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Leucovorin/levofolinate calcium
Leucovorin is a reduced form of folic acid that replenishes intracellular folate pools and enhances the cytotoxic effects of fluorouracil and other antifolate drugs.
Leucovorin is a reduced form of folic acid that replenishes intracellular folate pools and enhances the cytotoxic effects of fluorouracil and other antifolate drugs. Used for Metastatic colorectal cancer (in combination with 5-fluorouracil), Rescue agent for high-dose methotrexate therapy, Adjuvant in fluorouracil-based chemotherapy regimens.
At a glance
| Generic name | Leucovorin/levofolinate calcium |
|---|---|
| Sponsor | Merck Sharp & Dohme LLC |
| Drug class | Folate analog; chemotherapy adjuvant |
| Target | Thymidylate synthase (indirect); folate metabolism |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
Leucovorin (folinic acid) bypasses the dihydrofolate reductase step and directly provides one-carbon units needed for nucleotide synthesis. It is used as a rescue agent and potentiating agent in combination with 5-fluorouracil (5-FU) and methotrexate, increasing their therapeutic efficacy while reducing certain toxicities. By stabilizing the ternary complex between 5-FU metabolites and thymidylate synthase, leucovorin enhances the anticancer activity of fluoropyrimidines.
Approved indications
- Metastatic colorectal cancer (in combination with 5-fluorouracil)
- Rescue agent for high-dose methotrexate therapy
- Adjuvant in fluorouracil-based chemotherapy regimens
Common side effects
- Allergic sensitization
- Rash
- Urticaria
- Wheezing
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)
- 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)
- Clinical Trial of an Anti-cancer Drug, CA-4948 (Emavusertib), in Combination With Chemotherapy Treatment (FOLFOX Plus Bevacizumab) in Metastatic Colorectal Cancer (PHASE1)
- A Study of the Efficacy and Safety of Lisocabtagene Maraleucel (Liso-cel) as First-Line Therapy in Adults With Transplant-Ineligible Primary Central Nervous System Lymphoma (PHASE2)
- Testing the Addition of Radiotherapy to the Usual Treatment (Chemotherapy) for Patients With Esophageal and Gastric Cancer That Has Spread to a Limited Number of Other Places in the Body (PHASE3)
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/levofolinate calcium CI brief — competitive landscape report
- Leucovorin/levofolinate calcium updates RSS · CI watch RSS
- Merck Sharp & Dohme LLC portfolio CI