Pemetrexed is a folic acid antagonist with antitumoral, antiproliferative and cytostatic properties. In a narrower sense, folic acid analogues are a small group of (non-selectively acting) cytostatic drugs (so-called antimetabolites) with methotrexate (MTX) as the lead substance. The effects of pemetrexed are based on the inhibition of folate-dependent metabolic processes that are important for cell division. Pemetrexed inhibits the folate-dependent enzymes:
- Thymidylate synthase
- dihydrofolate reductase and
- Glycinamide ribonucleotide formyltransferase.
These enzymes are involved in the biosynthesis of pyrimidine and purine nucleotides. These are components of DNA and RNA that are required for these. The half-life of pemetrexed is about 3.5 hours.