What is Levoleucovorin used for?

Levoleucovorin is used to protect the body after high-dose methotrexate treatment and to help 5-fluorouracil work better when treating advanced colorectal cancer.

Can Levoleucovorin be used to treat anemia?

No, Levoleucovorin is not approved to treat pernicious anemia or anemia caused by a lack of vitamin B12.

What are the most common side effects of Levoleucovorin?

Common side effects include diarrhea, nausea, and mouth sores (stomatitis).

Is Levoleucovorin safe during pregnancy?

It is unknown if Levoleucovorin causes fetal harm, so it should only be used during pregnancy if absolutely necessary.

Can Levoleucovorin interact with seizure medications?

Yes, Levoleucovorin may make anti-seizure drugs like phenytoin or phenobarbital less effective, potentially increasing seizure frequency.

How should Levoleucovorin be administered?

Levoleucovorin must be given by intravenous injection and should never be injected into the spinal canal.

Why is the injection speed important for Levoleucovorin?

Because the solution contains calcium, it must not be injected faster than 16 mL per minute.

Does Levoleucovorin affect breastfeeding?

It is not known if the drug enters breast milk, so mothers should weigh the importance of the drug against the risk to the infant.

L-Folinic acid | CAS 68538-85-2 | VVIAGPKUTFNRDU

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Folate analog / Antidote

Levoleucovorin is a folate analog used primarily to protect the body after high doses of methotrexate or to help certain cancer treatments work better. It is used to counteract the toxic effects of folic acid antagonists and is also used in combination with 5-fluorouracil to treat advanced colorectal cancer.

How it worksLevoleucovorin is a form of folate that does not need specific enzymes to work. It can block the harmful effects of drugs like methotrexate or help drugs like 5-fluorouracil work more effectively against cancer cells.

Brand names:KHAPZORY

Used for

Rescue after high-dose methotrexate therapy in osteosarcomaReducing toxicity from methotrexate or other folic acid antagonistsCombination treatment with 5-fluorouracil for advanced metastatic colorectal cancer

Conditions

OsteosarcomaAdvanced metastatic colorectal cancer

Class

Folate analogAntidoteFolate analog / AntidoteGastrointestinalHematologic

How to take

FormsIntravenous injection

RoutesIntravenous

Dosage depends on the condition being treated. For methotrexate rescue, it is often given every 6 hours. For colorectal cancer, it is given via slow intravenous injection before 5-fluorouracil.

Do not administer this medication through the spinal canal (intrathecally). Administration rates must be controlled due to calcium content; do not exceed 16 mL per minute of solution.

Key warnings

·Levoleucovorin can make the toxic effects of 5-fluorouracil stronger.
·Because it contains calcium, it must be injected at a controlled rate (no more than 16 mL per minute).
·Improper use for certain types of anemia may improve blood counts but allow nerve damage to continue progressing.

Do not use if

·Do not use if you have had an allergic reaction to folic acid or foliinic acid.

Side effects

Common

DiarrheaNauseaStomatitis (mouth sores)Vomiting

Serious

·Severe diarrhea and dehydration
·Severe colitis (inflammation of the colon)
·Allergic reactions

Seek help if

·Severe diarrhea
·Severe dehydration
·Severe colitis

Interactions

·Can increase the toxicity of 5-fluorouracil.
·May reduce the effectiveness of anti-seizure medications like phenobarbital, phenytoin, and primidone.
·Use with trimethoprim/sulfamethoxazole in HIV patients may lead to treatment failure.

Special populations

PregnancyIt is unknown if levoleucovorin causes harm to a fetus. It should only be used during pregnancy if the benefit clearly outweighs the risk.

BreastfeedingIt is not known if this drug passes into breast milk. Because of the risk of serious reactions in infants, you should consider whether to stop breastfeeding or stop the medication.

PediatricClinical studies have been conducted in pediatric patients (ages 6 to 21) for osteosarcoma treatment.

GeriatricIn colorectal cancer studies, side effects in patients 65 and older were similar to those seen in younger patients.

Talk to your doctor

Monitor

·Serum creatinine
·Methotrexate levels
·Urinary pH

Questions to ask

·How will Levoleucovorin interact with my current seizure medications?
·What is the risk of increased 5-fluorouracil toxicity?
·How will my kidney function be monitored during treatment?

Pharmacokinetics

OnsetSerum concentrations of 5-methyl-5,6,7,8-tetrahydrofolate reach a peak at approximately 0.9 hours.

Half-lifeThe mean terminal half-life for total-THF is 5.1 hours and for (6S)-5-methyl-5,6,7,8-tetrahydrofolate is 6.8 hours.

MetabolismLevoleucovorin is readily converted to 5,10-methylenetetrahydrofolate.

Practical

OverdoseNo specific data is available regarding overdose for levoleucovorin.

Ingredients

Inactive

Sodium hydroxideSodium chlorideWater

Educational summary derived from FDA labeling, AI-assisted. Not medical advice — consult a healthcare professional. Updated 2026-04-25.