Voxelotor
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From MedlinePlus, U.S. National Library of Medicine
Hemoglobin S Polymerization Inhibitor
Dosing in kidney impairment
Drug reaction with eosinophilia and systemic symptoms (DRESS) has been reported in postmarketing experience with OXBRYTA [see Adverse Reactions ] . Patients who develop a combination of skin rash, fever, peripheral eosinophilia, and internal systemic organ involvement (e.g., hepatic, renal, pulmonary) while receiving OXBRYTA should undergo medical evaluation.
Dosing in liver impairment
Recommended Dosage for Adults and Pediatric Patients 12 Years and Older with Hepatic Impairment The recommended dosage of OXBRYTA in adults and pediatric patients 12 years and older with severe hepatic impairment (Child Pugh C) is 1,000 mg orally once daily. No dosage adjustment of OXBRYTA is required for patients with mild or moderate hepatic impairment [ see Use in Specific Populations and Clinical Pharmacology ].
Recommended Dosage for Pediatric Patients 4 Years to Less Than 12 Years with Hepatic Impairment The recommended dosage of OXBRYTA in pediatric patients 4 years to less than 12 years with severe hepatic impairment (Child Pugh C) is described in Table 2. No dosage adjustment of OXBRYTA is required for patients with mild or moderate hepatic impairment [see Use in Specific Populations and Clinical Pharmacology ] . [See table below.] tablets for oral suspension or three 300 mg tablets) 20 kg to less than 40 kg 600 mg 10 kg to less than 20 kg 300 mg
| Body Weight | Recommended Dose (once daily) |
|---|---|
| 40 kg or greater | 1,000 mg (two 500 mg tablets) or 900 mg (three 300 mg tablets for oral suspension or three 300 mg tablets) |
| 20 kg to less than 40 kg | 600 mg |
| 10 kg to less than 20 kg | 300 mg |
Preparation and administration
Important Administration Instructions Administer OXBRYTA orally, once daily with or without food. If a dose is missed, or not administered entirely, resume dosing the following day. OXBRYTA may be given with or without hydroxyurea. OXBRYTA 300 mg and 500 mg Tablets Patients should swallow OXBRYTA tablets whole. Do not cut, crush, or chew the tablets.
OXBRYTA 300 mg Tablets for Oral Suspension Patients should disperse tablets for oral suspension immediately before administration in a cup and in room temperature clear liquid (such as drinking water, clear soda, apple juice, clear electrolyte drinks, clear flavored drinks, or clear sports drinks) before swallowing. Do not swallow whole, cut, crush, or chew the tablets for oral suspension. [See table below.]
After the tablets start to disintegrate, swirl the contents of the cup until the tablets are dispersed, wait 1 to 5 minutes, swirl the contents of the cup again, and then orally administer the contents of the cup. The tablet(s) will not completely dissolve; there will still be small tablet clumps in the mixture.
Resuspend any residue left in the cup in more clear drink and administer. Repeat until no tablet residue is left in the cup. Tablets for oral suspension may be substituted for tablets in adults and pediatric patients 12 years and older with difficulty swallowing the tablets. Use the number of tablets for oral suspension needed to achieve the recommended dose.
| Recommended Daily Dose | Number of Tablets for Oral Suspension | Minimum Recommended Volume of Clear Drink |
|---|---|---|
| 300 mg | 1 | 5 mL (1 teaspoon) |
| 600 mg | 2 | 10 mL (2 teaspoons) |
| 900 mg | 3 | 15 mL (3 teaspoons) |
| 1,200 mg | 4 | 20 mL (4 teaspoons) |
| 1,500 mg | 5 | 25 mL (5 teaspoons) |
| 2,100 mg | 7 | 35 mL (7 teaspoons) |
| 2,400 mg | 8 | 40 mL (8 teaspoons) |
Drug interactions
Check voxelotor against a medication listLabel text (4 paragraphs)
7 DRUG INTERACTIONS • Sensitive CYP3A4 Substrates: Avoid coadministration of sensitive CYP3A4 substrates with a narrow therapeutic index. ( 7.2 ) • Strong or moderate CYP3A4 Inducers: Avoid coadministration with strong or moderate CYP3A4 inducers. If unavoidable, increase the dose of OXBRYTA. ( 2.5 , 2.6 , 7.1 )
7.1 Effect of Other Drugs on Voxelotor Strong or Moderate CYP3A4 Inducers Coadministration of strong or moderate CYP3A4 inducers may decrease voxelotor plasma and whole blood concentrations and may lead to reduced efficacy. Avoid coadministration of OXBRYTA with strong or moderate CYP3A4 inducers. Increase the OXBRYTA dosage when coadministration with a strong or moderate CYP3A4 inducer is unavoidable [see Dosage and Administration (2.5 , 2.6) and Clinical Pharmacology (12.3) ].
7.2 Effect of Voxelotor on Other Drugs Voxelotor increased the systemic exposure of midazolam (a sensitive CYP3A4 substrate) [see Clinical Pharmacology (12.3) ]. Avoid coadministration of OXBRYTA with sensitive CYP3A4 substrates with a narrow therapeutic index. If concomitant use is unavoidable, consider dose reduction of the sensitive CYP3A4 substrate(s).
7.3 Laboratory Test Interference OXBRYTA administration may interfere with measurement of Hb subtypes (HbA, HbS, and HbF) by HPLC [see Warnings and Precautions (5.2) ]. If precise quantitation of Hb species is required, chromatography should be performed when the patient has not received OXBRYTA therapy in the immediately preceding 10 days.
Contraindications
4 CONTRAINDICATIONS OXBRYTA is contraindicated in patients with a history of serious drug hypersensitivity reaction to voxelotor or excipients. Clinical manifestations may include generalized rash, urticaria, mild shortness of breath, mild facial swelling, and eosinophilia [see Warnings and Precautions (5.1) and Adverse Reactions (6.1) ]. Prior drug hypersensitivity to voxelotor or excipients. ( 4 )
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Risk Summary There are no available data on OXBRYTA use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal reproduction studies, oral administration of voxelotor to pregnant rats and rabbits during organogenesis at exposures up to 2.8-times (rats) and 0.3-times (rabbits) the exposure at the maximum recommended human dose resulted in no adverse developmental effects (see Data ). The estimated background risk of major birth defects and miscarriage for the indicated population is approximately 14% and up to 43%, respectively.
All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. There are adverse effects on maternal and fetal outcomes associated with SCD in pregnancy (see Clinical Considerations ). OXBRYTA should only be used during pregnancy if the benefit of the drug outweighs the potential risk. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk Women with SCD have an increased risk of adverse pregnancy outcomes for the mother and the fetus. Pregnant women are at greater risk for vasoocclusive crises, pre-eclampsia, eclampsia, and maternal mortality.
For the fetus, there is an increased risk for intrauterine growth restriction, preterm delivery, low birth weight, and perinatal mortality. Data Animal Data In embryo-fetal development studies, voxelotor was administered orally to pregnant rats at 15, 50, and 250 mg/kg/day (gestation days 7 through 17) and rabbits at 25, 75, and 150 mg/kg/day (gestation days 7 through 19) through organogenesis. Maternal toxicity was observed at the highest dose levels in these studies equivalent to 2.8-times (rats) and 0.3-times (rabbits) the exposures in patients receiving OXBRYTA at the recommended daily dose. There was no evidence of adverse developmental outcomes in rats or rabbits.
In a pre- and postnatal development study, voxelotor was administered orally to pregnant rats at 15, 50 and 250 mg/kg/day (gestation day 6 through lactation day 20). Maternal gestational body weights were decreased at 250 mg/kg/day, which continued to the end of lactation. The findings in offspring included reduced survival and reduced body weights throughout lactation, weaning and maturation. The effects in offspring were observed at the maternal dose of 250 mg/kg/day with an exposure approximately 2.8-times the exposure in patients at the recommended dose.
For breastfeeding, also see LactMed (National Library of Medicine), which summarizes milk levels and infant effects.
Supply and cost
Drug shortage status
Recalls (last 24 months)
Therapeutic equivalence (Orange Book)
Price ladder
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