Levoleucovorin (Fusilev)
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)
- Cervical cancer
- Cholangiocarcinoma
- Colorectal cancer
- Esophageal cancer
- Gastric cancer
- Hepatocellular carcinoma
- Pancreatic cancer
- Small bowel adenocarcinoma
Patient drug information
- Levoleucovorin (Fusilev) package insert[1]
- Levoleucovorin (Fusilev) patient drug information (UpToDate)[4]
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
References
- Drugs
- Intravenous medications
- Folic acid analog
- Chemotherapy protective agents
- Cervical cancer medications
- Cholangiocarcinoma medications
- Colon cancer medications
- Colorectal cancer medications
- Esophageal adenocarcinoma medications
- Esophageal cancer medications
- Gastric cancer medications
- Hepatocellular carcinoma medications
- Pancreatic cancer medications
- Rectal cancer medications
- Small bowel adenocarcinoma medications
- FDA approved in 2008