Chemical formula: C₂₀H₂₁N₅O₆ Molecular mass: 427.411 g/mol PubChem compound: 446556
Pemetrexed is a folate analog metabolic inhibitor that exerts its action by disrupting folate-dependent metabolic processes essential for cell replication. In vitro studies have shown that pemetrexed inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), glycinamide ribonucleotide formyltransferase (GARFT) and and to a lesser extent aminoimidazole carboxamide ribonucleotide formyltransferase (AICARFT), 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. Polyglutamation is a time- and concentration-dependent process that occurs in tumor cells and, is thought to occur to a lesser extent, in normal tissues. Polyglutamated metabolites are thought to have an increased intracellular half-life resulting in prolonged drug action in malignant cells.
This medicinal substance has been classified in the anatomical therapeutic chemical (ATC) classification according to its main therapeutic use as follows:
ATC code | Group title | Classification |
---|---|---|
L01BA04 | Pemetrexed | L Antineoplastic and immunomodulating agents → L01 Antineoplastic agents → L01B Antimetabolites → L01BA Folic acid analogues |
Competent medicine agencies globally have authorized commercialization of this active ingredient according to these medication package inserts (MPIs):
Title | Information Source | Document Type | |
---|---|---|---|
ARMISARTE Concentrate for solution for infusion | European Medicines Agency (EU) | MPI, EU: SmPC |
Pemetrexed is an active ingredient of these brands:
United States (US)
Australia (AU)Austria (AT)
Brazil (BR)
Canada (CA)
Cyprus (CY)
Ecuador (EC)Estonia (EE)Finland (FI)
Hong Kong (HK)Ireland (IE)Israel (IL)
Japan (JP)
Lithuania (LT)Mexico (MX)
Netherlands (NL)
New Zealand (NZ)
Poland (PL)Romania (RO)Singapore (SG)South Africa (ZA)Spain (ES)Turkey (TR)United Kingdom (UK)
Note the following: The list of brand names is continuously updated, and thus does not include the total of products circulating worldwide. |
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