KHAPZORY (levoleucovorin) for injection is a folate analog. KHAPZORY is the pharmacologically active isomer of leucovorin. In mCRC treatment, KHAPZORY works to enhance the therapeutic and toxic effects of fluorouracil.1

See indications and Important Safety Information below

Why is folinic acid included with fluorouracil in mCRC treatment?

Folinic acid has been shown to enhance the therapeutic and toxic effects of fluorouracil. The biological rationale for adding folinic acid into fluorouracil treatment derives from the mechanism of action of fluorouracil and folinic acid in blocking cell growth. 2,3

Is KHAPZORY the same as leucovorin?

No. KHAPZORY is levoleucovorin, the levo isomeric form of racemic d,l-leucovorin.1 While generic leucovorin is a racemic mixture of the d and lisomers of folinic acid, KHAPZORY is the pharmacologically active l-isomer. Learn more >

What is levoleucovorin?

KHAPZORY is levoleucovorin the pharmacologically active isomer in modulation of fluorouracil.1 Levoleucovorin is the only isomer that potentiates the activity of fluorouracil in mCRC treatment. > 4

How long have there been shortage issues with leucovorin supply?

Leucovorin supply issues have not been fully resolved since December 2008.5 Learn more about leucovorin supply issues >

What is the adverse event profile for KHAPZORY when used in mCRC?

View safety information for KHAPZORY >

Where can I order KHAPZORY?

KHAPZORY  is available — you can order it today through major distributors.

View detailed ordering information for hospitals >

View detailed ordering information for practices >

Are there any programs to help provide financial support to my patients?

Spectrum is committed to helping you and your patients access KHAPZORY. The STAR Program provides assistance with benefit verification, obtaining prior authorizations, appeals assistance, and financial assistance for uninsured or underinsured patients.

Learn more by visiting the STAR web site >

Indications and Usage

KHAPZORYTM is a folate analog indicated for:

  • Rescue after high-dose methotrexate therapy in patients with osteosarcoma.
  • Diminishing the toxicity associated with overdosage of folic acid antagonists or impaired methotrexate elimination.
  • Treatment of patients with metastatic colorectal cancer in combination with fluorouracil.

Limitations of Use

KHAPZORY is not indicated for the treatment of pernicious anemia and megaloblastic anemia secondary to lack of vitamin B12 because of the risk of progression of neurologic manifestations despite hematologic remission.

Important Safety Information


  • KHAPZORY is contraindicated in patients who have had severe hypersensitivity to leucovorin products, folic acid, or folinic acid.

Warnings and Precautions

  • Increased gastrointestinal toxicities with fluorouracil: Gastrointestinal toxicities, including stomatitis and diarrhea, occur more commonly and may be of greater severity and of prolonged duration. Deaths from severe enterocolitis, diarrhea, and dehydration have occurred in elderly patients receiving weekly d,l-leucovorin and 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 it has resolved as rapid deterioration leading to death can occur.
  • Drug interaction with trimethoprim-sulfamethoxazole: Concomitant use of d,l-leucovorin with trimethoprim-sulfamethoxazole for the acute treatment of Pneumocystis jiroveci pneumonia in patients with HIV infection increased treatment failure and morbidity.

Adverse Reactions

  • The most common adverse reactions (≥20%) in patients receiving high-dose methotrexate therapy with levoleucovorin rescue were stomatitis (38%) and vomiting (38%).
  • The most common adverse reactions (>50%) in patients receiving levoleucovorin in combination with fluorouracil for metastatic colorectal cancer were stomatitis (72%), diarrhea (70%), and nausea (62%).

Drug Interactions

Leucovorin products increase the toxicity of fluorouracil.

Use in Specific Populations

Levoleucovorin is administered in combination with methotrexate or fluorouracil, which can cause embryo-fetal harm. Refer to methotrexate and fluorouracil prescribing information for additional information.

Please click here to see full Prescribing Information for KHAPZORY.


Reporting of Suspected Adverse Reactions

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch or call 1-800-FDA-1088.

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