Drug intelligence / Profile preview

fruquintinib + FOLFIRI

Development stage
Unknown
Lead developer
Takeda
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Fruquintinib + FOLFIRI is a combination regimen used in the treatment of metastatic colorectal cancer (mCRC). Fruquintinib is a novel, highly selective small-molecule tyrosine kinase inhibitor that targets vascular endothelial growth factor receptors 1, 2, and 3 (VEGFR-1/2/3), thereby inhibiting angiogenesis and tumor blood vessel maturation. It is approved for use in adults with metastatic colorectal cancer who have previously received fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy as well as anti-VEGF therapy. FOLFIRI is a standard chemotherapy regimen consisting of folinic acid (leucovorin), fluorouracil (5-FU), and irinotecan. The combination of fruquintinib with FOLFIRI has shown promising clinical benefit as second-line or later therapy for patients with RAS-mutant mCRC, achieving high disease control rates and manageable safety profiles in ongoing clinical trials[2][8][5].

02

Targets

KIT (c-KIT proto-oncogene receptor tyrosine kinase)TS (Thymidylate synthase)TOP1 (DNA Topoisomerase I)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)

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