Voxelotor
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Omid Afkhami-Ardakani
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Overview
Voxelotor is a Hemoglobin S polymerization inhibitor that is FDA approved for the treatment of sickle cell disease (SCD) in adults and pediatric patients aged 4 years and older.. Common adverse reactions include Common Adverse Reactions (≥10% incidence): Headache, diarrhea, abdominal pain, nausea, rash, and pyrexia.
Note: As of September 2024, Pfizer has voluntarily withdrawn Oxbryta from all global markets due to safety concerns, including an increased risk of vaso-occlusive crises and fatalities..
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Treatment of sickle cell disease in adults: 1,500 mg orally once daily.
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Voxelotor in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Voxelotor in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
Treatment of sickle cell disease in pediatric patients aged 4 years and older: 10 kg to <20 kg: 600 mg once daily
20 kg to <40 kg: 900 mg once daily
≥40 kg: 1,500 mg once daily
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Voxelotor in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Voxelotor in pediatric patients.
Contraindications
Known hypersensitivity to voxelotor or any of its excipients
Warnings
Hypersensitivity Reactions: Monitor for signs and symptoms; discontinue if severe reactions occur.
Laboratory Test Interference: May interfere with hemoglobin subtyping assays.
Adverse Reactions
Clinical Trials Experience
Headache, diarrhea, abdominal pain, nausea, rash, and pyrexia.
Postmarketing Experience
There is limited information regarding Voxelotor Postmarketing Experience in the drug label.
Drug Interactions
CYP3A4 Inducers: Avoid concomitant use with strong or moderate CYP3A4 inducers; may decrease voxelotor efficacy.
Sensitive CYP3A4 Substrates: Avoid concomitant use with sensitive CYP3A4 substrates with a narrow therapeutic index.
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA):
There is no FDA guidance on usage of Voxelotor in women who are pregnant.
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Voxelotor in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Voxelotor during labor and delivery.
Nursing Mothers
It is advised against breastfeeding during treatment and for at least 2 weeks after the last dose.
Pediatric Use
Approved for use in patients aged 4 years and older.
Geriatic Use
There is no FDA guidance on the use of Voxelotor in geriatric settings.
Gender
There is no FDA guidance on the use of Voxelotor with respect to specific gender populations.
Race
There is no FDA guidance on the use of Voxelotor with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Voxelotor in patients with renal impairment.
Hepatic Impairment
Dose adjustment recommended for severe impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Voxelotor in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Voxelotor in patients who are immunocompromised.
Administration and Monitoring
Administration
Oral administration once daily, with or without food
Tablets should be swallowed whole; do not cut, crush, or chew.
Tablets for oral suspension should be dispersed in room temperature clear liquid and consumed immediately.
Monitoring
Monitor hemoglobin levels and signs of hemolysis.
Be aware of potential interference with hemoglobin subtyping assays.
IV Compatibility
Not applicable.
Overdosage
There is limited information regarding Voxelotor overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.
Pharmacology
There is limited information regarding Voxelotor Pharmacology in the drug label.
Mechanism of Action
Voxelotor binds to hemoglobin, increasing its affinity for oxygen, thereby inhibiting polymerization of hemoglobin S and preventing sickling of red blood cells.
Structure
There is limited information regarding Voxelotor Structure in the drug label.
Pharmacodynamics
Voxelotor increases hemoglobin's affinity for oxygen, thereby inhibiting HbS polymerization. Clinical studies have demonstrated that voxelotor treatment leads to dose-dependent increases in hemoglobin levels and reductions in markers of hemolysis, such as indirect bilirubin and reticulocyte counts.
Pharmacokinetics
Absorption: Voxelotor is rapidly absorbed after oral administration, with a plasma Tmax of approximately 2 hours.
Distribution: It preferentially partitions into red blood cells due to its high affinity for hemoglobin. The blood-to-plasma ratio is approximately 15:1 in patients with SCD.
Metabolism: Voxelotor is primarily metabolized by CYP3A4, with minor contributions from CYP2C19, CYP2B6, and CYP2C9. It undergoes oxidation, reduction, glucuronidation, and sulfation.
Elimination: The major route of elimination is metabolism, with subsequent excretion of metabolites into urine and feces. Less than 1% of the dose is excreted unchanged in urine.
Half-life: The terminal elimination half-life in patients with SCD is approximately 38.7 hours.
Nonclinical Toxicology
There is limited information regarding Voxelotor Nonclinical Toxicology in the drug label.
Clinical Studies
There is limited information regarding Voxelotor Clinical Studies in the drug label.
How Supplied
Voxelotor is supplied as film-coated tablets for oral administration in the following strengths:
300 mg tablets
500 mg tablets
Storage
Store at room temperature between 20°C to 25°C (68°F to 77°F).
Excursions permitted between 15°C to 30°C (59°F to 86°F).
Store in the original container to protect from moisture.
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
Voxelotor may cause side effects such as headache, diarrhea, abdominal pain, nausea, rash, and fever.
It can interfere with certain laboratory tests measuring hemoglobin subtypes; inform healthcare providers about voxelotor use before such tests.
Advise patients to take voxelotor exactly as prescribed and not to discontinue without consulting their healthcare provider.
Discuss the importance of adherence to therapy to achieve the desired treatment benefits.
Precautions with Alcohol
Alcohol-Voxelotor interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
Oxbryta®
Note: As of September 2024, Pfizer has voluntarily withdrawn Oxbryta from all global markets due to safety concerns, including an increased risk of vaso-occlusive crises and fatalities.
Look-Alike Drug Names
There is limited information regarding Voxelotor Look-Alike Drug Names in the drug label.
Price
References
The contents of this FDA label are provided by the National Library of Medicine.