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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