Drug intelligence / Profile preview

motesanib

Development stage
Phase 3
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

Motesanib is an orally administered small molecule angiokinase inhibitor that acts as an antagonist of multiple receptor tyrosine kinases, including vascular endothelial growth factor receptors (VEGFR1, VEGFR2, VEGFR3), platelet-derived growth factor receptor (PDGFR), and stem cell factor receptor (c-KIT). It was originally developed by Amgen and later investigated by Takeda. Motesanib inhibits angiogenesis and cellular proliferation by blocking these key signaling pathways involved in tumor growth. The drug was evaluated in clinical trials for several solid tumors such as non-small cell lung cancer, thyroid cancer, gastrointestinal stromal tumors, colorectal cancer, breast cancer, ovarian cancer, fallopian tube carcinoma, and primary peritoneal carcinoma. Despite initial promise in early-phase studies—particularly for thyroid cancers—later phase III trials failed to demonstrate sufficient efficacy for further development. As a result, development of motesanib has been discontinued[1][7][8].

Other names
motesanib diphosphateN-(3,3-dimethylindolin-6-yl)-2-(pyridin-4-ylmethylamino)nicotinamide
02

Targets

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

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