Last reviewed · How we verify
Leucovorin (or Levoleucovorin)
Leucovorin (or Levoleucovorin) is a Folate analog / Chemotherapy adjuvant Small molecule drug developed by Merck Sharp & Dohme LLC. It is currently in Phase 3 development for Methotrexate toxicity rescue (high-dose methotrexate therapy), Potentiation of fluorouracil in colorectal cancer and other solid tumors, Megaloblastic anemia due to folate deficiency.
Leucovorin is a reduced form of folic acid that replenishes intracellular folate pools and enhances the efficacy of antimetabolite chemotherapy agents.
Leucovorin is a reduced form of folic acid that replenishes intracellular folate pools and enhances the efficacy of antimetabolite chemotherapy agents. Used for Methotrexate toxicity rescue (high-dose methotrexate therapy), Potentiation of fluorouracil in colorectal cancer and other solid tumors, Megaloblastic anemia due to folate deficiency.
At a glance
| Generic name | Leucovorin (or Levoleucovorin) |
|---|---|
| Sponsor | Merck Sharp & Dohme LLC |
| Drug class | Folate analog / Chemotherapy adjuvant |
| Target | Dihydrofolate reductase (indirect); thymidylate synthase (potentiation) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
Leucovorin (folinic acid) bypasses the dihydrofolate reductase enzyme and directly provides reduced folate cofactors needed for one-carbon transfer reactions in nucleotide synthesis. It is used as a rescue agent to mitigate toxicity from high-dose methotrexate and to potentiate the cytotoxic effects of fluorouracil-based chemotherapy by stabilizing the ternary complex of thymidylate synthase, fluorodeoxyuridylate, and folate cofactor.
Approved indications
- Methotrexate toxicity rescue (high-dose methotrexate therapy)
- Potentiation of fluorouracil in colorectal cancer and other solid tumors
- Megaloblastic anemia due to folate deficiency
Common side effects
- Allergic sensitization (with repeated intrathecal administration)
- Nausea and vomiting
- Stomatitis
- Diarrhea
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 (or Levoleucovorin) CI brief — competitive landscape report
- Leucovorin (or Levoleucovorin) updates RSS · CI watch RSS
- Merck Sharp & Dohme LLC portfolio CI
Frequently asked questions about Leucovorin (or Levoleucovorin)
What is Leucovorin (or Levoleucovorin)?
How does Leucovorin (or Levoleucovorin) work?
What is Leucovorin (or Levoleucovorin) used for?
Who makes Leucovorin (or Levoleucovorin)?
What drug class is Leucovorin (or Levoleucovorin) in?
What development phase is Leucovorin (or Levoleucovorin) in?
What are the side effects of Leucovorin (or Levoleucovorin)?
What does Leucovorin (or Levoleucovorin) target?
Related
- Drug class: All Folate analog / Chemotherapy adjuvant drugs
- Target: All drugs targeting Dihydrofolate reductase (indirect); thymidylate synthase (potentiation)
- Manufacturer: Merck Sharp & Dohme LLC — full pipeline
- Therapeutic area: All drugs in Oncology
- Indication: Drugs for Methotrexate toxicity rescue (high-dose methotrexate therapy)
- Indication: Drugs for Potentiation of fluorouracil in colorectal cancer and other solid tumors
- Indication: Drugs for Megaloblastic anemia due to folate deficiency
- Compare: Leucovorin (or Levoleucovorin) vs similar drugs
- Pricing: Leucovorin (or Levoleucovorin) cost, discount & access