Drug intelligence / Profile preview

gefitinib + pemetrexed + cisplatin

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Gefitinib + pemetrexed + cisplatin is a combination regimen used primarily in the treatment of advanced or metastatic non-small cell lung cancer (NSCLC), particularly in patients with nonsquamous histology. Gefitinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that blocks EGFR signaling pathways involved in tumor cell proliferation and survival. Pemetrexed is an antifolate antineoplastic agent that inhibits multiple folate-dependent enzymes essential for DNA synthesis and cell replication. Cisplatin is a platinum-based chemotherapeutic agent that forms DNA crosslinks and induces apoptosis in rapidly dividing cells. This combination has been studied as first-line therapy or as induction chemotherapy followed by maintenance gefitinib in NSCLC patients with unknown or known EGFR mutation status. The rationale for combining these agents lies in their complementary mechanisms of action—targeting both the EGFR pathway and general cellular proliferation—and potential to delay resistance development to targeted therapy[1][2][4]. Clinical trials have shown mixed results regarding overall survival benefit compared to monotherapy but suggest possible advantages for certain patient subgroups[1][4].

Other names
gefitinib + pemetrexed + cisplatin
02

Targets

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

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