Levoleucovorin (Fusilev)

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General information

Class/mechanism: Folic acid analog that is the pharmacologically active isomer of 5-formyl tetrahydrofolic acid (racemic d,l Leucovorin (Folinic acid)). Counteracts the effects of folic acid antagonists such as methotrexate, which acts by inhibiting dihydrofolate reductase. Enhances the activity of Fluorouracil (5-FU) by inhibiting thymidylate synthase.[1][2][3]
Route: IV
Extravasation: no information

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Diseases for which it is used

Note: these are diseases where folinic acid is used as an adjuvant to Fluorouracil (5-FU), as opposed to an antidote as it is used in conjunction with Methotrexate (MTX)

Patient drug information

History of changes in FDA indication

  • 2008-03-07: FDA approved "to diminish the toxicity and counteract the effects of impaired methotrexate elimination and of inadvertent overdosage of folic acid antagonists." "Levoleucovorin rescue is indicated after high-dose methotrexate therapy in osteosarcoma."

History of changes in PMDA indication

  • 2013-12-20: New additional indication and a new dosage for the treatment of unresectable pancreatic cancer.
  • 2018-09-21: New indication and a new dosage for the treatment of small intestine cancer.

Also known as

  • Generic name: levoleucovorin calcium
  • Brand name: Fusilev, Isovorin


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