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Pemetrexed + oral folinic acid rescue
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 name | Pemetrexed + oral folinic acid rescue |
|---|---|
| Sponsor | Radboud University Medical Center |
| Drug class | Antifolate antimetabolite |
| Target | Thymidylate synthase, dihydrofolate reductase, glycinamide ribonucleotide formyltransferase |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-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
- Malignant pleural mesothelioma
- Non-small cell lung cancer
- Gastric cancer
Common side effects
- Myelosuppression (neutropenia, thrombocytopenia)
- Mucositis
- Nausea and vomiting
- Fatigue
- Renal toxicity
- Elevated liver enzymes
Key clinical trials
- Dose Individualization of Pemetrexed - IMPROVE-I (PHASE4)
- Folinic Acid for Prevention of Pemetrexed-induced Toxicity (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
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