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gefitinib + erlotinib + icotinib + pemetrexed + cisplatin + carboplatin

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a multi-drug combination regimen consisting of three first-generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs)—gefitinib, erlotinib, and icotinib—combined with three chemotherapeutic agents: pemetrexed, cisplatin, and carboplatin. EGFR-TKIs act by reversibly inhibiting the tyrosine kinase activity of the EGFR, thereby blocking downstream signaling pathways involved in cell proliferation and survival. Pemetrexed is an antifolate antineoplastic agent that inhibits multiple folate-dependent enzymes essential for DNA synthesis. Cisplatin and carboplatin are platinum-based chemotherapeutics that form DNA crosslinks leading to apoptosis. This combination targets both EGFR-mutant tumor cells through targeted inhibition as well as broader cytotoxic effects from chemotherapy. The primary indication for these drugs individually or in various combinations is non-small cell lung cancer (NSCLC), particularly in patients with activating EGFR mutations[1][2][6].

Brand names
Iressa (gefitinib)Tarceva (erlotinib)Conmana (icotinib)Alimta (pemetrexed)Platinol (cisplatin)Paraplatin (carboplatin)
02

Targets

GART (GAR transformylase)TS (Thymidylate synthase)DHFR (Dihydrofolate reductase)DNAEGFR T790M (Epidermal growth factor receptor T790M mutant)

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