Drug intelligence / Profile preview

cisplatin + vandetanib + vinorelbine

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen consisting of three drugs: cisplatin, vandetanib, and vinorelbine. Cisplatin is a platinum-based chemotherapy agent that forms DNA crosslinks and induces apoptosis in rapidly dividing cells. Vandetanib is an oral small molecule inhibitor targeting vascular endothelial growth factor receptor-2 (VEGFR-2), epidermal growth factor receptor (EGFR), and RET tyrosine kinase, thereby inhibiting tumor angiogenesis and cell proliferation. Vinorelbine is a third-generation vinca alkaloid that disrupts microtubule formation during mitosis, leading to cell cycle arrest and apoptosis. This combination has been investigated as first-line therapy for advanced non-small cell lung cancer (NSCLC) in clinical trials[2][4]. The rationale for combining these agents lies in their complementary mechanisms of action—targeting DNA integrity, angiogenesis/growth signaling pathways, and mitotic spindle assembly—to enhance antitumor efficacy.

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)DNAVEGFR3 (Vascular endothelial growth factor receptor 3)TUBB (Tubulin (alpha and beta subunits))VEGFR2 (Vascular endothelial growth factor receptor 2)RET (Rearranged during transfection receptor tyrosine kinase)

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