II. Indications

  1. HIV Infection in either Antiretroviral naive or experienced patients (combination therapy)

III. Contraindications

  1. Creatinine Clearance <30 ml/min and use of a strong CYP3A4 inhibitor or inducer

IV. Mechanism

  1. HIV Entry Inhibitor (CCR5 Receptor Antagonist)
    1. Blocks HIV to Chemokine (CCR5 - R5) receptor binding on CD4+ Cells
    2. Blocks HIV entry into host cells
  2. Maraviroc is only effective on R5 cells
    1. Requires high sensitivity R5 tropism test prior to initiating Maraviroc

V. Medications: Maraviroc

  1. Tabs: 25, 75, 150 and 300 mg
  2. Solution: 20 mg/ml

VI. Dosing: Adult

  1. Strong CYP3A4 Inhibitors (e.g. Clarithromycin, Itraconazole, most HIV Protease Inhibitors except Tipranavir/r)
    1. Take 150 mg orally twice daily
    2. Avoid if Creatinine Clearance <30 ml/min
  2. Insignificant CYP3A4 Effects (e.g. nRTIs, Nevirapine, Raltegravir, Tipranavir/r)
    1. Take 300 mg orally twice daily
  3. Strong CYP3A4 Inducers (e.g. Carbamazepine, Efavirenz, Etravirine, Phenobarbital, Phenytoin, Rifampin)
    1. Take 600 mg orally twice daily
    2. Avoid if Creatinine Clearance <30 ml/min

VII. Dosing: Child (age >2 years, weight >=10 kg)

  1. Strong CYP3A4 Inhibitors (e.g. Clarithromycin, Itraconazole, most HIV Protease Inhibitors except Tipranavir/r)
    1. Weight 10 to 20 kg: Give 50 mg orally twice daily
    2. Weight 20 to 30 kg: Give 75 mg orally twice daily
    3. Weight 30 to 40 kg: Give 100 mg orally twice daily
    4. Weight >40 kg: Give 150 mg orally twice daily (adult dose)
    5. Avoid if Creatinine Clearance <30 ml/min
  2. Insignificant CYP3A4 Effects (e.g. nRTIs, Nevirapine, Raltegravir, Tipranavir/r)
    1. Weight >=30 kg: Give 300 mg orally twice daily (adult dose)
  3. Strong CYP3A4 Inducers (e.g. Carbamazepine, Efavirenz, Etravirine, Phenobarbital, Phenytoin, Rifampin)
    1. Avoid Maraviroc in children with concurrent use of strong CYP3A4 inducers

VIII. Adverse Effects

  1. Well tolerated overall
  2. Fever
  3. Upper respiratory symptoms (e.g. cough, Bronchitis)
  4. Abdominal Pain
  5. Orthostatic Hypotension
    1. More common with Renal Insufficiency
  6. Myalgia
  7. Increased Myocardial Infarction risk
  8. Hypersensitivity Rash
    1. DRESS Syndrome risk (rash and Eosinophilia)
    2. May be associated with hepatoxicity
    3. Stop Maraviroc immediately for signs of Hypersensitivity
  9. Hepatotoxicity
    1. Higher risk if comorbid Hepatitis B or Hepatitis CVirus infection
    2. Comorbid hepatic Impairment (esp. with strong CYP3A4 Inhibitor use) also increases other adverse effects
    3. May be associated with DRESS Syndrome
    4. Liver Function Tests baseline and periodically
    5. Stop Maraviroc immediately for signs of hepatotoxicity

IX. Drug Interactions

  1. Maraviroc is a substrate of CYP3A4 and very sensitive to the enzyme's activity (see dosing above)
  2. Contraindicated agents with Maraviroc
    1. Unboosted Fosamprenavir
    2. St Johns Wort

XI. References

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Related Studies

Cost: Medications

selzentry (on 1/1/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
SELZENTRY 150 MG TABLET $26.39 each
SELZENTRY 300 MG TABLET $26.46 each

Ontology: HIV Entry Inhibitors (C1449715)

Concepts Pharmacologic Substance (T121)
MSH D023581
English HIV ENTRY INHIB, Entry Inhibitors, HIV, HIV Entry Inhibitors
Portuguese Inibidores da Entrada do HIV
Spanish Inhibidores de Entrada del VIH
French Inhibiteurs d'entrée du VIH
German HIV-Eintrittsinhibitoren

Ontology: maraviroc (C1667052)

Definition (NCI) A C-C Chemokine Receptor Type 5 (CCR5) antagonist with activity against human immunodeficiency virus (HIV). Maraviroc inhibits HIV-1 entry via CCR5 coreceptor interaction.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C502411
SnomedCT 429603001, 427805000
English Maraviroc, Maraviroc (substance), Maraviroc (product), maraviroc, maraviroc (medication), maraviroc [Chemical/Ingredient], MARAVIROC, 4,4-difluoro-N-((1S)-3-(exo-3-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo(3.2.1)oct-8-yl)-1-phenylpropyl)cyclohexanecarboxamide
Spanish maraviroc, maraviroc (sustancia), maraviroc (producto)

Ontology: Selzentry (C1964465)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C502411
English Selzentry, Pfizer Brand of maraviroc

Ontology: CCR5 Receptor Antagonists (C3850102)

Definition (MSH) Compounds and drugs that inhibit or block the activity of CCR5 RECEPTORS.
Concepts Pharmacologic Substance (T121)
MSH D065100
English CCR5 Receptor Antagonists, Chemokine Co-receptor 5 Antagonists, CCR5 Receptor Blockers, Antagonists, CCR5 Receptor, CC Chemokine Receptor 5 Blockers, HIV-1 Fusion Coreceptor Antagonists, HIV 1 Fusion Coreceptor Antagonists, Receptor Blockers, CCR5, Chemokine Co receptor 5 Antagonists, Receptor Antagonists, CCR5, CC Chemokine Receptor 5 Antagonists, Blockers, CCR5 Receptor