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Fact Table
| Fact Table | |
|---|---|
| Formula | C20H21CaN7O7 (leucovorin calcium); C20H23N7O7 (leucovorin/folinic acid) |
| License | FDA approved (initial U.S. approval 1952); Lederle Leucovorin authorized by Health Canada on Oct 25, 1996 and marketed in Canada as DIN 02170493 |
| Bioavailability | Dose-dependent oral absorption; apparent oral bioavailability about 97% at 25 mg, 75% at 50 mg and 37% at 100 mg; absorption is saturable above 25 mg |
| Legal status | Prescription only (Rx; Prescription in Canada) |
| Chemical Name | L-glutamic acid, N-[4-[[(2-amino-5-formyl-1,4,5,6,7,8-hexahydro-4-oxo-6-pteridinyl)methyl]amino]benzoyl]-, calcium salt (1:1) |
| Elimination half-life | Terminal half-life of total reduced folates approximately 5.7 hours after oral administration and 6.2 hours after IM/IV administration; IV levoleucovorin 0.5–1.3 hours and 5-MTHF 3–7 hours |
| Dosage (Strength) | Lederle Leucovorin: 5 mg oral tablets; U.S. leucovorin calcium tablets: 5 mg, 10 mg, 15 mg and 25 mg; methotrexate toxicity rescue commonly 10 mg/m2 up to 25 mg orally every 6 hours until methotrexate level is less than 10-8 M; megaloblastic anemia doses up to 15 mg daily have been suggested |
| Pregnancy | Available intermittent-use data for folate antagonist/DHFR-inhibitor toxicity in pregnancy have not identified a drug-associated risk; with chemotherapy combinations, refer to the concomitant agent as methotrexate or fluorouracil may cause fetal harm |
| Brands | Lederle Leucovorin; Wellcovorin; JAMP Leucovorin; Riva Leucovorin; Mint-Leucovorin; generic leucovorin calcium/calcium folinate tablets and injections |
| Protein binding | Levoleucovorin minimally bound to human serum albumin; 5-MTHF protein binding approximately 42–49% |
| PubChem CID | 135403647 (leucovorin calcium); 135403648 (leucovorin) |
| MedlinePlus | a682336; a608038 |
| ChEBI | 31340 (calcium folinate); 15640 (folinic acid/leucovorin) |
| ATC code | V03AF03 |
| DrugBank | DB00650 |
| KEGG | D01211 |
| Routes of administration | By mouth (oral tablets); intravenous or intramuscular injection for injectable leucovorin calcium products; not for intrathecal administration |
Leucovorin calcium, also called folinic acid, is a prescription drug related to vitamin B9. It is often used as a rescue medicine to help protect healthy cells from the harmful effects of methotrexate or similar drugs when the body cannot clear them well. It can also treat overdoses of certain medicines that block folate, and it is used for a rare genetic condition called cerebral folate transport deficiency in people with a confirmed FOLR1 gene change.
Directions
Leucovorin tablets are taken by mouth, with or without food, as directed by a healthcare provider.
To reduce methotrexate toxicity, the usual dose is based on body size: 10 mg per square meter, up to 25 mg, every 6 hours until methotrexate in the blood drops to a safe level.
If more than 25 mg is needed every 6 hours, the injectable form is used instead.
For an overdose of medicines that block folic acid, the usual dose is 5 mg to 15 mg per day.
Treatment should start as soon as possible after the overdose, or within 24 hours after methotrexate if the body is not clearing it properly.
For cerebral folate transport deficiency, the starting dose is 1 to 2 mg per kg of body weight per day.
The dose may be adjusted up to 8.5 mg/kg/day for people under 40 kg, or up to 330 mg/day for people 40 kg or more.
Ingredients
The active ingredient is leucovorin calcium. Inactive ingredients may include colloidal silicon dioxide, croscarmellose sodium, magnesium stearate, microcrystalline cellulose, povidone, and pregelatinized starch.
Cautions
Before using this medication, you may want to consult a healthcare provider about the following:
- Any existing health conditions
- Any allergies
- A list of all medications currently being taken
Leucovorin should not be used as the sole treatment for pernicious anemia or other megaloblastic anemias caused by vitamin B12 deficiency.
Leucovorin is not recommended in people known to have a deficiency of methenyltetrahydrofolate synthetase (MTHFS), as MTHFS is needed to convert leucovorin into its active form.
When given with fluorouracil (5-FU) for chemotherapy, leucovorin can increase the toxicity of 5-FU. This combination should only be used under the supervision of a cancer specialist.
Leucovorin may reduce the effectiveness of certain antiseizure medications such as phenytoin, phenobarbital, and primidone. People taking these medicines may need closer monitoring for seizure activity.
Avoid using leucovorin with trimethoprim-sulfamethoxazole (Bactrim, Septra) in the treatment of Pneumocystis pneumonia, as it may reduce the antibiotic’s effectiveness.
For methotrexate toxicity, oral doses greater than about 25 mg are not well absorbed since absorption becomes saturated. If higher single doses are needed, the injectable form of leucovorin should be used instead.
Contraindications
Avoid taking or using this medication if you have a history of a severe hypersensitivity reaction to leucovorin, levoleucovorin, folic acid, or any ingredients in leucovorin calcium tablets.
Side Effects
Reported side effects of Leucovorin include:
- Itching
- Skin rash
- Hives
- Shortness of breath
- Shaking chills
- Changes in body temperature (such as a low-grade fever)
- Mild gastrointestinal effects (nausea, vomiting, or diarrhea)
Get medical help for any signs of a serious allergic reaction such as swelling of the face, lips, tongue, or throat, trouble breathing, or a severe rash.
When leucovorin is used with fluorouracil, it is important to get medical care for severe diarrhea, dehydration, or severe stomach pain.
When leucovorin is used together with antiseizure medications, more frequent or harder-to-control seizures should be reported.
People with FOLR1-related cerebral folate transport deficiency may have other neurologic symptoms that should be tracked with their specialist during treatment.
References
- Leucovorin Calcium Tablets Highlights of Prescribing Information. Berkeley Heights, NJ: Hikma Pharmaceuticals USA Inc.; 2026.
- Leucovorin Calcium Drug Label Information. Berkeley Heights, NJ: Hikma Pharmaceuticals USA Inc.; 2026.
