Drug intelligence / Profile preview

axitinib + FOLFIRI

Development stage
Phase 2
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral (axitinib), Intravenous (folfiri: Folinic Acid, Fluorouracil, Irinotecan)
01

Overview

**axitinib + FOLFIRI** is an experimental combination therapy composed of axitinib, a potent selective small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2, and 3, and the standard FOLFIRI chemotherapy regimen, which includes irinotecan (a topoisomerase I inhibitor), fluorouracil (an antimetabolite that disrupts DNA synthesis), and folinic acid (leucovorin, which enhances fluorouracil efficacy). This combination has been evaluated in patients with metastatic colorectal cancer (mCRC) and other advanced gastrointestinal tumors, primarily in phase I-II studies. Axitinib targets tumor angiogenesis by blocking VEGFR signaling to inhibit tumor blood vessel growth, while FOLFIRI disrupts cancer cell replication through cytotoxic and DNA-damaging mechanisms. The combination has shown tolerability, with key toxicities including neutropenia, hypertension, and fatigue, but has not demonstrated superiority over bevacizumab plus chemotherapy. The combination is not approved for general clinical use and remains investigational for most indications[1][3][5][7].

Other names
axitinib plus FOLFIRIaxitinib and FOLFIRI
02

Targets

PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)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)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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