Drug intelligence / Profile preview

aflibercept + irinotecan + fluorouracil

Development stage
Unknown
Lead developer
Sanofi
Modality
Small Molecules, Fc-Fusion Proteins → Carrier/Scaffold Proteins → Recombinant Proteins and Enzymes
Administration
Intravenous
01

Overview

This drug is a **combination therapy** consisting of aflibercept, irinotecan, and fluorouracil, commonly used in the treatment regimen for metastatic colorectal cancer (mCRC) that is resistant to or has progressed after an oxaliplatin-containing regimen[1][2][3][6][7]. - **Aflibercept** is a recombinant fusion protein (sometimes called "VEGF Trap") acting as a soluble decoy receptor that binds to vascular endothelial growth factor-A (VEGF-A), VEGF-B, and placental growth factor (PIGF)[5][7]. This inhibits their activation of VEGF receptors, blocking angiogenesis—essential for tumor growth[5][7]. - **Irinotecan** is a small molecule chemotherapeutic agent, a topoisomerase I inhibitor, which prevents DNA from unwinding and replicating, causing cell death. - **Fluorouracil** (5-FU) is a cytotoxic antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis and leading to cell death. Together, this regimen is standard second-line therapy for mCRC, often referred to as "FOLFIRI-A" (aflibercept + FOLFIRI = fluorouracil, leucovorin, irinotecan)[6]. Clinical trials have shown that this combination modestly improves overall and progression-free survival versus chemotherapy alone, although side effects are significant[4][6][7].

02

Targets

TS (Thymidylate synthase)PGF (Placental Growth Factor)TOP1 (DNA Topoisomerase I)VEGFA (Vascular endothelial growth factor A)VEGFB (Vascular endothelial growth factor B)

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