Products
Pemetrexed is commercially available as an infusion drug (Alimta, generic). It has been approved in many countries since 2005.
Structure and properties
Pemetrexed (C20H21N5O6, Mr = 427.4 g/mol) is a folic acid analog. It is present in drugs hydrated and as a disodium salt, in the original preparation as pemetrexed disodium heptahydrate, a white powder that is readily soluble in water.
Effects
Pemetrexed (ATC L01BA04) has antitumor, antiproliferative, and cytostatic properties. The effects are due to the disruption of folate-dependent metabolic processes important for cell division. Pemetrexed inhibits the folate-dependent enzymes thymidylate synthase, dihydrofolate reductase, and glycinamidribonucleotide formyltransferase. These enzymes are involved in the biosynthesis of pyrimidine and purine nucleotides. These are components of DNA and RNA that are required for cell division. The half-life is approximately 3.5 hours.
Indications
- Malignant pleural mesothelioma
- Non-small cell lung carcinoma
Other indications for use are described in the literature.
Dosage
According to the SmPC. The drug is administered as an intravenous infusion.
Contraindications
- Hypersensitivity
- Hepatic insufficiency
- Impaired renal function
- Pregnancy and lactation
Full precautions can be found in the drug label.
Interactions
Pemetrexed is filtered and actively secreted unchanged at the kidney. It is a substrate of OAT3 and corresponding interactions are possible.
Adverse effects
The most common potential adverse effects of monotherapy include fatigue, nausea, and poor appetite.
