Drug intelligence / Profile preview

gefitinib + icotinib + pemetrexed

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

Overview

This is a combination of three drugs used in the treatment of advanced non-small cell lung cancer (NSCLC), particularly in patients with EGFR mutations. Gefitinib and icotinib are both epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs), which block the activity of EGFR to inhibit tumor cell proliferation. Pemetrexed is an antifolate chemotherapy agent that disrupts DNA synthesis by inhibiting thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase. The combination aims to improve efficacy by targeting multiple pathways involved in cancer cell growth and survival[2][4][7]. Recent computational studies suggest that combining gefitinib, paclitaxel, and icotinib may be effective for targeting specific cancer-associated proteins/genes; however, clinical data specifically for the gefitinib + icotinib + pemetrexed triplet are limited[4]. Preclinical evidence supports additive or synergistic effects when combining EGFR TKIs with pemetrexed in EGFR-mutant lung adenocarcinoma models[7].

Other names
gefitinib and icotinib and pemetrexedgefitinib, icotinib, pemetrexed combination
02

Targets

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

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