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Pemetrexed is a multi-targeted antitumor antifolate that exerts its effects by disrupting key folate-dependent metabolic processes critical for cell replication.

In vitro studies have shown that pemetrexed behaves as a multi-targeted antifolate by inhibiting thymidylate synthase (TS), dihydrofolate reductase (DHFR), glycinamidribonucleotide formyltransferase (GARFT), which are key folate-dependent enzymes in the biosynthesis of thymidine and purine nucleotides. Pemetrexed enters cells via the reduced folate transporter and membrane protein folate-binding transport systems. Upon entering the cell, pemetrexed is rapidly and efficiently converted to polyglutamate forms by the enzyme folylpolyglutamate synthetase. The polyglutamate forms are retained in cells and are more potent inhibitors of TS and GARFT.

Polyglutaminylation is a time- and concentration-dependent process that occurs in tumor cells and, to a lesser extent, in normal tissues. Metabolites produced by the polyglutaminylation process have an increased intracellular half-life, resulting in increased drug action in tumor cells.

Synergism of antitumor action was observed in in vitro studies when pemetrexed and cisplatin were used in combination.

Manufacturer

JSC Pharmasyntez-Nord

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