voxelotor (Rx)

Brand and Other Names:Oxbryta
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 500 mg

Sickle Cell Disease

Indicated for treatment of sickle cell disease

1500 mg PO qDay

May take with or without hydroxyurea

Dosage Modifications

Renal impairment

  • Mild, moderate, or severe: No dose adjustment required
  • End-stage renal disease: Not studied

Hepatic impairment

  • Mild-to-moderate (Child-Pugh A or B): No dose adjustment required
  • Severe (Child-Pugh C): Decrease dose to 1000 mg PO qDay

Drug interactions requiring dose modification

  • Strong CYP3A4 inhibitor or fluconazole: Decrease dose to 1000 mg PO qDay
  • Moderate or strong CYP3A4 inducers: Increase dose to 2500 mg PO qDay

Dosage Forms & Strengths

tablet

  • 500 mg

Sickle Cell Disease

Indicated for treatment of sickle cell disease in adults and pediatric patients aged ≥12 years

<12 years: Safety and efficacy not established

≥12 years: 1500 mg PO qDay

May take with or without hydroxyurea

Dosage Modifications

Renal impairment

  • Mild, moderate, or severe: No dose adjustment required
  • End-stage renal disease: Not studied

Hepatic impairment

  • Mild-to-moderate (Child-Pugh A or B): No dose adjustment required
  • Severe (Child-Pugh C): Decrease dose to 1000 mg PO qDay

Drug interactions requiring dose modification

  • Strong CYP3A4 inhibitor or fluconazole: Decrease dose to 1000 mg PO qDay
  • Moderate or strong CYP3A4 inducers: Increase dose to 2500 mg PO qDay
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Interactions

Interaction Checker

and voxelotor

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Headache (26%)

            Diarrhea (20%)

            Abdominal pain (19%)

            Nausea (17%)

            Fatigue (14%)

            Rash (14%)

            Pyrexia (12%)

            1-10%

            Drug hypersensitivity (<10%)

            <1%

            Serious hypersensitivity

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            Warnings

            Contraindications

            Hypersensitivity; clinical manifestations may include generalized rash, urticaria, mild shortness of breath, mild facial swelling, and eosinophilia

            Cautions

            Serious hypersensitivity reactions have occurred in <1% of patients treated

            Voxelotor may interfere with laboratory measurement of Hb subtypes (HbA, HbS, and HbF) by high-performance liquid chromatography (HPLC)

            Drug interaction overview

            • Strong CYP3A4 inhibitors or fluconazole
              • Avoid coadministration with strong CYP3A4 inhibitors or fluconazole
              • Decrease voxelotor dose if unable to avoid
            • Strong or moderate CYP3A4 inducers
              • Avoid coadministration with strong or moderate CYP3A4 inducers
              • Increase voxelotor dose if unable to avoid
            • Effect of voxelotor on other drugs
              • Voxelotor increased the systemic exposure of midazolam (a sensitive CYP3A4 substrate)
              • Avoid co-administration with sensitive CYP3A4 substrates with a narrow therapeutic index
              • Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid
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            Pregnancy & Lactation

            Pregnancy

            Data are not available regarding use in pregnant women to evaluate for drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes

            Animal data

            • Administration 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

            Clinical considerations

            • Women with sickle cell disease 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

            Lactation

            Data are not available on the presence of voxelotor in human milk, effects on the breastfed child, or effects on milk production

            Voxelotor was detected in milk in lactating rats; plasma concentrations of voxelotor in pregnant rats were higher than the concentration in milk

            Advise women not to breastfeed during treatment and for at least 2 weeks after the last dose

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Voxelotor is a hemoglobin S (HbS) polymerization inhibitor that binds to HbS with a 1:1 stoichiometry and exhibits preferential partitioning to RBCs

            By increasing the affinity of Hb for oxygen, voxelotor demonstrates dose-dependent inhibition of HbS polymerization

            Nonclinical studies suggest voxelotor may inhibit RBC sickling, improve RBC deformability, and reduce whole blood viscosity

            Absorption

            Peak plasma and whole blood time: 2 hr; peak concentration in whole blood and RBCs 6-12 hr

            Peak plasma concentration: 12.6 mcg/mL (plasma); 179 mcg/mL (whole blood)

            AUC: 246 mcg⋅hr/mL (plasma); 3820 mcg⋅hr/mL (whole blood)

            Distribution

            Protein bound: 99.8%

            Vd

            • Central compartment, plasma: 338 L
            • Peripheral compartment, plasma: 72.2 L

            Metabolism

            Extensively metabolized through Phase I (oxidation and reduction), Phase II (glucuronidation), and combinations of Phase I and II metabolism

            Oxidation mediated primarily by CYP3A4, with minor contribution from CYP2C19, CYP2B6, and CYP2C9

            Elimination

            Half-life: 35.5 hr

            Excretion: Feces 62.6%; urine 35.5%

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            Administration

            Oral Administration

            May take with or without food

            Swallow tablets whole; do not cut, crush, or chew

            Missed dose: Continue dosing on the day following the missed dose

            Storage

            Store at or below 30ºC (86ºF)

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            Images

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.