US Brand: Alimta
Indian (Generic) Brand: PEMNAT
Active Substance: Pemetrexed
Form release: Vial
Shipping time: 9 – 14 days
Anticancer agent, an antimetabolite. Pemetrexed is a folic acid antagonist, applicable to many of the target and its metabolism in vitro inhibiting thymidylate synthase (TS), dihydrofolate reductase (DHFR), glycinamide ribonucleotide-formiltransferazu (GARFT), which are key folate-dependent enzyme in the biosynthesis of thymidine and purine nucleotides. Pemetrexed enters cells via transporter of reduced folates and folate binding protein transport systems. In the cells, pemetrexed quickly and efficiently converted to polyglutamate forms using folilpoliglutamatsintetazy enzyme.
Polyglutamate forms are retained in the cells and are more potent inhibitors of TS and GARFT. Poliglutaminirovanie – this process is time-dependent and concentration, which occurs in tumor cells and to a lesser degree in normal tissues. Poliglutaminirovannyh metabolites have increased half-life, thereby increasing the drug effect on tumor cells.
The combined use of pemetrexed and cisplatin in vitro studies observed synergistic antitumor effect.
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