Drug intelligence / Profile preview

gefitinib + pemetrexed + platinum

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding 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.

Brand names
Iressa
Other names
gefitinib + chemotherapygefitinib plus chemotherapygefitinib combined with chemotherapy
02

Targets

GAK (Cyclin G-associated kinase)RIPK2 (Receptor-interacting protein serine/threonine kinase 2)TS (Thymidylate synthase)ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)DHFR (Dihydrofolate reductase)DNAGART (GAR transformylase)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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