Levoleucovorin: uses, dosing, side effects & brands
Levoleucovorin is a folate analog sold in the U.S. under 2 brand and generic names, for drug-related side effects and adverse reactions. Below: what the FDA label says, every product that contains it, what the pills look like, and its recall record.
Key facts
- Drug class
- Folate Analog
- Treats (across its forms)
- Drug-Related Side Effects and Adverse Reactions
- Available as
- Solution · Powder · Injectable
- Sold as
- 2 products — Fusilev and Khapzory
- Prescription?
- Prescription only
- Generic available?
- Not in our catalog
How Khapzory is dosed
From the FDA label for Khapzory (application NDA211226). Other levoleucovorin products — different forms, different strengths — are dosed differently. Follow the label for the one you were prescribed.
For intravenous administration only. Do not administer intrathecally. ( 2.1 ) Rescue After High-Dose Methotrexate Therapy Rescue recommendations are based on a methotrexate dose of 12 grams/ m 2 administered by intravenous infusion over 4 hours. Initiate rescue at a dose of 7.5 mg (approximately 5 mg/m 2 ) every 6 hours, 24 hours after the beginning of the methotrexate infusion. ( 2.2 ) Continue until the methotrexate level is below 5 x 10 -8 M (0.05 micromolar). Adjust dose if necessary, based on methotrexate elimination; refer to Full Prescribing Information. ( 2.2 ) Overdosage of Folic Acid Antagonists or Impaired Methotrexate Elimination Start as soon as possible after methotrexate overdosage or within 24 hours of delayed methotrexate elimination. ( 2.3 ) Administer KHAPZORY 7.5 mg (approximately 5 mg/m 2 ) intravenously every 6 hours until methotrexate level is less than 5 x 10 -8 M (0.05 micromolar). ( 2.3 ) Metastatic Colorectal Cancer in Combination with Fluorouracil The following regimens have been used for the treatment of colorectal cancer. o KHAPZORY 100 mg/m 2 by intravenous injection over a minimum of 3 minutes, followed by fluorouracil 370 mg/m 2 once daily for 5 consecutive days. ( 2.4 ) o KHAPZORY 10 mg/m 2 by intravenous injection followed by fluorouracil 425 mg/m 2 once daily for 5 consecutive days. ( 2.4 ) The above five-day courses may be repeated every 4…
Everything below is the FDA label for Khapzory (injectable). Levoleucovorin is also sold as solution and powder, and those are different medicines to take — follow the label for the one you were prescribed.
Khapzory side effects
The following clinical significant adverse reactions are described elsewhere in the labeling: • Increased gastrointestinal toxicities with fluorouracil [see Warnings and Precautions ( 5.1 )] The most common adverse reactions (≥ 20%) in patients receiving high-dose methotrexate therapy with levoleucovorin rescue are stomatitis and vomiting. ( 6.1 ) The most common adverse reactions (>50%) in patients receiving levoleucovorin in combination with fluorouracil for metastatic colorectal cancer are stomatitis, diarrhea, and nausea. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Acrotech Biopharma Inc at 1-888-292-9617 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. High-Dose Methotrexate Therapy Table 2 presents the frequency of adverse reactions which occurred during the administration of 58 courses of high-dose methotrexate 12 grams/m 2 followed by levoleucovorin rescue, for osteosarcoma, in 16 patients aged 6 to 21 years. Most patients received levoleucovorin 7.5 mg every 6 hours for 60 hours or longer, beginning 24 hours after completion of methotrexate administration. Table 2…
Who shouldn’t take Khapzory
KHAPZORY is contraindicated in patients who have had severe hypersensitivity to leucovorin products, folic acid, or folinic acid [see Adverse Reactions ( 6.2 )] . Patients who have had severe hypersensitivity reactions to leucovorin products, folic acid, or folinic acid. ( 4 )
Khapzory drug interactions
7.1 Effects of Leucovorin Products on Other Drugs Antiepileptic Drugs Folic acid in large amounts may counteract the antiepileptic effect of phenobarbital, phenytoin and primidone and increase the frequency of seizures in susceptible children. It is not known whether folinic acid has the same effects; however, both folic and folinic acids share some common metabolic pathways. Monitor patients taking folinic acid in combination with antiepileptic drugs. Fluorouracil Leucovorin products increase the toxicity of fluorouracil. Do not initiate or continue therapy with Khapzory and fluorouracil in patients with symptoms of gastrointestinal toxicity until those symptoms have resolved. Monitor patients with diarrhea until the diarrhea has resolved, as rapid deterioration leading to death can occur [see Warnings and Precautions ( 5.1 )] . Trimethoprim-Sulfamethoxazole The concomitant use of d, l -leucovorin with trimethoprim-sulfamethoxazole for the acute treatment of Pneumocystis jiroveci pneumonia in patients with HIV infection was associated with increased rates of treatment failure and morbidity in a placebo-controlled study [see Warnings and Precautions ( 5.2 )] .
Every levoleucovorin product we track (2)
Same active ingredient — different manufacturer, form, price and FDA recall record. That last one is what our independent score measures.
| # | Drug | Rating | Type | Form | Generic? | Pharmacy pays | |
|---|---|---|---|---|---|---|---|
| 1 | Not yet rated | Prescription | Solution | No data | — | View → | |
| 2 | Not yet rated | Prescription | Injectable | No data | — | View → |
How long levoleucovorin keeps
No levoleucovorin label we read sets a separate limit for after opening, but they do specify how it must be stored — and the stability behind any date assumes those conditions.
Does levoleucovorin expire? The in-use limits and storage rules from its labelsWhat people report to the FDA about levoleucovorin
The FDA Adverse Event Reporting System (FAERS) collects reports from patients and clinicians. It holds 3,763 reports naming levoleucovorin, and the FDA flagged 99% of those reports as serious. The effects reported most often — leaving out reports about overdose, misuse or the condition being treated, which dominate the raw list for common medicines:
- nausea290 reports
- neutropenia282 reports
- diarrhoea259 reports
- decreased appetite187 reports
- vomiting164 reports
- neuropathy peripheral155 reports
- asthenia151 reports
- malignant neoplasm progression149 reports
Read these as a signal, not a rate. A report does not mean levoleucovorin caused the effect — anyone can file one, and many describe people taking several medicines for several conditions. Crucially there is no denominator: FAERS does not record how many people took the drug, so these counts cannot be turned into “X% of patients” — a bigger number often just means a more widely used or more talked-about drug. Duplicates exist, and publicity drives reporting. For what is actually established, read the FDA label section above.
Source: openFDA drug/event (FAERS), retrieved July 25, 2026.
Related calculators
Frequently asked questions
What is Khapzory?
Levoleucovorin is a folate analog and the pharmacologically active levo-isomer of d,l- leucovorin.
What kind of drug is levoleucovorin?
The FDA classifies levoleucovorin as a folate analog. If you are checking whether it is safe to combine with something else, the class is what matters — two drugs from the same class usually should not be stacked.
Can you take levoleucovorin with other medicines?
It depends on the medicine. We check it against the FDA labels rather than guessing: our interaction checker searches each drug's own label for the other and quotes what it says, naming the section it came from. Run levoleucovorin against whatever else you take — and remember that a label not naming a drug is not the same as that combination being safe.
What brand names is levoleucovorin sold under?
We track 2 levoleucovorin-containing products in the U.S.: Fusilev and Khapzory. They are the same active ingredient; they differ in form, manufacturer, price and FDA recall record.
What forms does levoleucovorin come in?
Across the brands we track, levoleucovorin is currently marketed as solution, powder and injectable, per the FDA's National Drug Code Directory. Each form is dosed differently — follow the label for the exact product you were prescribed.
Is there a generic levoleucovorin?
We do not currently list a generic-labelled levoleucovorin product. That does not always mean none exists — it means none appears under a generic name in the FDA data we track. Ask your pharmacist.
Cite this page
- APA
- pharmaranks. (2026, July 24). Levoleucovorin: uses, dosing, side effects & brands. https://pharmaranks.com/drugs/levoleucovorin
- MLA
- “Levoleucovorin: uses, dosing, side effects & brands.” pharmaranks, 24 July 2026, https://pharmaranks.com/drugs/levoleucovorin.
We summarise public FDA and NIH sources — for a clinical claim, cite the primary source we link to as well.
Sources: FDA openFDA drug label, National Drug Code Directory, and Enforcement (recall) database. This page reproduces public FDA data and is not medical advice. Dosing is set by your prescriber.
Read the full FDA label for levoleucovorin on DailyMed (NIH) ↗.