Drug intelligence / Profile preview

1G EGFR-TKI + pemetrexed + cisplatin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination therapy for non-small cell lung cancer (NSCLC), particularly in patients with EGFR wild-type or certain EGFR-mutant tumors. The regimen typically includes a first-generation epidermal growth factor receptor tyrosine kinase inhibitor (1G EGFR-TKI, such as erlotinib or gefitinib), combined with the chemotherapy agents pemetrexed and cisplatin. Pemetrexed is an antifolate that inhibits thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase, disrupting DNA synthesis. Cisplatin is a platinum-based alkylating agent that crosslinks DNA, leading to apoptosis. 1G EGFR-TKIs block the intracellular domain of the epidermal growth factor receptor (EGFR), inhibiting downstream signaling pathways involved in tumor cell proliferation and survival[1][2][5]. The combination aims to provide synergistic effects by targeting both proliferative signaling and DNA synthesis/repair mechanisms.

Other names
erlotinib + pemetrexed + cisplatingefitinib + pemetrexed + cisplatin
02

Targets

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

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