Glucarpidase
Glucarpidase is an enzyme used to rapidly lower dangerously high methotrexate levels in the blood when the kidneys cannot clear methotrexate fast enough.
🧬 Where this information comes from
The clinical label records used on this page are FDA-filed Structured Product Labeling (SPL) retrieved through openFDA. We identified 1 clinical label set within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. Forms, routes, brands, labelers, strengths, and NDC product-record counts are built separately from matching FDA National Drug Code Directory records. The linked DailyMed document is a representative official source for verification, not the page’s only clinical source. View the linked label on DailyMed →
Glucarpidase (Voraxaze) is a specialist rescue drug, on the U.S. market since about 2012, for when methotrexate builds to dangerous levels because the kidneys cannot clear it. This engineered enzyme breaks methotrexate into inactive pieces within minutes, a cleanup route that does not depend on the kidneys. Most people handle the single IV dose, given in a supervised hospital setting, quite well, and the side effects reported, such as tingling, flushing, nausea or headache, tend to be mild. The one thing to watch for is an allergic reaction or a drop in blood pressure, so speak up right away about rash, trouble breathing, swelling or feeling faint.
Clinical pearls
- For up to 48 hours afterward, standard methotrexate blood tests read falsely high, so the lab must use a different method called chromatography.
- Glucarpidase also lowers leucovorin levels, so leucovorin is given at least 2 hours before or after the injection.
- It is not given when methotrexate is clearing on schedule, because lowering it then could weaken the cancer treatment.
- Tell the team about any other folate-related medicines, since glucarpidase may lower their levels too.
Patient Information Guide A plain-language walkthrough of Glucarpidase, written from its FDA label.
What Glucarpidase Is Used For
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Glucarpidase is used to rapidly lower methotrexate to safe levels when the kidneys cannot clear it fast enough after high-dose treatment.
- Voraxaze (intravenous injection) is approved to reduce toxic plasma methotrexate concentrations (greater than 1 micromole per liter) in adults and children with delayed methotrexate clearance due to impaired kidney function.
- Voraxaze is not recommended for patients whose methotrexate is clearing normally — lowering levels in those patients could make the cancer treatment less effective.
How Glucarpidase Works
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Glucarpidase is a lab-made (recombinant) bacterial enzyme. It breaks methotrexate down by clipping off a piece of the molecule, converting it into two inactive substances: DAMPA and glutamate. Because this process doesn't rely on the kidneys, it gives the body an entirely separate pathway to eliminate methotrexate — critical when kidney function is too impaired to do it on its own.
Glucarpidase Dosage
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Voraxaze is given as a single intravenous (IV) injection over 5 minutes in a hospital or clinical setting — it is not taken by mouth or self-administered at home. The IV line is flushed before and after the injection. Your care team will continue monitoring your methotrexate levels using the correct type of blood test and will adjust your leucovorin treatment based on those readings. Follow all instructions from your prescriber and care team exactly.
Dosing details from the FDA-approved label
From the Glucarpidase prescribing information (“Dosage and Administration”). Doses are set by your prescriber for your product, condition, kidney function and age — never change a dose on your own.
- Recommended dosage (glucarpidase, VORAXAZE)
- 50 Units per kilogram (kg) as a single intravenous injection administered over 5 minutes
- Flush intravenous line before and after administration
- Concomitant leucovorin rescue: first 48 hours after a dose of VORAXAZE
- Administer the same leucovorin dosage given prior to the VORAXAZE dose
- Administer leucovorin at least 2 hours before or 2 hours after the VORAXAZE dose
- Concomitant leucovorin rescue: beyond 48 hours after a dose of VORAXAZE
- Determine the leucovorin dosage based on the measured methotrexate concentration
- Continue leucovorin until the methotrexate concentration has been maintained below the leucovorin rescue threshold for a minimum of 3 days
- Do not discontinue leucovorin based on a single methotrexate concentration below the leucovorin rescue threshold
Read the label’s full dosing text
2 DOSAGE AND ADMINISTRATION The recommended dosage of VORAXAZE is 50 Units per kilogram as a single intravenous injection over 5 minutes. ( 2.1 ). For the first 48 hours after the dose of VORAXAZE, administer the same leucovorin dose given prior to VORAXAZE. Administer leucovorin at least 2 hours before or 2 hours after the dose of VORAXAZE. ( 2.2 ) Beyond 48 hours after the dose of VORAXAZE, administer leucovorin based on the measured methotrexate concentration. Continue leucovorin until the methotrexate concentration has been maintained below the leucovorin treatment threshold for a minimum of 3 days. ( 2.2 ) 2.1 Recommended Dosage The recommended dosage of VORAXAZE is 50 Units per kilogram (kg) as a single intravenous injection administered over 5 minutes. Flush intravenous line before and after administration. 2.2 Concomitant Use with Leucovorin Rescue When administering VORAXAZE concomitantly with leucovorin, administer leucovorin at least 2 hours before or 2 hours after the VORAXAZE dose [see Drug Interactions ( 7.1 )] . For the first 48 hours after a dose of VORAXAZE: Administer the same leucovorin dosage given prior to the VORAXAZE dose. Beyond 48 hours after a dose of VORAXAZE : Determine the leucovorin dosage based on the measured methotrexate concentration. Do not discontinue leucovorin based on the determination of a single methotrexate concentration below the leucovorin rescue threshold. Continue leucovorin until the methotrexate concentration has been maintained below the leucovorin rescue threshold for a minimum of 3 days. Continue intravenous hydration and urinary alkalinization as indicated. When measuring methotrexate concentrations following a VORAXAZE dose, a chromatographic method is preferred over an immunoassay [see Warnings and Precautions ( 5.2 )] . 2.3 Preparation Reconstitute the contents of the vial with 1 mL of 0.9% Sodium Chloride Injection, USP. Roll and tilt the vial gently to mix. Do not shake. Inspect the vial and discard VORAXAZE if the solution is not clear, colorless, and free of particulate matter. Use reconstituted VORAXAZE immediately or store under refrigeration at 36° to 46°F (2° to 8°C) for up to 4 hours if not used immediately. VORAXAZE contains no preservative and is supplied as a single-dose vial. Discard any unused product.
Read the full Dosage and Administration section on DailyMed →
Glucarpidase Side Effects
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The most common side effects reported with Voraxaze include:
Common side effects
- Tingling or numbness (paresthesia)
- Flushing, feeling hot, or burning sensation
- Nausea and/or vomiting
- Headache
- Low blood pressure (hypotension)
- Blurred vision
When to get medical help
- Get emergency medical help immediately if you notice signs of a serious allergic reaction: rash, difficulty breathing, swelling, or severe dizziness.
- Tell your care team right away if you feel your blood pressure dropping, feel faint, or have severe flushing during or after the injection.
Serious allergic reactions have occurred in less than 1% of patients — get immediate medical help if you have trouble breathing, swelling, or feel faint during or after the infusion.
Glucarpidase Warnings and Precautions
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- Serious allergic (hypersensitivity) reactions: Though rare (less than 1% of patients), serious reactions can happen. You will be monitored closely by your care team during and after the injection.
- Inaccurate methotrexate blood tests for 48 hours: After Voraxaze, a byproduct called DAMPA interferes with the standard immunoassay blood test for methotrexate, causing it to read falsely high. For up to 48 hours after your dose, only a chromatographic test gives an accurate methotrexate level. Your care team is responsible for using the right test — this is important so that leucovorin dosing decisions are made correctly.
Glucarpidase Interactions
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Voraxaze has two key interactions your care team needs to manage carefully:
- Leucovorin (folinic acid): Voraxaze can lower leucovorin levels in the blood. To protect the effectiveness of leucovorin rescue, leucovorin must be given at least 2 hours before or 2 hours after the Voraxaze dose — not at the same time. Your leucovorin schedule will be adjusted by your care team around the Voraxaze dose.
- Other folate analog drugs: Voraxaze may also reduce the levels of other medications that are folate analogs or folate analog metabolic inhibitors — make sure your care team knows all medications you are taking.
- Methotrexate immunoassay tests: Voraxaze causes DAMPA to appear in the blood, which falsely inflates immunoassay readings for methotrexate for up to 48 hours — chromatographic testing must be used during this window for accurate results.
Interactions listed in the FDA-approved label
From the Glucarpidase prescribing information (“Drug Interactions”): what the manufacturer studied or reported to the FDA.
- Leucovorin: VORAXAZE can decrease leucovorin concentration, which may decrease the effect of leucovorin rescue unless leucovorin is dosed as recommended. Administer leucovorin at least 2 hours before or 2 hours after the VORAXAZE dose; for the first 48 hours give the same leucovorin dose as prior to VORAXAZE, and beyond 48 hours dose based on measured methotrexate concentration.
- Other folate analogs or folate analog metabolic inhibitors: VORAXAZE may also reduce the concentrations of other folate analogs or folate analog metabolic inhibitors.
- Methotrexate concentration measurement by immunoassay: DAMPA, an inactive metabolite of methotrexate formed after VORAXAZE, interferes with immunoassay measurement and results in an overestimation of the methotrexate concentration, for approximately 48 hours following a VORAXAZE dose. When measuring methotrexate concentration following a VORAXAZE dose, a chromatographic method is preferred over an immunoassay.
Read the label’s full interactions text
7 DRUG INTERACTIONS 7.1 Effects of VORAXAZE on Leucovorin VORAXAZE can decrease leucovorin concentration, which may decrease the effect of leucovorin rescue unless leucovorin is dosed as recommended [see Dosage and Administration ( 2.2 ), Clinical Pharmacology ( 12.3 )] . VORAXAZE may also reduce the concentrations other folate analogs or folate analog metabolic inhibitors. 7.2 Effect of VORAXAZE on Measurement of Methotrexate Concentration DAMPA (4-deoxy-4-amino-N10- methylpteroic acid), an inactive metabolite of methotrexate formed following VORAXAZE administration, interferes with the measurement of methotrexate concentration using immunoassays. This interference results in an overestimation of the methotrexate concentration. Based on the half-life of DAMPA, VORAXAZE may interfere with the measurement of methotrexate concentrations for approximately 48 hours following a VORAXAZE dose [see Warnings and Precautions ( 5.2 )] . When measuring methotrexate concentration following a VORAXAZE dose, a chromatographic method is preferred over an immunoassay.
Not a complete list. The label covers the interactions the manufacturer studied or reported, and our own interaction database does not cover every medicine either. Bring your full medication list, including vitamins and herbal products, to your pharmacist.
Before Taking Glucarpidase
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- Pregnancy: There are no human data on Voraxaze use in pregnancy. Voraxaze is given alongside methotrexate, which is known to cause harm to a developing baby — discuss risks with your doctor.
- Breastfeeding: It is not known whether glucarpidase passes into breast milk. Voraxaze is given with methotrexate, which carries its own breastfeeding risks — ask your doctor before breastfeeding.
- Children: Voraxaze is approved for pediatric patients and has been studied in children from 1 month to 17 years of age. No overall differences in safety were found compared to adults.
- Older adults: Patients 65 and older received Voraxaze in clinical studies with no overall differences in safety or effectiveness compared to younger adults.
- Kidney impairment: Voraxaze is specifically used in patients with impaired kidney function — it does not require dose adjustment for renal impairment based on available pharmacokinetic data.
What Glucarpidase Does in the Body
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After a single Voraxaze dose, methotrexate levels measured by a chromatographic method dropped by 97% or more within just 15 minutes in clinical study patients. This reduction was sustained — more than 95% below pre-treatment levels — for up to 8 days in nearly all patients studied. This rapid, sustained reduction is what makes Voraxaze effective at rescuing patients from methotrexate toxicity.
How Your Body Processes Glucarpidase
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After intravenous injection, glucarpidase distributes into a relatively small volume — meaning it stays fairly concentrated in the bloodstream rather than spreading widely into tissues. Its activity in the blood declines with a half-life of about 5 to 6 hours, while total glucarpidase concentration has a somewhat longer half-life of about 9 hours. The drug is cleared from the body with a mean systemic clearance of 7.5 mL/min. In patients with severe kidney impairment, the pharmacokinetics of glucarpidase itself are not significantly affected — the kidneys do not appear to play a major role in clearing glucarpidase from the body.
How to Store Glucarpidase
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Store VORAXAZE refrigerated at 36°F to 46°F (2°C to 8°C). Do not freeze.
Written from the FDA-approved label with AI and reviewed by our pharmacy team. How we use AI →
Glucarpidase: Pharmacist Answers to Common Questions
Quick, plain-English answers to the questions patients ask most about Glucarpidase — the kind of thing our pharmacy team would talk through with you at the counter.
What exactly does Voraxaze do, and why do I need it?
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How is Voraxaze given, and will I need more than one dose?
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What side effects should I watch out for after getting Voraxaze?
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I'm also getting leucovorin — does Voraxaze affect that?
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Why does my doctor need to use a special blood test to check methotrexate levels after Voraxaze?
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Is Voraxaze safe for children, and are there concerns about pregnancy?
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Is Glucarpidase available over the counter?
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When was Glucarpidase first available?
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Answers drafted from the FDA-approved label with AI and reviewed by our pharmacy team. How we use AI →
More About Glucarpidase on HelloPharmacist
Glucarpidase Forms and Strengths (How It Comes)
Glucarpidase is available in 1 form. Different forms and brands can have different approved uses, doses, schedules, and directions. Follow the instructions for your exact product, and do not switch forms without guidance from your prescriber or pharmacist.
Need a version that does not list lactose, a gluten source, a dye or gelatin? Inactive ingredients differ by manufacturer: see Glucarpidase inactive ingredients by manufacturer.
Injection
How this form is used
- Voraxaze is used intravenously to reduce toxic plasma methotrexate concentrations (above 1 micromole per liter) in adults and children whose kidneys are not clearing methotrexate fast enough after high-dose treatment.
- Voraxaze is not indicated for patients who are clearing methotrexate at the expected rate.
- Voraxaze is given as a single intravenous injection administered over 5 minutes by a healthcare provider.
- Voraxaze: flush the IV line before and after administration.
- Voraxaze must be reconstituted with 1 mL of 0.9% Sodium Chloride — roll and tilt gently to mix, do not shake; use immediately or refrigerate for up to 4 hours.
- When given alongside leucovorin, Voraxaze requires leucovorin to be administered at least 2 hours before or 2 hours after the Voraxaze dose.
Glucarpidase on the U.S. Market: Products, Makers and Brands
How Glucarpidase appears in the FDA’s National Drug Code Directory — including its dosage forms, strengths, brand names, manufacturers, and FDA-listed product records. These are directory records, not sales or prescription volume.
1 company lists 1 Glucarpidase product record with the FDA, mostly as injection; the earliest marketing or approval year on record is 2012. Brand names on the directory include Voraxaze; the rest are generics.
Also listed with the FDA, not a patient dose form: Unfinished liquid (1) — bulk drug substance and unfinished product sold to compounders and other manufacturers to finish, and multi-item kits. These aren’t counted in the dose-form total above.
Compare Glucarpidase Products
A representative set of FDA-listed product records for Glucarpidase — across manufacturers, strengths, and dosage forms, grouped by form with each product’s manufacturer and how the FDA approved it. The same medicine may be made and packaged by different companies, so a single drug can have many directory entries. (It’s also why a refill can look different — a new shape, color, or box — even though it contains the same medication.)
| Strength | Route | Manufacturer / Labeler | Category ⓘ | Details |
|---|---|---|---|---|
| 💊Injection | ||||
| 1000 [USP'U] | Intravenous | BTG International Inc. | BLA | View NDC → |
Showing 1 of 1 products — FDA National Drug Code Directory. See every product, package size and price: browse all 1 Glucarpidase NDCs →
Glucarpidase Side Effects Reported to the FDA (FAERS)
After a medicine reaches the market, patients, doctors and drugmakers can send the FDA reports of problems they think may be linked to it. Here’s what’s been reported for Glucarpidase — a signal of what to watch for, not proof the drug caused it.
Source: openFDA, from the FDA Adverse Event Reporting System (FAERS). These are voluntary reports — they don’t prove the drug caused the effect, and counts reflect how often something was reported, not how often it actually happens. Reports also often name the very problem the medicine is taken for — a common reason to file one is that the drug didn’t help — so for a pain reliever you may see “pain” high on the list; that points to why the report was filed, not to the drug causing the symptom. This counts every report that lists Glucarpidase in any role, so the total runs higher than the FDA’s official dashboard, which counts only cases where the drug is the suspect. For the authoritative figures, see the FDA FAERS Public Dashboard. Always talk to your pharmacist or doctor.
Glucarpidase FDA Approval History
How Glucarpidase went from FDA review to the pharmacy shelf — the key milestones in its regulatory journey.
Source: Drugs@FDA.
Glucarpidase Recall History
A recall is when a specific batch of a medicine is pulled from the market — usually a manufacturing issue, not a problem with the drug itself. Class I is most serious, Class III least.
The FDA’s enforcement reports list no Glucarpidase recalls since July 2021.
✅No Glucarpidase recalls on record since July 2021Source: FDA enforcement (recall) reports, via openFDA; our copy was last updated Oct 8, 2026.
RxNorm Concept Web — From Ingredient to Every Form and Strength
This page starts with one ingredient concept (IN). The branches below show its dose-form concepts (SCDF), then the available clinical drug and strength concepts (SCD). Combination products remain separate concepts with their own pages.
RxCUI 1242127 1 dose form · 1 strength
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Dose form (SCDF) Injection RxCUI 1739546In current FDA listingsClinical drug / strength (SCD) 1000 UNTRxCUI 1242131
Look up RxCUI 1242127 in the RxCUI Atlas →
RxNorm is the U.S. National Library of Medicine’s normalized drug vocabulary. Its concept hierarchy can include forms that are not currently marketed; the status on each branch compares that concept with current FDA listings. RxCUIs identify vocabulary concepts, not individual packages or manufacturers.
Glucarpidase Supply and Shortage Status
Whether Glucarpidase is in short supply in the U.S. right now, plus any shortage history the FDA has on record. A shortage usually reflects a manufacturing or demand issue — not a safety problem with the drug.
Source: openFDA, from the FDA Drug Shortages database.
Glucarpidase Brand Names
Glucarpidase is sold under one brand name in the FDA directory — Voraxaze. A brand and its generic contain the same active ingredient; the brand name belongs to one company's product.
Who Makes Glucarpidase: Manufacturers and Labelers
One company lists Glucarpidase products with the FDA. By number of product records, the largest are BTG International Inc.. Labelers include manufacturers and repackagers; the product in your bottle depends on which one your pharmacy stocks.
Sources for This Glucarpidase Page
Core label, product, RxNorm, safety, and utilization data on this page come from the sources identified below. AI-written, editorial, and licensed sections are labeled separately.
How this page is built
HelloPharmacist combines public FDA and NLM records and does not author the underlying clinical facts. The plain-language sections are written with AI from the FDA-approved label text and reviewed by our pharmacy team before publication. BTG International Inc. is the representative DailyMed label linked for verification and dates. This is general education, not medical advice: always talk to your doctor or pharmacist about your own medicines. How we build and review drug pages →