Drug intelligence / Profile preview

carboplatin + cediranib + gemcitabine

Development stage
Phase 2
Lead developer
AstraZeneca
Modality
Classical Binding Small Molecules → Small Molecules, 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: - **Carboplatin** (a platinum-based chemotherapy agent that causes DNA crosslinking and apoptosis in rapidly dividing cells) - **Cediranib** (an oral small molecule inhibitor targeting vascular endothelial growth factor receptors 1, 2, and 3 [VEGFR1/2/3], thereby inhibiting angiogenesis) - **Gemcitabine** (a nucleoside analog that inhibits DNA synthesis by incorporation into DNA and inhibition of ribonucleotide reductase) The combination has been investigated as first-line therapy for advanced non-small cell lung cancer (NSCLC) in randomized phase II studies. The addition of cediranib to carboplatin and gemcitabine increased toxicity but did not significantly improve overall response rate compared to chemotherapy alone. Cediranib’s mechanism targets tumor angiogenesis, while carboplatin and gemcitabine act as cytotoxic agents against proliferating tumor cells[6][8]. This regimen remains investigational.

02

Targets

DNADNA polymerase familyFGFR1 (Fibroblast growth factor receptor 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)RNR (Ribonucleotide reductase)VEGFR-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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