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Pemetrexed + oral folinic acid rescue

Radboud University Medical Center · FDA-approved active Small molecule

Pemetrexed inhibits multiple folate-dependent enzymes involved in nucleotide synthesis, and oral folinic acid rescue protects normal cells from toxicity while allowing cancer cell death.

Pemetrexed inhibits multiple folate-dependent enzymes involved in nucleotide synthesis, and oral folinic acid rescue protects normal cells from toxicity while allowing cancer cell death. Used for Malignant pleural mesothelioma, Non-small cell lung cancer, Gastric cancer.

At a glance

Generic namePemetrexed + oral folinic acid rescue
SponsorRadboud University Medical Center
Drug classAntifolate antimetabolite
TargetThymidylate synthase, dihydrofolate reductase, glycinamide ribonucleotide formyltransferase
ModalitySmall molecule
Therapeutic areaOncology
PhaseFDA-approved

Mechanism of action

Pemetrexed is a multitargeted antifolate that disrupts thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase, blocking DNA and RNA synthesis in rapidly dividing cells. Oral folinic acid (leucovorin) rescue is administered to replenish folate pools in normal tissues, reducing toxicity to bone marrow and gastrointestinal epithelium while maintaining pemetrexed's anticancer activity against tumor cells with different folate metabolism.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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