LEVOLEUCOVORIN CALCIUM · MEITHEAL
Levoleucovorin calcium is a folate analog indicated for rescue therapy following high-dose methotrexate administration in adult and pediatric patients with osteosarcoma. It is also used to diminish toxicity associated with folic acid antagonist overdosage or impaired methotrexate elimination in both adult and pediatric populations. Additionally, it is indicated for the treatment of adults with metastatic colorectal cancer when used in combination with fluorouracil. **Limitations of Use:** It is not indicated for the treatment of pernicious anemia or megaloblastic anemias secondary to vitamin B12 deficiency, as it may allow neurological progression despite hematologic remission.
How LEVOLEUCOVORIN CALCIUM Works
Levoleucovorin is the pharmacologically active isomer of 5-formyl tetrahydrofolic acid. Unlike folic acid, it does not require reduction by the enzyme dihydrofolate reductase (DHFR) to participate in folate-dependent reactions; this allows it to bypass the methotrexate-induced block of DHFR and provide the necessary "one-carbon" moieties for DNA/RNA synthesis. When used with fluorouracil, levoleucovorin is converted to 5,10-methylenetetrahydrofolate, which stabilizes the binding of the fluorouracil metabolite FdUMP to thymidylate synthase. This stabilization enhances the inhibition of thymidylate synthase, further disrupting DNA repair and replication.
Details
- Status
- Discontinued
- First Approved
- 2008-03-07
- Routes
- INTRAVENOUS
- Dosage Forms
- POWDER, SOLUTION
Companies
LEVOLEUCOVORIN CALCIUM Approval History
What LEVOLEUCOVORIN CALCIUM Treats
4 indicationsLEVOLEUCOVORIN CALCIUM is approved for 4 conditions since its original approval in 2015. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Osteosarcoma
- Folic Acid Antagonist Overdose
- Methotrexate Elimination Impairment
- Colorectal Cancer
LEVOLEUCOVORIN CALCIUM Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Direct competitors
Same target(s) AND same indication — head-to-head.
MoA expansion candidates
Same target(s), different indications — where else is this mechanism being explored?
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
What's emerging in LEVOLEUCOVORIN CALCIUM's indications
See all emerging drugs →Phase 3 candidates targeting molecules with no FDA-approved drug, in indications LEVOLEUCOVORIN CALCIUM treats. First-in-class if their pivotal trials read out positive.
Drugs Similar to LEVOLEUCOVORIN CALCIUM
3 of 12FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Clinical Trial Registry
2 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT04060017 | DOD Leucovorin | Ph 2 | active not recruiting | Early Treatment of Language Impairment in Young Children With Autism Spectrum Disorder With Leucovorin Calcium |
| NCT04060030 | AS Leucovorin | Ph 2 | recruiting | Treatment of Social and Language Deficits With Leucovorin for Young Children With Autism |
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
LEVOLEUCOVORIN CALCIUM FDA Label Details
Indications & Usage
FDA Label (PDF)Levoleucovorin injection is indicated for: rescue after high-dose methotrexate therapy in adult and pediatric patients with osteosarcoma. diminishing the toxicity associated with overdosage of folic acid antagonists or impaired methotrexate elimination in adult and pediatric patients. the treatment of adults with metastatic colorectal cancer in combination with fluorouracil. Limitations of Use Levoleucovorin injection is not indicated for pernicious anemia and megaloblastic anemia secondary to the lack of vitamin B 12 , because of the risk of progression of neurologic manifestations despite he...
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FUSILEV
Full clinical data, patents, trials, and competitive landscape for levoleucovorin calcium.
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.