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motesanib + FOLFIRI
- Development stage
- Unknown
- Lead developer
- Amgen
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Motesanib + FOLFIRI is a combination regimen consisting of **motesanib**, a small molecule angiogenesis inhibitor, and **FOLFIRI**, a chemotherapy protocol comprising folinic acid (leucovorin), fluorouracil (5-FU), and irinotecan. - **Motesanib** inhibits vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3), platelet-derived growth factor receptor (PDGFR), and stem cell factor receptor (c-Kit), thus blocking tumor angiogenesis. - **FOLFIRI** acts by disrupting DNA synthesis (5-FU), inhibiting DNA replication (irinotecan), and potentiating 5-FU activity (folinic acid). This combination was primarily investigated for **metastatic colorectal cancer (mCRC)** in clinical trials. The regimen was tolerated and showed modest efficacy in both first- and second-line settings.
02
Targets
KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFR (PDGFR family)TS (Thymidylate synthase)TOP1 (DNA Topoisomerase I)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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