Drug intelligence / Profile preview

bevacizumab + erlotinib + imatinib

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

Overview

A three-drug anticancer regimen combining the VEGF-A–neutralizing monoclonal antibody bevacizumab, the EGFR tyrosine kinase inhibitor erlotinib, and the PDGFR/KIT/BCR-ABL tyrosine kinase inhibitor imatinib. The rationale was simultaneous inhibition of tumor angiogenesis (VEGF/PDGFR signaling) and tumor cell proliferation/survival (EGFR signaling). In phase I/II studies in metastatic clear cell renal cell carcinoma, the regimen was found tolerable at bevacizumab 10 mg/kg IV every 2 weeks, erlotinib 150 mg PO daily, and imatinib 400 mg PO daily in dose-finding; however, in a larger cohort it produced substantial added toxicity without clear efficacy improvement over bevacizumab + erlotinib, leading investigators to recommend against further development of this triplet in RCC.[1][3][7]

Other names
bevacizumab erlotinib imatinib
02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)EGFR (Epidermal growth factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFA (Vascular endothelial growth factor A)PDGFRB (Platelet-derived growth factor receptor beta)

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