Drug intelligence / Profile preview

pemetrexed + gefitinib

Development stage
Phase 3
Lead developer
AstraZeneca
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

Pemetrexed + gefitinib is a combination regimen of two small molecule drugs used primarily in the first-line treatment of advanced non-small cell lung cancer (NSCLC) with activating mutations in the epidermal growth factor receptor (EGFR). Pemetrexed is an antifolate antineoplastic agent that inhibits several folate-dependent enzymes involved in nucleotide synthesis, thereby disrupting DNA replication and cell division. Gefitinib is an EGFR tyrosine kinase inhibitor that blocks signaling pathways critical for tumor cell proliferation and survival. The combination has demonstrated synergistic cytotoxic effects, improved progression-free survival, and higher objective response rates compared to monotherapy with either agent alone in patients with EGFR-mutant NSCLC. This regimen aims to enhance efficacy and delay or prevent resistance to EGFR-TKI therapy[1][2][3][5][8].

02

Targets

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

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