- Lead developer
- Bristol Myers Squibb
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
Overview
BMS-690514 is an investigational small molecule inhibitor targeting multiple receptor tyrosine kinases, including the epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2/ErbB2), and vascular endothelial growth factor receptor (VEGFR). It has been studied in combination with established chemotherapy regimens for cancer treatment. FOLFIRI is a standard chemotherapy regimen composed of folinic acid (leucovorin), fluorouracil (5-FU), and irinotecan. Folinic acid enhances the effectiveness of fluorouracil, which acts as an antimetabolite inhibiting DNA synthesis, while irinotecan inhibits topoisomerase I to prevent DNA replication. The combination is primarily used for metastatic colorectal cancer and other gastrointestinal cancers[1][6][8]. The combination of BMS-690514 with FOLFIRI has been evaluated in clinical trials for advanced solid tumors such as colorectal cancer[2].
- Brand names
- Camptosar
- Other names
- folinic acid + fluorouracil + irinotecanleucovorin calcium + 5-fluorouracil + irinotecan hydrochloride
02
Targets
LCK (Proto-oncogene tyrosine-protein kinase Lck)TS (Thymidylate synthase)ERBB4 (Erb-b2 receptor tyrosine kinase 4)PKA (Cyclic amp-dependent protein kinase)FLT3 (Fms related receptor tyrosine kinase 3)TOP1 (DNA Topoisomerase I)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR2 (Vascular endothelial growth factor receptor 2)ERBB2 (Erb-b2 receptor tyrosine kinase 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)EGFR T790M (Epidermal growth factor receptor T790M mutant)
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