maraviroc (Rx)

Brand and Other Names:Selzentry
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 150mg; 300mg

oral solution

  • 20mg/mL

HIV-1 Infection

Indicated in combination with other antiretroviral agents for treatment of only CCR5-tropic human immunodeficiency virus type 1 (HIV-1) infection

General dosage recommendations

Administer PO BID

Must be given in combination with other antiretroviral medications

Recommended dose differs based on concomitant medications owing to drug interactions

Recommended dosage differs based on concomitant medications owing to drug interactions; examples are listed below (ie, not an exhaustive list)

Noninteracting concomitant medications

  • 300 mg PO BID
  • Noninteracting drugs include: tipranavir/ritonavir, dolutegravir, nevirapine, raltegravir, all NRTIs, and enfuvirtide
  • Also, all other medications that are not potent CYP3A inhibitors or inducers

Potent CYP3A inhibitors (with or without a potent CYP3A inducer)

  • 150 mg PO BID
  • Potent CYP3A inhibitors include: protease inhibitors (except tipranavir/ritonavir), elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, cobicistat, nefazodone, and telithromycin

Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor)

  • 600 mg PO BID
  • Potent and moderate CYP3A inducers include: efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, and phenytoin

Dosage Modifications

Renal impairment

  • Mild-to-moderate (CrCl 30-80 mL/min): No dosage adjustment required
  • Severe (CrCl <30 mL/min)
    • Coadministered with potent CYP3A inhibitors: Contraindicated
    • Coadministered with noninteracting medications: No dose adjustment required
    • Coadministered with potent and moderate CYP3A inducers: Contraindicated
  • ESRD on hemodialysis
    • Coadministered with potent CYP3A inhibitors: Contraindicated
    • Coadministered with noninteracting medications: Reduce to 300 mg qDay
    • Coadministered with potent and moderate CYP3A inducers: Contraindicated

Hepatic impairment

  • Mild to moderate impairment: Serum concentrations increased but dose adjustment not recommended; monitor
  • Moderate impairment and strong CYP 3A4 inhibitor: Use caution; monitor closely for adverse reactions
  • Maraviroc concentrations are higher when 150 mg BID administered in patients with moderate hepatic impairment who are taking a potent CYP3A inhibitor compared with 300 mg BID without a CYP3A inhibitor
  • Severe impairment: Not studied

Dosing Considerations

Limitations of use

  • Not recommended in patients with dual/mixed- or CXCR4-tropic HIV-1

Testing before initiating

  • Test all patients for CCR5 tropism using a highly sensitive tropism assay
  • Only indicated for patients with CCR5-tropic HIV-1 infection
  • Outgrowth of pre-existing low-level CXCR4- or dual/mixed-tropic HIV-1 not detected by tropism testing at screening has been associated with virologic failure on maraviroc
  • Monitor ALT, AST, and bilirubin prior to initiating, and periodically during treatment

Dosage Forms & Strengths

tablet

  • 25mg
  • 75mg
  • 150mg
  • 300mg

oral solution

  • 20mg/mL

HIV-1 Infection

Indicated in combination with other antiretroviral agents for treatment of only CCR5-tropic human immunodeficiency virus type 1 (HIV-1) infection in patients weighing at least 2 kg

General dosing recommendations

  • Administer PO BID
  • Must be given in combination with other antiretroviral medications
  • Recommended dose differs based on concomitant medications owing to drug interactions

Aged 2 years and older weighing at least 10 kg (tablets)

  • Noninteracting concomitant medications
    • 10 kg to <14 kg: 150 mg PO BID
    • 14 kg to <30 kg: 200 mg PO BID
    • ≥30 kg: 300 mg PO BID
    • Noninteracting drugs include:dolutegrative, tipranavir/ritonavir, nevirapine, raltegravir, all NRTIs, and enfuvirtide
    • Also, all other medications that are not potent CYP3A inhibitors or inducers
  • Potent CYP3A inhibitors (with or without a potent CYP3A inducer)
    • 10 kg to <20 kg: 50 mg PO BID
    • 20 kg to <30 kg: 75 mg PO BID
    • 30 kg to <40 kg: 100 mg PO BID
    • ≥40 kg: 150 mg PO BID
    • Potent CYP3A inhibitors include: protease inhibitors (except tipranavir/ritonavir), elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, nefazodone, and telithromycin
  • Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor)
    • Not recommended for children taking potent CYP3A inducers
    • Potent and moderate CYP3A inducers include: efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, and phenytoin

Pediatric patients weighing at least 2 kg (oral solution)

  • Noninteracting concomitant medications
    • 2 kg to <4 kg: 30 mg (1.5 mL) PO BID
    • 4 kg to <6 kg: 40 mg (2 mL) PO BID
    • 6 kg to <10 kg: 100 mg (5 mL) PO BID
    • 10 kg to <14 kg: 150 mg (7.5 mL) PO BID
    • 14 kg to <30 kg: 200 mg (10 mL) PO BID
    • ≥30 kg: 300 mg (15 mL) PO BID
  • Potent CYP3A inhibitors (with or without a potent CYP3A inducer)
    • 2 kg to <10 kg: Not recommended
    • 10 kg to <20 kg: 50 mg (2.5 mL) PO BID
    • 20 kg to <30 kg: 80 mg (4 mL) PO BID
    • 30 kg to <40 kg: 100 mg (5 mL) PO BID
    • ≥40 kg: 150 mg (7.5 mL) PO BID
  • Potent CYP3A inducers (without a potent CYP3A inhibitor)
    • NOT recommended for children taking potent CYP3A inducers
    • Potent and moderate CYP3A inducers include: efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, and phenytoin

Dosage Modifications

Renal impairment

  • Mild-to-moderate (CrCl 30-80 mL/min): Data are not available to recommend specific doses in children
  • Patients with severe impairment or ESRD on hemodialysis who are also taking potent CYP3A inhibitors or inducers: Contraindicated

Dosing Considerations

Limitations of use

Not recommended in patients with dual/mixed- or CXCR4-tropic HIV-1

Testing before initiating

  • Test all patients for CCR5 tropism using a highly sensitive tropism assay
  • Only indicated for patients with CCR5-tropic HIV-1 infection
  • Outgrowth of pre-existing low-level CXCR4- or dual/mixed-tropic HIV-1 not detected by tropism testing at screening has been associated with virologic failure on maraviroc
  • Monitor ALT, AST, and bilirubin prior to initiating, and periodically during treatment
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Interactions

Interaction Checker

and maraviroc

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Upper respiratory infections (20%)

            Arthritis and musculoskeletal S/S (15%)

            Cough (13%)

            Pyrexia (12%)

            Rash (11%)

            Fever (13%)

            2-10%

            Dizziness (9%)

            Appetite disorder (8%)

            Herpes infection (8%)

            Bronchitis (7%)

            Sinusitis (7%)

            Constipation (6%)

            Apocrine and eccrine gland disorder (5%)

            Paresthesia/dysesthesia (5%)

            Renal/urinary disorder (3-5%)

            Depression (4%)

            Disturbed consciousness (4%)

            Periph neuropathies (4%)

            Pruritus (4%)

            Sensory abnormalities (4%)

            Folliculitis (3%)

            Hypertension (3%)

            Lipodystrophy (3%)

            Muscle pain (3%)

            Influenza (2%)

            Pneumonia (2%)

            Condyloma acuminata

            Dermatitis/eczema

            Dyspepsia

            GI pain

            Stomatitis/ulceration

            <2% (critical ADRs)

            CBN

            Cardiac disorder

            CVA

            Hepatic cirrhosis

            Hepatic failure

            Neoplasms

            C. difficile colitis

            Viral meningitis

            Pneumonia

            Septic shock

            Myositis

            Osteonecrosis

            Rhabdomyolysis

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            Warnings

            Black Box Warnings

            Hepatotoxicity reported; may be preceded by systemic allergic reaction (eg, pruritic rash, eosinophilia, elevated IgE)

            Immediately evaluate if signs or symptoms of hepatitis or allergic reaction occur

            Contraindications

            Hypersensitivity

            Severe renal impairment or end-stage renal disease (CrCl <30 mL/min) in patients taking potent CYP3A4 inhibitors or inducers

            Cautions

            Risks of hepatotoxicity

            Risk of immune reconstitution syndrome if used in combination with other antiretroviral drugs

            Autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) reported in the setting of immune reconstitution, however, the time to onset is more variable, and can occur many months after initiation of treatment

            Do not use in treatment-naïve patients; more likely to experienced virologic failure and developed lamivudine resistance compared to efavirenz

            Tropism testing with a highly sensitive tropism assay is required for the appropriate use

            Evaluate if signs/symptoms of hepatitis, increase LFTs, or rash develop

            Preexisting liver dysfunction or viral hepatitis B or C coinfection

            Patient history of increased risk for cardiovascular events

            History of postural hypotension or concomitant use of blood pressure lowering medication

            Caution in renal and hepatic impairment; postural hypotension reported in patients with renal impairment

            Monitor for developing infections

            When administering to patients with pre-existing liver dysfunction or who are co-infected with hepatitis B and/or C virus, additional monitoring may be warranted

            Cardiovascular adverse events triggered by postural hypotension’ additional monitoring may be warranted

            Antiretroviral Pregnancy Registry has been established.to monitor maternal-fetal outcomes of pregnant women; register patients by calling 1-800-258-4263

            Drug interaction overview

            • Drug is metabolized by CYP3A, and is also a substrate for P-glycoprotein (P-gp), organic anion-transporting polypeptide (OATP)1B1, and multidrug resistance-associated protein (MRP)2; pharmacokinetics of maraviroc are likely to be modulated by inhibitors and inducers of CYP3A and P-gp, and may be modulated by inhibitors of OATP1B1 and MRP2; therefore, dosage adjustment may be required when maraviroc is coadministered with those drugs
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            Pregnancy & Lactation

            Pregnancy: Limited data on pregnancy from the APR and case reports are not sufficient to inform a drug-associated risk of birth defects and miscarriage; n animal reproduction studies, no evidence of adverse developmental outcomes observed with maraviroc

            Lactation: Centers for Disease Control and Prevention recommend that HIV-1-infected mothers in United States not breastfeed their infants to avoid risking postnatal transmission of HIV-1 infection

            There are no data on presence of maraviroc in human milk, effects on breastfed infant, or effects on milk production; when administered to lactating rats, maraviroc was present in milk; because of potential for (1) HIV transmission (in HIV-negative infants), (2) developing viral resistance (in HIV-positive infants), and (3) serious adverse reactions in a breastfed infant similar to those seen in adults, instruct mothers not to breastfeed if they are receiving therapy

            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

            Selective antagonist of the interaction between human CCR5 and HIV-1 gp120; blocking this interaction prevents CCR5-tropic HIV-1 entry into cells

            Absorption

            Bioavailability: 23-33%

            Peak plasma time: 0.5-4 hr

            Peak plasma concentration: 333 ng/mL (330 mg BID)

            Distribution

            Protein bound: 76%

            Vd: 194 L

            Metabolism

            Metabolized by cytochrome P450 system, with CYP3A as major enzyme of metabolism

            Elimination

            Half-life: 14-18 hr

            Excretion: 76% (feces); 20% (urine)

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            Administration

            Oral Administration

            Tablets and oral solution are taken twice daily

            May take with or without food

            Must be given in combination with other antiretroviral medications

            The recommended dosage of maraviroc differs based on concomitant medications owing to drug interactions

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            Formulary

            FormularyPatient Discounts

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            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.
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