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pemetrexed + platinum + osimertinib
- Development stage
- Unknown
- 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, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
Overview
This is a combination regimen consisting of three agents: pemetrexed (an antifolate antineoplastic agent), a platinum-based chemotherapy drug (either cisplatin or carboplatin), and osimertinib (a third-generation epidermal growth factor receptor [EGFR] tyrosine kinase inhibitor). The combination is used as first-line therapy for patients with advanced non-small cell lung cancer (NSCLC) harboring EGFR mutations, specifically exon 19 deletions or exon 21 L858R substitutions. Osimertinib targets mutant forms of EGFR including T790M resistance mutations; pemetrexed inhibits folate-dependent enzymes involved in nucleotide synthesis; and the platinum agent causes DNA crosslinking leading to apoptosis. This regimen has demonstrated improved progression-free survival and response rates compared to osimertinib monotherapy in phase III clinical trials[1][2][3][4][5]. The safety profile reflects the known toxicities of each component.
- Brand names
- TagrissoAlimta
- Other names
- pemetrexed plus platinum plus osimertinibOPP (osimertinib, pemetrexed, and platinum-based chemotherapy)
02
Targets
GART (GAR transformylase)TS (Thymidylate synthase)DHFR (Dihydrofolate reductase)DNAEGFR T790M (Epidermal growth factor receptor T790M mutant)
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