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gefitinib + pemetrexed + platinum
- Development stage
- Unknown
- Lead developer
- AstraZeneca
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Gefitinib + pemetrexed + platinum is a combination regimen used primarily in the first-line treatment of advanced non-small cell lung cancer (NSCLC) harboring activating mutations in the epidermal growth factor receptor (EGFR). Gefitinib is an EGFR tyrosine kinase inhibitor that blocks signaling pathways involved in tumor cell proliferation and survival. Pemetrexed is an antifolate chemotherapeutic agent that inhibits multiple folate-dependent enzymes essential for DNA synthesis, while "platinum" refers to a class of platinum-based chemotherapy agents, most commonly carboplatin or cisplatin, which cause DNA crosslinking and apoptosis. This combination has demonstrated improved progression-free survival (PFS), overall survival (OS), and objective response rate (ORR) compared to gefitinib monotherapy in randomized clinical trials involving patients with EGFR-mutant NSCLC[1][4][5][6][7]. The regimen is generally administered as gefitinib daily plus intravenous pemetrexed and a platinum agent every three weeks for several cycles.
- Other names
- gefitinib + chemotherapygefitinib plus chemotherapygefitinib combined with chemotherapy
02
Targets
ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)DHFR (Dihydrofolate reductase)EGFR (Epidermal growth factor receptor)GAK (Cyclin G-associated kinase)GART (GAR transformylase)RIPK2 (Receptor-interacting protein serine/threonine kinase 2)TS (Thymidylate synthase)Pt-DNA adduct (DNA-oxaliplatin adduct)
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