TheraRadar
Data updated: May 26, 2026

LEVOLEUCOVORIN CALCIUM

Oncology Approved 2015-03-09

LEVOLEUCOVORIN CALCIUM is indicated for the treatment of Osteosarcoma; Folic Acid Antagonist Overdose; Methotrexate Elimination Impairment; Colorectal Cancer.

Source: FDA Label • GLAND

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.

12
Indications
--
Phase 3 Trials
11
Years on Market

Details

Status
Prescription
First Approved
2015-03-09
Routes
INTRAVENOUS
Dosage Forms
SOLUTION, POWDER

LEVOLEUCOVORIN CALCIUM Approval History

2016
2017
2018
2019
2020
2021
2022
2023
2024
2025
2026
Original
New Indication
New Form
Label Update
44 FDA actions from 2015 to 2023
Sep 2023 SUPPL
Label · Labeling
Jul 2023 SUPPL
Label · Labeling
May 2023 ORIGINAL
Update

What LEVOLEUCOVORIN CALCIUM Treats

4 indications

LEVOLEUCOVORIN 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
Source: FDA Label

LEVOLEUCOVORIN CALCIUM Competitive Set

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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

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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

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IMCLONE
Shared indications:
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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

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Ongoing clinical trials by development phase

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Key Completed Trials

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Completed studies with published results, ranked by significance

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Trial Timeline

Full development history with FDA approval milestones

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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 CALCIUM is indicated for the treatment of Osteosarcoma; Folic Acid Antagonist Overdose; Methotrexate Elimination Impairment; Colorectal Cancer.

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Data Sources

Data sourced from official FDA and NIH databases. Click links to verify on original sources.