Maraviroc

Class: HIV Entry and Fusion Inhibitors
VA Class: AM800
Chemical Name: 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
Molecular Formula: C₂₉H₄₁F₂N₅O
CAS Number: 376348-65-1
Brands: Selzentry

• 
  

  Hepatotoxicity reported;¹ may be preceded by signs of a systemic allergic reaction (e.g., pruritic rash, eosinophilia, elevated IgE antibody levels).¹ (See Hepatic Effects under Cautions.)

  
  


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  Immediately evaluate signs or symptoms of hepatitis or allergic reactions.¹

  
  

Introduction

Antiretroviral; HIV entry inhibitor and^{1 6 8 9} CC chemokine receptor 5 (CCR5) antagonist.^{1 6 8 9}

Uses for Maraviroc

Treatment of HIV Infection

Treatment of HIV-1 infection in adults infected with CCR5-tropic HIV-1.¹

Coreceptor tropism testing (assay detects CCR5- and CXCR4-using virus; results reported as CCR5-tropic, CXCR4-tropic, or dual/mixed tropic HIV-1) is required for appropriate use of maraviroc.¹ (See Laboratory Testing under Cautions.)

Consider the following when initiating therapy.¹ Only adults infected with CCR5-tropic HIV-1 should receive maraviroc.¹ Use a highly sensitive assay to identify appropriate patients; low levels of CXCR4-tropic or dual/mixed HIV-1 not detected at screening are associated with virologic failure.¹

Not recommended in patients with dual/mixed or CXCR4-tropic HIV-1 infection; viral response was minimal in such patients in phase 2 study.¹

Safety and efficacy not yet established in pediatric patients <16 years of age.¹

In clinical studies, more treatment-naive individuals receiving maraviroc experienced virologic failure and developed resistence to lamivudine than individuals receiving efavirenz.¹

Maraviroc Dosage and Administration

Administration

Oral Administration

Administer orally without regard to food.¹

Dosage

Dosage depends on whether maraviroc is administered concomitantly with drugs affecting hepatic metabolism or the P-glycoprotein transport system.^{1 9}

Must be given in combination with other antiretrovirals.¹

Pediatric Patients

Treatment of HIV Infection

Adolescents Receiving a CYP3A Inhibitor (with or without a CYP3A Inducer)

Oral

Adolescents ≥16 years of age receiving concomitant therapy with a CYP3A inhibitor (e.g., protease inhibitors [PIs] [except ritonavir-boosted tipranavir], delavirdine, ketoconazole, itraconazole, clarithromycin, other potent CYP3A inhibitors [nefazodone, telithromycin]): 150 mg twice daily.^{1 9}

Not necessary to alter dosage if therapy also includes a CYP3A inducer.^{1 9}

Adolescents Receiving Drugs that are not CYP3A Inhibitors or Inducers

Oral

Adolescents ≥16 years of age receiving concomitant therapy with ritonavir-boosted tipranavir, nevirapine, nucleoside and nucleotide reverse transcriptase inhibitors (NRTIs), enfuvirtide, raltegravir, or other drugs that are not potent CYP3A inhibitors or inducers: 300 mg twice daily.^{1 9}

Adolescents Receiving a CYP3A Inducer (without a Potent CYP3A Inhibitor)

Oral

Adolescents ≥16 years of age receiving concomitant therapy with a CYP3A inducer (e.g., efavirenz, etravirine, rifampin, carbamazepine, phenobarbital, phenytoin) and the regimen does not include a potent CYP3A inhibitor: 600 mg twice daily.^{1 9}

Adults

Treatment of HIV Infection

Adults Receiving a CYP3A Inhibitor (with or without a CYP3A Inducer)

Oral

Patients receiving concomitant therapy with a CYP3A inhibitor (e.g., PIs [except ritonavir-boosted tipranavir], delavirdine, ketoconazole, itraconazole, clarithromycin, other potent CYP3A inhibitors [nefazodone, telithromycin]): 150 mg twice daily.^{1 9}

Not necessary to alter dosage if therapy also includes a CYP3A inducer.^{1 9}

Adults Receiving Drugs that are not CYP3A Inhibitors or Inducers

Oral

Patients receiving concomitant therapy with ritonavir-boosted tipranavir, nevirapine, NRTIs, enfuvirtide, raltegravir, other drugs that are not potent CYP3A inhibitors or inducers: 300 mg twice daily.^{1 9}

Adults Receiving a CYP3A Inducer (without a Potent CYP3A Inhibitor)

Oral

Patients receiving concomitant therapy with a CYP3A inducer (e.g., efavirenz, etravirine, rifampin, carbamazepine, phenobarbital, phenytoin) and the regimen does not include a potent CYP3A inhibitor: 600 mg twice daily.^{1 9}

Special Populations

Hepatic Impairment

Dosage recommendations not available.⁹

Renal Impairment

Dosage recommendations not available.⁹

Cautions for Maraviroc

Contraindications

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  Manufacturer states none known.¹

  
  

Warnings/Precautions

Warnings

Hepatic Effects

Hepatotoxicity reported.¹ (See Boxed Warning.)

Adverse hepatic effects also reported.¹

Immediately evaluate signs and symptoms of hepatitis or elevated transaminase concentrations accompanied by rash or other systemic symptoms; consider discontinuance of maraviroc.¹

Sensitivity Reactions

Signs of a systemic allergic reaction may develop prior to an adverse hepatotoxic event.¹ (See Boxed Warning.)

Other Warnings and Precautions

Cardiovascular Effects

Cardiovascular events (i.e., myocardial ischemia and/or MI) reported.¹ Events generally occurred in individuals with cardiac disease or risk factors for cardiac disease.¹ Use with caution in patients at increased risk for cardiovascular events.¹

Symptomatic postural hypotension reported in healthy individuals receiving higher than recommended dosages of maraviroc.¹ Caution in patients with a history of postural hypotension and those receiving a drug that lowers BP.¹

Immune Reconstitution Syndrome

During initial treatment, patients who respond to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections (e.g., Mycobacterium avium complex [MAC], M. tuberculosis, cytomegalovirus [CMV], Pneumocystis jiroveci [formerly P. carinii], herpes simplex virus, varicella-zoster virus [VZV]); this may necessitate further evaluation and treatment.¹

Infectious Complications

Possible increased risk of infection with agents that bind to CCR5 receptors (e.g., maraviroc).^{1 11} Monitor for infection.¹

Malignancies

Possible increased risk of malignancy with agents that bind to CCR5 receptors (e.g., maraviroc).^{1 11} Risk not fully evaluated.¹

Laboratory Testing

Coreceptor tropism testing with a highly sensitive tropism assay is required for appropriate use of maraviroc.¹ In addition, consider this test in patients who exhibit virologic failure while receiving a CCR5 antagonist.⁹

Specific Populations

Pregnancy

Category B.¹

Antiretroviral Pregnancy Registry at 800-258-4263.¹

Some experts state that safety and pharmacokinetic data are insufficient to recommend maraviroc in pregnant women.¹³

Lactation

Distributed into milk in rats; not known whether distributed into human milk.¹

Instruct HIV-infected women not to breast-feed because of risk of HIV transmission and risk of adverse effects in the infant.¹

Pediatric Use

Safety and efficacy not established in pediatric patients <16 years of age.¹

Not recommended for use in pediatric patients <16 years of age.¹ Data insufficient to make recommendations for initial therapy in children.¹⁹

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether they respond differently than younger adults.¹

Use with caution and monitor because of age-related decreases in hepatic, renal, and/or concomitant disease and drug therapy.¹

Hepatic Impairment

Use caution; maraviroc concentrations increased in individuals with mild or moderate hepatic impairment.¹

Not evaluated in patients with severe hepatic impairment.¹

Monitor individuals with moderate hepatic impairment receiving maraviroc 150 mg twice daily and a drug that strongly inhibits CYP3A for maraviroc-associated adverse effects.¹

Insufficient data available to determine whether patients with coexisting hepatitis B virus (HBV) or hepatitis C virus (HCV) infection are at increased risk for adverse hepatic effects.¹

Renal Impairment

Use caution:^{1 9} safety and efficacy in patients with renal impairment not specifically evaluated.¹

Plasma maraviroc concentrations may be increased, especially in those receiving concomitant therapy with a CYP3A inhibitor.¹

Individuals with a Cl_cr <50 mL/minute receiving concomitant therapy with a CYP3A inhibitor may be at increased risk for adverse effects (e.g., dizziness, postural hypotension) due to increased plasma concentrations of maraviroc.¹ Use this combination in individuals with Cl_cr <50 mL/minute only if potential benefits outweigh risks; monitor for adverse effects.¹

Common Adverse Effects

Cough, pyrexia, upper respiratory tract infections, rash, dizziness.¹

Interactions for Maraviroc

Metabolized by CYP3A.¹

Does not inhibit CYP1A2, 2B6, 2C8, 2C9, 2C19, or 3A; may inhibit CYP2D6 at higher than recommended dosage.¹ Does not induce CYP1A2.¹

A p-glycoprotein substrate.¹

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Potential pharmacokinetic interactions with drugs that induce or inhibit CYP3A with possible altered metabolism of maraviroc.¹

Drugs Affecting or Affected by P-Glycoprotein Transport

Pharmacokinetic interactions likely with drugs that are p-glycoprotein inhibitors or inducers with possible altered metabolism of maraviroc.¹

Inhibits the P-glycoprotein transport system; may affect bioavailability of certain other drugs.¹

Specific Drugs

Drug	Interaction	Comments
Abacavir	No in vitro evidence of antagonistic antiretroviral effects 1	Recommended dosage of maraviroc is 300 mg twice daily when used in conjunction with NRTIs, provided the regimen does not include a CYP3A inhibitor or inducer1 16
Anticonvulsants (carbamazepine, phenobarbital, phenytoin)	Possible decreased maraviroc concentrations9	Carbamazepine, phenobarbital, phenytoin: Recommended dosage of maraviroc is 600 mg twice daily, provided the regimen does not include a potent CYP3A inhibitor;1 9 16 consider alternative anticonvulsants9
Antifungals, azoles (itraconazole, ketoconazole, voriconazole)	Itraconazole: Possible increased maraviroc concentrations 9 Ketoconazole: Increased maraviroc concentrations1 9 21 Voriconazole: Possible increased maraviroc concentrations 9	Itraconazole: Recommended dosage of maraviroc is 150 mg twice daily1 9 Ketoconazole: Recommended dosage of maraviroc is 150 mg twice daily1 9 Voriconazole: Consider using maraviroc 150 mg twice daily9
Antimycobacterials (rifabutin, rifampin, rifapentine)	Rifabutin: Possible decreased maraviroc concentrations9 Rifampin: Decreased maraviroc concentrations1 9 22	Rifabutin: Recommended dosage of maraviroc is 300 mg twice daily if regimen does not include a potent CYP3A inducer or inhibitor9 Rifabutin: Recommended dosage of maraviroc is 150 mg twice daily if regimen includes a potent CYP3A inhibitor9 Rifampin: Recommended dosage of maraviroc is 600 mg twice daily if regimen does not include a potent CYP3A inhibitor1 9 16 Rifampin: Recommended dosage of maraviroc is 300 mg twice daily if regimen includes a potent CYP3A inhibitor9 Rifapentine: Concomitant use not recommended 9
Atazanavir	Atazanavir or ritonavir-boosted atazanavir: Increased maraviroc concentrations1 9 No in vitro evidence of antagonistic antiretroviral effects1	Atazanavir or ritonavir-boosted atazanavir: Recommended dosage of maraviroc is 150 mg twice daily1 9
Clarithromycin	Possible increased maraviroc concentrations9	Recommended dosage of maraviroc is 150 mg twice daily1 9
Co-trimoxazole	Pharmacokinetic interaction unlikely; no change in the pharmacokinetics of maraviroc1
Darunavir	Ritonavir-boosted darunavir: Increased maraviroc concentrations1 9 No in vitro evidence of antagonistic antiretroviral effects1	Ritonavir-boosted darunavir: Recommended dosage of maraviroc is 150 mg twice daily1 9
Delavirdine	Possible increased maraviroc concentrations 9 No in vitro evidence of antagonistic antiretroviral effects1	Recommended dosage of maraviroc is 150 mg twice daily1 9
Didanosine	No in vitro evidence of antagonistic antiretroviral effects1	Recommended dosage of maraviroc is 300 mg twice daily when used in conjunction with NRTIs, provided the regimen does not include a CYP3A inhibitor or inducer1 16
Efavirenz	Efavirenz: Decreased maraviroc concentrations1 9 22 Efavirenz and lopinavir/ritonavir: Increased maraviroc concentrations1 9 16 Efavirenz and ritonavir-boosted saquinavir: Increased maraviroc concentrations1 9 Efavirenz: No in vitro evidence of antagonistic antiretroviral effects1	Efavirenz: Recommended dosage of maraviroc is 600 mg twice daily, provided the regimen does not include a potent CYP3A inhibitor1 9 Regimens that include efavirenz and lopinavir/ritonavir: Recommended dosage of maraviroc is 150 mg twice daily9 Regimens that include efavirenz and ritonavir-boosted saquinavir: Recommended dosage of maraviroc is 150 mg twice daily9
Emtricitabine	No in vitro evidence of antagonistic antiretroviral effects 1	Recommended dosage of maraviroc is 300 mg twice daily when used in conjunction with NRTIs, provided the regimen does not include a CYP3A inhibitor or inducer1 16
Enfuvirtide	In vitro evidence of additive to synergistic antiretroviral effects1	Recommended dosage of maraviroc is 300 mg twice daily, provided the regimen does not include a CYP3A inhibitor or inducer1
Estrogens or Progestins	Oral contraceptives: Pharmacokinetic interaction unlikely;1 9 no change in the pharmacokinetics of ethinyl estradiol and levonorgestrel1	Considered safe to use maraviroc with oral contraceptive preparations9
Etravirine	Etravirine: Decreased maraviroc concentrations9 Etravirine and ritonavir-boosted darunavir: Increased maraviroc concentrations9	Etravirine: Recommended dosage of maraviroc is 600 mg twice daily9 Regimens that include etravirine and ritonavir-boosted darunavir: Recommended dosage of maraviroc is 150 mg twice daily9
Fosamprenavir	Fosamprenavir: Possible increased maraviroc concentrations1 9 No in vitro evidence of antagonistic antiretroviral effects between amprenavir and maraviroc1	Fosamprenavir: Recommended dosage of maraviroc is 150 mg twice daily1 9
Indinavir	Possible increased maraviroc concentrations9 No in vitro evidence of antagonistic antiretroviral effects1	Recommended dosage of maraviroc is 150 mg twice daily1 9
Lamivudine	Pharmacokinetic interaction unlikely1 No in vitro evidence of antagonistic antiretroviral effects1	Recommended dosage of maraviroc is 300 mg twice daily when used in conjunction with NRTIs, provided the regimen does not include a CYP3A inhibitor or inducer1 16
Lopinavir	Lopinavir/ritonavir: Substantially increased maraviroc concentrations1 9 21 Lopinavir/ritonavir and efavirenz: Increased maraviroc concentrations1 9 No in vitro evidence of antagonistic antiretroviral effects 1	Lopinavir/ritonavir: Recommended dosage of maraviroc is 150 mg twice daily1 9 Regimens that include lopinavir/ritonavir and efavirenz: Recommended dosage of maraviroc is 150 mg twice daily1 9
Midazolam	No change in the pharmacokinetics of midazolam1
Nefazodone	Possible pharmacokinetic interaction 1	Recommended dosage of maraviroc is 150 mg twice daily1
Nelfinavir	No in vitro evidence of antagonistic antiretroviral effects 1	Recommended dosage of maraviroc is 150 mg twice daily1
Nevirapine	No change in maraviroc concentrations1 9 No in vitro evidence of antagonistic antiretroviral effects1	Recommended dosage of maraviroc is 300 mg twice daily if the regimen does not include a PI or other potent CYP3A inhibitor;9 recommended dosage of maraviroc is 150 mg twice daily if the regimen includes a PI (except ritonavir-boosted tipranavir)9
Raltegravir	Decreased concentrations of raltegravir1	Not considered clinically important1
Ritonavir	Low-dose ritonavir (ritonavir 100 mg twice daily): Increased maraviroc concentrations 1 9 21 No in vitro evidence of antagonistic antiretroviral effects1	Regimens that include low-dose ritonavir (except ritonavir-boosted tipranavir): Recommended dosage of maraviroc is 150 mg twice daily 1 9
Saquinavir	Ritonavir-boosted saquinavir (saquinavir 1 g twice daily with ritonavir 100 mg twice daily): Substantially increased maraviroc concentrations9 21 Ritonavir-boosted saquinavir and efavirenz: Increased maraviroc concentrations1 9 Saquinavir: No in vitro evidence of antagonistic antiretroviral effects 1	Ritonavir-boosted saquinavir: Recommended dosage of maraviroc is 150 mg twice daily 1 9 Regimens that include ritonavir-boosted saquinavir and efavirenz: Recommended dosage of maraviroc is 150 mg twice daily 9
Stavudine	No in vitro evidence of antagonistic antiretroviral effects1	Recommended dosage of maraviroc is 300 mg twice daily when used in conjunction with NRTIs, provided the regimen does not include a CYP3A inhibitor or inducer1 16
St. John’s wort (Hypericum perforatum)	Potential decreased maraviroc concentrations and loss of virologic response1	Concomitant use not recommended1 9
Telithromycin	Possible pharmacokinetic interaction 1	Recommended dosage of maraviroc is 150 mg twice daily1
Tenofovir	No change in maraviroc concentrations1 No in vitro evidence of antagonistic antiretroviral effects 1	Recommended dosage of maraviroc is 300 mg twice daily when used in conjunction with NRTIs, provided the regimen does not include a CYP3A inhibitor or inducer1 16
Tipranavir	Ritonavir-boosted tipranavir: Pharmacokinetic interaction unlikely 9 No in vitro evidence of antagonistic antiretroviral effects1	Ritonavir-boosted tipranavir: Recommended dosage of maraviroc is 300 mg twice daily, provided the regimen does not include a CYP3A inhibitor or inducer1 9 16
Zidovudine	Pharmacokinetic interaction unlikely1 No in vitro evidence of antagonistic antiretroviral effects 1	Recommended dosage of maraviroc is 300 mg twice daily when used in conjunction with NRTIs, provided the regimen does not include a CYP3A inhibitor or inducer1 16

Maraviroc Pharmacokinetics

Absorption

Bioavailability

Absolute bioavailability of a 100-mg oral dose is 23%; absolute bioavailability of a 300-mg dose predicted to be 33%.^{1 20}

Following oral administration, peak plasma concentrations attained in 0.5–4 hours.¹

Food

When a 300-mg tablet was administered with a high fat meal, AUC was decreased by 33%.¹

Special Populations

Increased plasma concentrations expected in patients with renal impairment, especially in those receiving concomitant therapy with a CYP3A inhibitor.¹

Increased plasma concentrations reported in individuals with mild or moderate hepatic impairment, especially in those with moderate hepatic impairment receiving concomitant therapy with a potent CYP3A inhibitor.¹

Distribution

Extent

Distributed into milk in rats; not known whether distributed into human milk.¹

Plasma Protein Binding

76%.¹

Elimination

Metabolism

Principally metabolized by CYP3A to inactive metabolites.¹

Elimination Route

Approximately 20% eliminated in urine (8% as unchanged maraviroc) and 76% excreted in feces (25% as unchanged maraviroc).¹

Half-life

14–18 hours.^{1 20}

Special Populations

Pharmacokinetics not studied in patients with severe hepatic impairment.¹

Stability

Storage

Oral

Tablets

25°C (may be exposed to 15–30°C).¹

ActionsActions

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  Active against HIV-1;¹ antiviral activity against HIV-2 not evaluated.¹

  
  


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  CCR5 antagonist;^{1 6 8 9} CCR5 is a co-receptor for the most commonly transmitted HIV-1 strains that predominate during the early stages of infection^{6 9} and remains the dominant form in many patients with late-stage infection.⁶

  
  


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  Selectively binds to CCR5 on the cell membrane and prevents the interaction of HIV-1 glycoprotein 120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells.^{1 6}

  
  


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  Does not inhibit CXCR4-tropic and dual/mixed-tropic HIV-1 entry into cells.¹

  
  


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  Active against some strains of HIV-1 resistant to NRTIs, nonnucleoside reverse transcriptase inhibitors (NNRTIs), PIs, and HIV entry and fusion inhibitors (enfuvirtide).¹

  
  

Advice to Patients

• 
  

  Critical nature of compliance with HIV therapy.¹ Used in conjunction with other antiretrovirals; do not use for monotherapy.¹

  
  


• 
  

  Antiretroviral therapy is not a cure for HIV infection, and opportunistic infections still may occur.¹ HIV transmission via sexual contact or sharing needles is not prevented by antiretrovirals.¹

  
  


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  Importance of reading patient information provided by the manufacturer.¹

  
  


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  If a dose is missed, administer as soon as possible and resume the regular schedule.¹ If there are <6 hours before the next scheduled dose when the missed dose is remembered, omit the dose and take the next dose at the scheduled time.¹

  
  


• 
  

  Advise patients that hepatitis and allergic reactions have occurred.¹ Importance of discontinuing maraviroc and seeking medical attention if signs or symptoms of these adverse events (e.g., rash, yellow skin or eyes, dark urine, vomiting, abdominal pain) occur.¹

  
  


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  Possibility of dizziness.¹ Advise patients to avoid driving a motor vehicle or operating hazardous machinery if they experience dizziness.¹

  
  


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  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and herbal products (e.g., St. John’s wort), and any concomitant illnesses.¹

  
  


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  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹

  
  


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  Importance of advising patients of other important precautionary information.¹ (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Maraviroc

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets, film-coated	150 mg	Selzentry	Pfizer
		300 mg	Selzentry	Pfizer

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions April 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Pfizer. Selzentry (maraviroc) tablets prescribing information. New York, NY; 2009 Nov.

2. Nelson M, Fätkenheuer G, Konourina I et al. Efficacy and safety of maraviroc plus optimized background therapy in viremic, ART-experienced patients infected with CCR5-tropic HIV-1 in Europe, Australia, and North America: 24-week results. 14th Conference on Retroviruses and Opportunistic Infections, Los Angeles, CA. 2007 Feb 25-28. Abstract 104aLB. From website.

3. Lalezari J, Goodrich J, DeJesus E et al. Efficacy and safety of maraviroc plus optimized background therapy in viremic ART-experienced patients infected with CCR5-tropic HIV-1: 24-week results of a phase 2b/3 study in the United States and Canada. 14th Conference on Retroviruses and Opportunistic Infections, Los Angeles, CA. 2007 Feb 25-28. Abstract 104bLB. From website.

4. Mayer H, van der Ryst E, Saag M et al. Safety and efficacy of maraviroc (MVC), a novel CCR5 antagonist, when used in combination with optimized background therapy (OBT) for the treatment of antiretroviral-experienced subjects infected with dual/mixed-tropic HIV-1: 24-week results of a phase 2b exploratory trial. XVI International AIDS Conference, Toronto, Canada. 2006 Aug 13-18. Abstract. From website.

5. Daar ES, Kesler KL, Petropoulos J et al. Baseline HIV type 1 coreceptor tropism predicts disease progression. Clin Infect Dis. 2007; 45:643-9. [PubMed 17683002]

6. Dorr P, Westby M, Dobbs S et al. Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity. Antimicrob Agents Chemother. 2005; 49:4721-32. [PubMed 16251317]

7. Stephenson J. Researchers buoyed by novel HIV drugs: will expand drug arsenal against resistant virus. JAMA. 2007; 297:1535-6. [PubMed 17426263]

8. Lederman MM, Penn-Nicholson A, Cho M et al. Biology of CCR5 and its role in HIV infection and treatment. JAMA. 2006; 296:815-26. [PubMed 16905787]

9. Panel on Antiretroviral Guidelines for Adults and Adolescents of the Department of Health and Human Services (DHHS). Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents (November 3, 2008). From the US Department of Health and Human Services HIV/AIDS Information Services (AIDSinfo) website.

10. Hammer SM, Saag MS, Schechter M et al. Treatment of adult HIV infection: 2006 recommendations of the International AIDS Society–USA panel. JAMA. 2006; 296:827-43. [PubMed 16905788]

11. Anon. Two new drugs for HIV infection. Med Lett Drugs Ther. 2008; 50:2-4.

12. Fätkenheuer G, Konourina I, Nelson M et al. Efficacy and safety of maraviroc (MCV) plus optimized background therapy (OBT) in viraemic, antiretroviral treatment-experienced patients infected with CCR5-tropic (R5) HIV-1 in Europe, Australia, and North America (MOTIVATE 2): 48-week results. 11th European AIDS Conference, Madrid, Spain. 2007 Oct 24-27. Abstract PS3/5.

13. Perinatal HIV Guidelines Working Group. Public Health Service task force recommendations for use of antiretroviral drugs in pregnant HIV-1-infected women for maternal health and interventions to reduce perinatal HIV-1 transmission in the United States (April 29, 2009). From the US Department of Health and Human Services HIV/AIDS Information Services (AIDSinfo) website.

14. Hitt E. Maraviroc misses noninferiority endpoint compared with efavirenz in antiretroviral-naive patients. Medscape Medical News. From website. Accessed 29 Jan 2008.

15. Saag M, I’ve P, Heera J et al. A multicenter, randomized, double-blind, comparative trial of a novel CCR5 antagonist, maraviroc versus efavirenz, both in combination with Combivir (zidovudine [ZDV]/lamivudine [3TC]) for the treatment of antiretroviral naive patients infected with R5 HIV1: week 48 results of the MERIT study. 4th IAS Conference, Sydney, Australia. 2007 Jul 22-25. Abstract.

16. Pfizer, New York, NY: Personal communication.

17. Gulick RM, Lalezari J, Goodwich J et al. Maraviroc for previously treated patients with R5 HIV-1 infection. N Engl J Med. 2008; 359:1429-41. [PubMed 18832244]

18. Heera J, Ive P, Botes M et al. The MERIT study of maraviroc in antiretroviral-naive patients with R5 HIV-1: 96-week results. 5th IAS Conference, Cape Town, South Africa. 2009 Jul 19-22.Abstract.

19. Working Group on Antiretroviral Therapy and Medical Management of HIV-infected Children of the National Pediatric and Family HIV Resource Center (NPHRC), Health Resources and Services Administration (HRSA), and National Institutes of Health (NIH). Guidelines for the use of antiretroviral agents in pediatric HIV infection (February 23, 2009). From the US Department of Health and Human Services HIV/AIDS Information Services (AIDSinfo) website.

20. Abel S, Russell D, Whitlock LA et al. Assessment of the absorption, metabolism and absolute bioavailability of maraviroc in healthy male subjects. Br J Clin Pharmacol. 2008; 65(Suppl 1):60-7. [PubMed 18333867]

21. Abel S, Russell D, Taylor-Worth RJ et al. Effects of CYP3A4 inhibitors on the pharmacokinetics of maraviroc in healthy volunteers. Br J Clin Pharmacol. 2008; 65(Suppl 1):27-37. [PubMed 18333863]

22. Abel S, Jenkins TM, Whitlock LA et al. Effects of CYP3A4 inducers with and without CYP3A4 inhibitors on the pharmacokinetics of maraviroc in healthy volunteers. Br J Clin Pharmacol. 2008; 65(Suppl 1):38-46. [PubMed 18333864]

More Maraviroc resources

• Maraviroc Side Effects (in more detail)
• Maraviroc Dosage
• Maraviroc Use in Pregnancy & Breastfeeding
• Maraviroc Drug Interactions
• Maraviroc Support Group
• 1 Review for Maraviroc - Add your own review/rating

• Maraviroc MedFacts Consumer Leaflet (Wolters Kluwer)


• Maraviroc Professional Patient Advice (Wolters Kluwer)


• maraviroc Advanced Consumer (Micromedex) - Includes Dosage Information


• Selzentry Prescribing Information (FDA)


• Selzentry Consumer Overview

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