6/18/2017

Pemetrexed Description


Pemetrexed is a chemotherapy biologic bogus and marketed by Eli Lilly and Company. Its break are the analysis of pleural mesothelioma as able-bodied as non-small corpuscle lung cancer.

Pemetrexed is an antifolate absolute the pyrrolopyrimidine-based basis that exerts its antineoplastic activity by abolition folate-dependent metabolic processes capital for corpuscle replication. In vitro studies accept crystalline that pemetrexed inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), all folate-dependent enzymes complex in the de novo biosynthesis of thymidine and purine nucleotides. Pemetrexed is transported into beef by both the bargain folate carrier and film folate bounden protein carriage systems. Once in the cell, pemetrexed is adapted to polyglutamate forms by the agitator folylpolyglutamate synthetase. The polyglutamate forms are retained in beef and are inhibitors of TS and GARFT. Polyglutamation is a time- and concentration-dependent activity that occurs in bump beef and, to a bottom extent, in accustomed tissues. Polyglutamated metabolites accept an added intracellular half-life consistent in abiding biologic activity in cancerous cells.

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