Drug intelligence / Profile preview

bevacizumab + imatinib mesylate

Development stage
Phase 2
Lead developer
Genentech
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination of two targeted cancer therapies: bevacizumab, a monoclonal antibody that inhibits vascular endothelial growth factor A (VEGF-A), thereby blocking angiogenesis, and imatinib mesylate, a small molecule tyrosine kinase inhibitor that targets BCR-ABL, platelet-derived growth factor receptors (PDGFR), c-Kit, and other kinases. The rationale behind combining these agents is to simultaneously inhibit tumor angiogenesis (via VEGF blockade) and disrupt tumor cell signaling pathways critical for proliferation and survival (via tyrosine kinase inhibition). This combination has been studied in clinical trials primarily in metastatic melanoma[1], gastrointestinal stromal tumors (GIST)[6], and preclinical models of colorectal cancer[2]. While the regimen can be administered safely at standard doses of each agent, significant clinical benefit has not been consistently demonstrated in melanoma or GIST patients. Preclinical data suggest potential synergistic effects on tumor vasculature normalization.

Other names
bevacizumab and imatinibbevacizumab plus imatinib mesylate
02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)NQO2 (Ribosyldihydronicotinamide dehydrogenase [quinone])PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)SRC (Proto-oncogene tyrosine-protein kinase Src)VEGFA (Vascular endothelial growth factor A)

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