Alimta ® (pemetrexed)

För fullständig produktresumé för Alimta® se FASS.

Denna information är endast avsedd för sjukvårdspersonal verksam i Sverige och som svar på din fråga. Informationen nedan är på engelska

Alimta (pemetrexed): Verkningsmekanism

Pemetrexed är en folsyreantagonist med flera angreppspunkter som avbryter kritiska, folatberoende metaboliska processer nödvändiga för cellreplikationen.

  • In vitro studies have shown that pemetrexed behaves by inhibiting thymidylate synthase (TS), dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase (GARFT), which are key folate-dependent enzymes for the de novo biosynthesis of thymidine and purine nucleotides (Alimta Summary of Product Characteristics [SPC]).

  • Pemetrexed is transported into cells by both the reduced folate carrier and membrane folate‑binding protein transport systems. Once in the cell, pemetrexed is rapidly and efficiently converted to polyglutamate forms by the enzyme folyl polyglutamate synthetase. The polyglutamate forms are retained in cells and are even more potent inhibitors of TS and GARFT (Alimta SPC).

  • Polyglutamation is a time- and concentration-dependent process that occurs in tumor cells and, to a lesser extent, in normal tissues. Polyglutamated metabolites have an increased intracellular half-life, resulting in prolonged drug action in malignant cells (Alimta SPC).


Reference

Alimta EU Summary of Product Characteristics. Utrecht, The Netherlands: Eli Lilly and Company Limited.



Datum fӧr senaste ӧversyn 2017 M07 03

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