Drug intelligence / Profile preview

osimertinib + pemetrexed

Development stage
Phase 2
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Tagrisso + pemetrexed is a combination regimen pairing Tagrisso (osimertinib), an oral third-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, with pemetrexed, an intravenous folate analog metabolic inhibitor. Developed by AstraZeneca, this combination is approved as a first-line treatment for adults with locally advanced or metastatic non-small cell lung cancer (NSCLC) whose tumors harbor EGFR exon 19 deletions or exon 21 L858R mutations. In the Phase III FLAURA2 trial, the addition of pemetrexed and platinum-based chemotherapy (cisplatin or carboplatin) to osimertinib significantly prolonged progression-free survival and overall survival compared to osimertinib monotherapy, establishing a new therapeutic benchmark. Osimertinib selectively inhibits both sensitizing and T790M resistance mutations of EGFR, while pemetrexed targets multiple folate-dependent enzymes to disrupt DNA and RNA synthesis.

Other names
osimertinib + pemetrexedosimertinib plus pemetrexedpemetrexed + osimertinibTagrisso + pemetrexedTagrisso plus pemetrexed
02

Targets

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

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