Brand Name

Khapzory

Generic Name
Levoleucovorin
View Brand Information
FDA approval date: July 07, 2016
Classification: Folate Analog
Form: Injection

What is Khapzory (Levoleucovorin)?

For people undergoing cancer treatment, the journey can be physically and emotionally demanding. Chemotherapy, while vital for fighting cancer cells, can also harm healthy tissues and cause challenging side effects. Khapzory (levoleucovorin) is a medication designed to protect healthy cells and enhance the effectiveness of certain chemotherapy drugs, helping patients tolerate treatment better and improve outcomes. 

Khapzory belongs to a group of medications known as chemoprotective agents or folate analogs. It is the active form of leucovorin, a drug that supports the body’s use of folic acid, an essential vitamin for cell repair and DNA synthesis. Approved by the U.S. Food and Drug Administration (FDA), Khapzory is used in combination with specific cancer therapies or as a rescue medication after high-dose chemotherapy. It plays a critical role in balancing efficacy with safety, allowing patients to benefit from powerful treatments while reducing harmful side effects. 

What does Khapzory do? 

Khapzory is used primarily in cancer care and certain medication overdose situations. Its main purposes include: 

  • Enhancing chemotherapy effectiveness: Khapzory is often combined with fluorouracil (5-FU) to treat cancers such as colorectal cancer. In this setting, it strengthens the cancer-fighting effect of fluorouracil, helping the drug work more efficiently against tumor cells.[Text Wrapping Break] 
  • Reducing chemotherapy toxicity: After high doses of methotrexate, which can damage healthy cells, Khapzory acts as a rescue agent to protect normal tissues. This is known as “leucovorin rescue,” and it allows higher doses of methotrexate to be used safely in treating cancers like leukemia or osteosarcoma.[Text Wrapping Break] 
  • Treating folate deficiency or overdose: In some cases, Khapzory may also be used to reverse the effects of folate-blocking medications or to help manage toxic reactions caused by certain drugs. 

Patients receiving Khapzory as part of chemotherapy typically experience better tolerance to treatment and improved recovery of normal cell function. Clinical studies have shown that using levoleucovorin instead of racemic leucovorin provides a more efficient active form of the drug, meaning the body can use it immediately without needing to convert it (NIH, 2024). 

How does Khapzory work? 

Khapzory works by supplying the body with levoleucovorin, the biologically active form of folinic acid. To understand how it works, it helps to know that folic acid is essential for DNA production and cell repair, both of which are vital during cancer treatment. 

Some chemotherapy drugs, like methotrexate, block the body’s ability to use folic acid, stopping cancer cells from dividing. While this approach kills cancer cells, it can also harm normal cells that need folic acid to survive. Khapzory “rescues” these healthy cells by bypassing the blocked pathway and restoring the folate balance, allowing them to recover. 

In other cases, such as with fluorouracil therapy, Khapzory has the opposite role: it boosts the anticancer effect. When combined with fluorouracil, levoleucovorin enhances the drug’s ability to interfere with DNA production in cancer cells, making the chemotherapy more potent. 

Clinically, this dual role protecting normal cells while strengthening chemotherapy makes Khapzory a critical supportive treatment in oncology care. 

Khapzory side effects 

Khapzory is generally well-tolerated, but like all medications, it can cause side effects. The type and severity often depend on the patient’s overall health and the other drugs being used alongside it. 

Common side effects may include: 

  • Nausea or vomiting[Text Wrapping Break] 
  • Diarrhea or stomach upset[Text Wrapping Break] 
  • Fatigue or weakness[Text Wrapping Break] 
  • Mouth sores[Text Wrapping Break] 
  • Mild redness or irritation at the injection site 

Serious side effects (less common): 

  • Allergic reactions such as rash, itching, or swelling of the face or throat[Text Wrapping Break] 
  • Trouble breathing or dizziness[Text Wrapping Break] 
  • Seizures (rare, but possible with very high doses or certain medical conditions) 

Khapzory with fluorouracil can worsen chemotherapy side effects like mouth sores, diarrhea, or low white blood cell counts. Use with caution in dehydrated patients, those with kidney problems, or folinic acid hypersensitivity.  

Seek immediate medical attention for allergic reactions or severe diarrhea. Most patients tolerate Khapzory well with regular supervision to manage side effects. 

Khapzory dosage 

Khapzory is an IV injection or infusion given by a healthcare professional. Dosage and schedule vary based on cancer type, chemotherapy, body size, and kidney function. With methotrexate, it’s started hours after chemo and continued until methotrexate clears. With fluorouracil, it’s given the same day to enhance effect. 

Doctors monitor blood counts, kidney function, and methotrexate levels (if applicable) for treatment safety. Patients should stay hydrated and report unusual symptoms. Older adults or those with kidney impairment may need dosage adjustments due to slower drug clearance. 

Does Khapzory have a generic version? 

Yes. Levoleucovorin, the active ingredient in Khapzory, is available in the United States as both a brand-name and generic injectable formulation. FDA-approved generic versions are considered equally safe and effective as Khapzory because they contain the same active ingredient and are held to identical manufacturing and quality standards. 

Khapzory, like other levoleucovorin formulations such as Fusilev, is interchangeable. The choice depends on insurance, availability, and treatment setting, but efficacy is maintained when properly administered. 

Conclusion 

Khapzory (levoleucovorin) is a vital part of modern cancer therapy, serving both as a rescue medication and a chemotherapy enhancer. By protecting healthy cells from methotrexate toxicity and boosting the action of fluorouracil, it allows oncologists to use powerful treatments more safely and effectively. 

Side effects are typically mild and manageable with professional oversight, ensuring treatment effectively targets cancer while protecting healthy tissue. Understanding Khapzory’s role in the treatment plan empowers patients and caregivers. Prescribed and monitored by experts, Khapzory aids the body’s resilience, helping patients move forward with strength. 

References 

  1. U.S. Food and Drug Administration (FDA). (2024). Khapzory (levoleucovorin) injection prescribing information. Retrieved from https://www.accessdata.fda.gov[Text Wrapping Break] 
  1. MedlinePlus. (2024). Levoleucovorin injection: Drug information. National Library of Medicine. Retrieved from https://medlineplus.gov[Text Wrapping Break] 
  1. Mayo Clinic. (2024). Levoleucovorin (injection route) description and precautions. Retrieved from https://www.mayoclinic.org[Text Wrapping Break] 
  1. National Institutes of Health (NIH). (2024). Folinic acid rescue and chemotherapy modulation overview. Retrieved from https://www.nih.gov[Text Wrapping Break] 

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Brand Information

KHAPZORY (levoleucovorin)
1INDICATIONS AND USAGE
KHAPZORY is indicated for:
  • rescue after high-dose methotrexate therapy in adult and pediatric patients with osteosarcoma.
  • diminishing the toxicity associated with overdosage of folic acid antagonists or impaired methotrexate elimination adult and pediatric patients.
  • The treatment of adults with metastatic colorectal cancer in combination with fluorouracil.
Limitations of Use
KHAPZORY is not indicated for pernicious anemia and megaloblastic anemia secondary to lack the of vitamin B
2DOSAGE FORMS AND STRENGTHS
For Injection: 175 mg of levoleucovorin as a sterile, white to yellowish lyophilized powder in a single-dose vial for reconstitution.
3CONTRAINDICATIONS
KHAPZORY is contraindicated in patients who have had severe hypersensitivity to leucovorin products, folic acid, or folinic acid
4ADVERSE REACTIONS
The following clinical significant adverse reactions are described elsewhere in the labeling:
  • Increased gastrointestinal toxicities with fluorouracil
4.1Clinical 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/m2 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.
Combination with Fluorouracil in Colorectal Cancer
Table 3 presents the frequency of adverse reactions which occurred in 2 arms of a randomized controlled trial conducted by the North Central Cancer Treatment Group (NCCTG) in patients with metastatic colorectal cancer. The trial failed to show superior overall survival with fluorouracil + levoleucovorin compared to fluorouracil + d,l-leucovorin. Patients were randomized to fluorouracil 370 mg/m2 intravenously and levoleucovorin 100 mg/m2 intravenously, both daily for 5 days, or to fluorouracil 370 mg/m2 intravenously and d,l-leucovorin 200 mg/m2 intravenously, both daily for 5 days. Treatment was repeated week 4 and week 8, and then every 5 weeks until disease progression or unacceptable toxicity.
*Includes abdominal pain, upper abdominal pain, lower abdominal pain, and abdominal tenderness
4.2Postmarketing Experience
The following adverse reactions have been identified during post-approval use of levoleucovorin products. Because these adverse reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. The following have been reported:
  • Dermatologic: pruritus, rash
  • Respiratory: dyspnea
  • Other Clinical Events: temperature change, rigors, allergic reactions
5DESCRIPTION
Levoleucovorin is a folate analog and the pharmacologically active levo-isomer of
Levoleucovorin Chemical Structure
Levoleucovorin is a slightly hygroscopic, crystalline, yellow powder which is soluble in water when pH is at or above 8.
KHAPZORY 175 mg is a sterile lyophilized powder consisting of 175 mg levoleucovorin, 29.6 mg sodium hydroxide, and 105 mg mannitol in each vial. Additional sodium hydroxide and/or hydrochloric acid may be used to adjust the pH during manufacture. It is intended for intravenous administration after reconstitution with 3.6 mL of sterile 0.9% Sodium Chloride Injection, USP.
6HOW SUPPLIED/STORAGE AND HANDLING
KHAPZORY (levoleucovorin) for injection is a sterile, preservative-free, white to yellowish lyophilized powder in a single-dose vial. It is available as:
175 mg vial –NDC 72893-004-01.
Distributed by:
KHAPZORY is a registered trademark of Acrotech Biopharma Inc.
7PACKAGE/LABEL PRINCIPAL DISPLAY PANEL
carton-175
Carton Label
NDC 72893-004-01
175 mg/vial
For Intravenous use only
Single-dose vial
vial-175
Vial Label
NDC 72893-004-01
175 mg/vial
For Intravenous use only
Single-dose vial