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Levoleucovorin is the levo isomeric form of racemic d,l-leucovorin, present as the calcium salt. Levoleucovorin is the pharmacologically active isomer of leucovorin [(6-S)-leucovorin].

Fusilev for Injection and Fusilev Injection contain levoleucovorin calcium, which is one of several active, chemically reduced derivatives of folic acid. It is useful as antidote to the inhibition of dihydrofolate reductase by methotrexate. This compound has the chemical designation calcium (6S)-N-{4-[[(2-amino-5-formyl-1,4,5,6,7,8-hexahydro-4-oxo-6pteridinyl)methyl] amino]benzoyl}-L-glutamate pentahydrate. The molecular weight is 601.6 and the structural formula is:

Fusilev® (levoleucovorin) Structural Formula Illustration

Its molecular formula is: C20H21CaN7O7• 5H2O.

Fusilev for Injection is supplied as a sterile lyophilized powder consisting of 64 mg levoleucovorin calcium pentahydrate (equivalent to 50 mg levoleucovorin) and 50 mg mannitol per 50 mg vial. Sodium hydroxide and/or hydrocholoric acid are used to adjust the pH during manufacture. It is intended for intravenous administration after reconstitution with 5.3 mL of sterile 0.9% Sodium Chloride Injection, USP [See DOSAGE AND ADMINISTRATION]

Fusilev Injection is supplied as a sterile solution of either 175 mg levoleucovorin in 17.5 mL or 250 mg levoleucovorin in 25 mL. Each mL contains levoleucovorin calcium pentahydrate equivalent to 10 mg levoleucovorin and 8.3 mg sodium chloride. Sodium hydroxide is used for pH adjustment to pH 8.0 (6.5 to 8.5).

What are the possible side effects of levoleucovorin (Fusilev)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Tell your doctor or caregivers at once if you have a serious side effect such as:

  • white patches or sores inside your mouth or on your lips;
  • urinating more or less than usual;
  • severe or ongoing diarrhea;
  • feeling very thirsty or hot, being unable to urinate, heavy sweating, or hot and dry skin;
  • fever, chills;
  • confusion; or
  • trouble breathing.


Read All Potential Side Effects and See Pictures of Fusilev »

Last reviewed on RxList: 6/6/2011
This monograph has been modified to include the generic and brand name in many instances.

Report Problems to the Food and Drug Administration


You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.


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