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Leucovorin/ levoleucovorin
Leucovorin and levoleucovorin are reduced forms of folic acid that enhance the activity of antimetabolite chemotherapy drugs by providing essential one-carbon units for nucleotide synthesis.
Leucovorin and levoleucovorin are reduced forms of folic acid that enhance the activity of antimetabolite chemotherapy drugs by providing essential one-carbon units for nucleotide synthesis. Used for Metastatic colorectal cancer (in combination with fluorouracil), Methotrexate toxicity rescue, Advanced gastric cancer (in combination with fluorouracil and cisplatin).
At a glance
| Generic name | Leucovorin/ levoleucovorin |
|---|---|
| Also known as | Folinic Acid, Fusilev^®, Khapzory^TM |
| Sponsor | Merck Sharp & Dohme LLC |
| Drug class | Folate analog / chemotherapy adjuvant |
| Target | Dihydrofolate reductase (bypass); tetrahydrofolate-dependent enzymes |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
Leucovorin (a racemic mixture) and levoleucovorin (the active L-isomer) bypass the need for dihydrofolate reductase and directly supply tetrahydrofolate cofactors. This potentiates the cytotoxic effects of fluorouracil and methotrexate by stabilizing their target enzymes and increasing intracellular folate pools, while also mitigating methotrexate toxicity when used as a rescue agent.
Approved indications
- Metastatic colorectal cancer (in combination with fluorouracil)
- Methotrexate toxicity rescue
- Advanced gastric cancer (in combination with fluorouracil and cisplatin)
Common side effects
- Nausea and vomiting
- Diarrhea
- Stomatitis
- Myelosuppression
- Allergic reactions
Key clinical trials
- Testing the Addition of the Anti-cancer Drug Venetoclax and/or the Anti-cancer Immunotherapy Blinatumomab to the Usual Chemotherapy Treatment for Infants With Newly Diagnosed KMT2A-rearranged or KMT2A-non-rearranged Leukemia (PHASE2)
- A Study to Investigate Blinatumomab in Combination With Chemotherapy in Patients With Newly Diagnosed B-Lymphoblastic Leukemia (PHASE3)
- Neoadjuvant mFolfirinox With or Without Preoperative Concomitant Chemoradiotherapy in Patients With Borderline Resectable Pancreatic Carcinoma (PANDAS-PRODIGE 44) (PHASE2)
- Targeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Screening Trial (PHASE2)
- Studying Chemotherapy With or Without Panitumumab for Unresectable, Locally Advanced, or Metastatic Pancreatic Cancer Without KRAS Mutations (PHASE3)
- Testing the Addition of Atezolizumab to Combination Chemotherapy or Atezolizumab Alone for Metastatic Colon or Rectal Cancer, the COMMIT Study (PHASE3)
- Study of Chemotherapy, With or Without Binimetinib in Advanced Biliary Tract Cancers in 2nd Line Setting (A ComboMATCH Treatment Trial) (PHASE2)
- Combination Chemotherapy With or Without Donor Stem Cell Transplant in Treating Patients With Acute Lymphoblastic Leukemia (PHASE2)
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 |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Leucovorin/ levoleucovorin CI brief — competitive landscape report
- Leucovorin/ levoleucovorin updates RSS · CI watch RSS
- Merck Sharp & Dohme LLC portfolio CI