Pemetrexed Disodium (3 brand names, 2 dosage forms, 1 route)
Available dosage forms: POWDER, SOLUTION.
Routes of administration: INTRAVENOUS.
Brand Names
- ALIMTA
- PEMETREXED
- PEMETREXED DISODIUM
Contraindications
Pemetrexed Injection is contraindicated in patients with a history of severe hypersensitivity reaction to pemetrexed [see Adverse Reactions (6.1)].
Adverse Reactions
The following adverse reactions are discussed in greater detail in other sections of the labeling: •Myelosuppression [see Warnings and Precautions (5.1)] •Renal failure [see Warnings and Precautions (5.2)] •Bullous and exfoliative skin toxicity [see Warning and Precautions (5.3)] •Interstitial pneumonitis [see Warnings and Precautions (5.4)] •Radiation recall [see Warnings and Precautions (5.5)]
Mechanism of Action
Pemetrexed is a folate analog metabolic inhibitor that disrupts folate-dependent metabolic processes essential for cell replication. In vitro studies show that pemetrexed inhibits thymidylate synthase (TS), dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase (GARFT), which are folate-dependent enzymes involved in the de novo biosynthesis of thymidine and purine nucleotides. Pemetrexed is taken into cells by membrane carriers such as the reduced folate carrier and membrane folate binding protein transport systems. Once in the cell, pemetrexed is converted to polyglutamate forms by the enzyme folylpolyglutamate synthetase. The polyglutamate forms are retained in cells and are inhibitors of TS and GARFT.
Overdosage
No drugs are approved for the treatment of pemetrexed overdose. Based on animal studies, administration of leucovorin may mitigate the toxicities of pemetrexed overdosage. It is not known whether pemetrexed is dialyzable.