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Alimta ® (pemetrexed for injection)

100 mg and 500 mg vials

This information is provided in response to your request. Resources may contain information about doses, uses, formulations and populations different from product labeling. See Prescribing Information above, if applicable.

ALIMTA® (pemetrexed): Mechanism of Action

Alimta (pemetrexed) is a folate analog metabolic inhibitor that disrupts folate-dependent metabolic processes essential for cell replication.

Detailed Information

Pemetrexed is a folate analog metabolic inhibitor that disrupts folate-dependent metabolic processes essential for cell replication.1

Data From In Vitro Studies

In vitro studies show that pemetrexed inhibits several folate-dependent enzymes involved in the de novo biosynthesis of thymidine and purine nucleotides including

  • TS

  • DHFR, and

  • GARFT.1

Mechanism of Action

  1. Pemetrexed is taken into cells by membrane carriers such as the reduced folate carrier and membrane folate binding protein transport systems.1

  2. Once in the cell, pemetrexed is converted to polyglutamate forms by the enzyme folylpolyglutamate synthetase.1

  3. The polyglutamate forms are retained in cells and are inhibitors of TS and GARFT.1

Enclosed Prescribing Information

ALIMTA® (pemetrexed for injection), for intravenous use, Lilly

Reference

1. Alimta [package insert]. Indianapolis, IN: Eli Lilly and Company; 2019.

Glossary

DHFR = dihydrofolate reductase

GARFT = glycinamide ribonucleotide formyltransferase

TS = thymidylate synthase 

Date of Last Review: July 20, 2020

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