Drug intelligence / Profile preview

motesanib + FOLFOX4

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

**motesanib + FOLFOX4** is an experimental combination therapy for metastatic colorectal cancer (mCRC) consisting of motesanib, an oral small-molecule inhibitor of several angiogenesis-related receptor tyrosine kinases (including VEGF receptors 1, 2, and 3, PDGF receptor, and Kit), plus the FOLFOX4 chemotherapy regimen, which includes folinic acid (leucovorin), fluorouracil (5-FU), and oxaliplatin. Motesanib works by inhibiting angiogenesis, thereby reducing tumor blood supply, while FOLFOX4 is a standard cytotoxic chemotherapy that injures rapidly dividing tumor cells. The combination was evaluated in early-phase clinical trials for safety and efficacy in patients with mCRC and demonstrated tolerability and modest clinical activity[1][3].\n- Motesanib was developed by Amgen and Takeda.\n- FOLFOX4, as a regimen, is not a commercial product but is composed of standard chemotherapeutics.

02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR3 (Vascular endothelial growth factor receptor 3)PDGFR (PDGFR family)

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