Drug intelligence / Profile preview

pemetrexed + folinic acid

Development stage: Preclinical
Lead developer: Eli Lilly
Modality: Small Molecules
Administration: Oral, Intravenous

Overview

Pemetrexed + folinic acid is a combination therapy where pemetrexed is used as an antifolate chemotherapy agent and folinic acid (leucovorin) is administered as a rescue therapy to reduce pemetrexed-induced toxicity. Pemetrexed is a multi-targeted antifolate that inhibits multiple enzymes in the folate pathway (thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase), disrupting DNA synthesis. Folinic acid helps mitigate toxicity by providing reduced folate that bypasses the enzymatic blockade caused by pemetrexed.

Targets

GART (GAR transformylase)RFC1 (Reduced folate carrier type 1)DHFR (Dihydrofolate reductase)FOLR1 (FRα)TS (Thymidylate synthase)

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