Pemetrexed (LY-231514) is an antifolate that inhibits thymidylate synthase (TS) (Ki = 1.3 nM) and multiple folate-requiring enzymes, such as dihydrofolate reductase (DHFR) (Ki = 7.2 nM) and glycinamide ribonucleotide formyltransferase (GARFT) (Ki = 65 nM). [1]
Pemetrexed (LY-231514) has been studied as a potential treatment option in multiple tumor types, and has been approved in 2004 for the treatment of pleural mesothelioma [2] and non-small cell lung cancer (NSCLC) [3].
A recent clinical study reveals that platinum combination with Pemetrexed (LY-231514) significantly improved the disease control rate and resulted in a tendency toward prolongation of progression-free survival in NSCLC patients who progressed after first-line epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs). [4]"