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motesanib + gemcitabine + erlotinib
- Development stage
- Phase 1
- Lead developer
- Amgen
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
This is a **combination regimen** of three anticancer agents: motesanib, gemcitabine, and erlotinib. **Motesanib** is an oral small molecule antagonist that targets vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3), platelet-derived growth factor receptor, and Kit, inhibiting angiogenesis and tumor growth. **Gemcitabine** is a nucleoside analog (antimetabolite) used as chemotherapy that inhibits DNA synthesis, leading to apoptosis of rapidly dividing cells. **Erlotinib** is a small molecule tyrosine kinase inhibitor of the epidermal growth factor receptor (EGFR), blocking downstream proliferative signals in cancer cells. This combination was evaluated as a multi-agent regimen in phase 1b clinical trials for patients with advanced solid tumors, notably to determine safety, maximum tolerated dose, and pharmacokinetics. The regimen was found to be tolerable at motesanib 100 mg QD alongside standard gemcitabine and erlotinib doses[1][4].
- Other names
- motesanib + gemcitabine + erlotinib
02
Targets
DNADNA polymerase familyEGFR (Epidermal growth factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFR (PDGFR family)RET (Rearranged during transfection receptor tyrosine kinase)RRM1VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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