Drug intelligence / Profile preview

motesanib + gemcitabine + erlotinib

Development stage
Unknown
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

KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)DNA polymerase familyPDGFR (PDGFR family)VEGFR-1 (Vascular endothelial growth factor receptor 1)DNAVEGFR3 (Vascular endothelial growth factor receptor 3)EGFR T790M (Epidermal growth factor receptor T790M mutant)RET (Rearranged during transfection receptor tyrosine kinase)RRM1

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