Product image of Levofolene (Levoleucovorin) supplied by GNH India

Levofolene

Active Ingredient:
Levoleucovorin
Origin:
EU

Levofolene (Levoleucovorin)

Levoleucovorin, the active ingredient in Levofolene, is a folate analog presented as a sterile injectable solution for intramuscular and intravenous use. It provides reduced folate to patients experiencing methotrexate toxicity, folate deficiency, or requiring folate supplementation during cancer chemotherapy.

GNH India supplies Levofolene as a licensed, GDP‑compliant international pharmaceutical supplier serving hospitals, oncology centres and pharmacies worldwide. The company adheres to EU quality standards and offers reliable global distribution.

Manufacturer / TM Owner

Alfasigma S.P.A.

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Indications & Clinical Uses

Levoleucovorin is used in clinical situations that involve folate pathway disruption, such as methotrexate toxicity and folate deficiency.

  • Methotrexate toxicity rescue: restores folate‑dependent DNA synthesis to reduce toxic effects.
  • Folate deficiency: supplies reduced folate to correct deficiency states.
  • Adjunct in cancer chemotherapy: supports patients receiving antifolate agents by mitigating folate depletion.

How It Works

  • Levoleucovorin is a reduced form of folic acid that bypasses the enzymatic block created by dihydrofolate reductase inhibition. By entering cells as 5‑methyltetrahydrofolate, it supplies methyl groups required for thymidylate and purine synthesis, allowing DNA replication and repair to continue despite the presence of antifolate drugs such as methotrexate. The molecule is taken up via reduced folate carriers and converted to active tetrahydrofolate cofactors, directly supporting one‑carbon transfer reactions essential for nucleotide biosynthesis.

Side Effects

Levofolene may be associated with a range of adverse reactions, most of which are mild and reversible.

Common Side Effects

  • Nausea: mild to moderate feeling of stomach upset.
  • Headache: transient cranial discomfort.
  • Injection site pain: localized soreness or erythema.
  • Mild fatigue: temporary decrease in energy levels.

Serious or Rare Side Effects

  • Anaphylactic reaction: severe hypersensitivity requiring immediate medical attention.
  • Acute renal failure: sudden loss of kidney function, especially in patients with pre‑existing renal impairment.
  • Severe hepatic toxicity: marked elevation of liver enzymes indicating liver injury.

Precautions & Warnings

Before using Levofolene, healthcare professionals should consider several precautionary measures to ensure safe administration.

  • Assess renal function: adjust use in patients with impaired kidney function.
  • Monitor hepatic status: watch for liver enzyme elevations during therapy.
  • Review concomitant antifolate drugs: avoid overlapping toxicities.
  • Evaluate for hypersensitivity: discontinue if signs of allergic reaction appear.
  • Pregnancy and lactation: use only if benefits outweigh potential risks, as safety data are limited.
  • Store at 2-8°C: keep refrigerated, protect from light, do not freeze.

Avoid Interactions

Levofolene can interact with other medicines, altering its efficacy or safety profile.

Major Interactions (Avoid)

  • High‑dose methotrexate: concurrent use without rescue may increase toxicity.
  • Trimethoprim‑sulfamethoxazole: can potentiate folate deficiency.
  • Anticonvulsants (e.g., phenytoin, carbamazepine): may reduce folate levels, diminishing rescue effect.

Moderate Interactions (Monitor Closely)

  • NSAIDs: may affect renal clearance of folate analogs.
  • Proton pump inhibitors: possible reduction in absorption of oral folate forms.
  • Vitamin B12 supplements: monitor for altered methylation cycles.

Frequently Asked Questions

Levofolene is employed as a folate rescue agent in patients who have received high‑dose methotrexate, to treat folate deficiency, and as an adjunct in cancer chemotherapy regimens that involve antifolate drugs. By supplying reduced folate, it helps restore normal DNA synthesis and reduces the risk of toxicity associated with folate‑depleting therapies.

Levoleucovorin is a reduced form of folic acid that bypasses the blockade of dihydrofolate reductase caused by drugs like methotrexate. It enters cells as 5‑methyltetrahydrofolate, providing methyl groups needed for thymidylate and purine production, thereby allowing DNA replication and repair to continue despite antifolate exposure.

The dose of Levofolene is individualized and determined by the prescribing clinician based on the specific indication, patient weight, renal function, and the concurrent methotrexate regimen. Healthcare providers calculate the appropriate amount to achieve effective folate rescue while minimizing adverse effects.

Safety data for Levofolene in pregnancy and lactation are limited. It should only be used when the potential benefit to the mother outweighs any possible risk to the fetus or infant. Clinicians must evaluate each case carefully and discuss potential risks with the patient.

To order Levofolene, submit an enquiry on the product page at gnhindia.com, specifying the required quantity. GNH India works with hospitals, pharmacies and procurement teams worldwide, verifies trade or institutional credentials, and then provides pricing, availability, shipping details (including cold‑chain logistics if needed) and assistance with import documentation.

Levofolene (levoleucovorin) is a reduced folate that offers rapid intracellular conversion to active tetrahydrofolate, often providing more efficient rescue than folic acid itself. Compared with calcium folinate, it has similar efficacy but may be preferred in settings requiring sterile injectable formulations and precise dosing for high‑dose methotrexate protocols.

Levofolene should be stored at 2‑8 °C, protected from light, and kept in its original packaging to maintain stability. It must not be frozen or shaken vigorously. If the product is supplied as a lyophilised powder, reconstitute with the recommended diluent immediately before use and discard any unused portion after the specified time.

Levofolene is administered by intramuscular or intravenous injection, depending on the clinical protocol. The route, rate of infusion, and timing relative to methotrexate administration are determined by the treating physician to ensure optimal folate rescue and minimize toxicity.

Serious adverse events include anaphylactic reactions, acute renal failure, and severe hepatic toxicity. Patients should be monitored for signs of hypersensitivity, sudden changes in kidney function, or marked elevations in liver enzymes, and treatment should be discontinued promptly if any of these occur.

Levofolene is contraindicated in individuals with known hypersensitivity to levoleucovorin or any component of the formulation. Caution is also advised for patients with severe renal or hepatic impairment, as well as for those receiving overlapping antifolate therapies without appropriate monitoring.

Published by

GNH India Pharmaceuticals Limited

Licensed pharmaceutical supplier

Last updated:

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