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| Pronunciation | /məˈrævɪrɒk/mə-RAV-i-rok Selzentry:/sɛlˈzɛntri/ |
| Trade names | Selzentry, Celsentri |
| Other names | UK-427857, 4,4-Difluoro-N-[(1S)-3-{(1R,3s,5S)-3-[3-methyl-5-(propan-2-yl)-4H-1,2,4-triazol-4-yl]-8-azabicyclo[3.2.1]octan-8-yl}-1-phenylpropyl] cyclohexanecarboxamide |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a607076 |
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| Routes of administration | By mouth |
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| Bioavailability | 23%[4] |
| Protein binding | ~76%[2] |
| Metabolism | Liver (CYP, predominantlyCYP3A)[2] |
| Metabolites | Secondary amine formed byN-dealkylation (major) |
| Eliminationhalf-life | 14–18 hours[2] (mean 16 hours)[5] |
| Excretion | Feces (76%),urine (20%)[2] |
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| ECHA InfoCard | 100.124.927 |
| Chemical and physical data | |
| Formula | C29H41F2N5O |
| Molar mass | 513.678 g·mol−1 |
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Maraviroc, sold under the brand namesSelzentry (US) andCelsentri (EU), is anantiretroviral medication used to treatHIV infection.[2][3] It is takenby mouth.[2][3] It is in theCCR5 receptor antagonist class.[2][3]
It was approved for medical use in the United States in August 2007,[2] and in the European Union in September 2007.[3]
Maraviroc isindicated, in combination with other antiretroviral medications, for the treatment of only CCR5-tropic HIV-1 infection.[2][3]
Maraviroc can cause serious, life-threatening side effects. These include liver problems, skin reactions, and allergic reactions. An allergic reaction may happen before liver problems occur.[6] Official labeling of Selzentry hasblack box warning forhepatotoxicity.[2] The MOTIVATE trials showed no clinically relevant differences in safety between the maraviroc and placebo groups.[7]
Maraviroc is anentry inhibitor. Specifically, maraviroc is a negativeallosteric modulator of theCCR5 receptor, which is found on the surface of certain human cells. Thechemokine receptor CCR5 is an essential co-receptor for most HIV strains and necessary for theentry process of the virus into the host cell. The drug binds to CCR5, thereby blocking the HIV proteingp120 from associating with the receptor.HIV is then unable to enter humanmacrophages andT cells.[8] Because HIV can also use other coreceptors, such asCXCR4, anHIV tropism test such as atrofile assay must be performed to determine if the drug will be effective.[9]
Maraviroc, originally designated UK-427857, was developed by the drug companyPfizer in its UK labs located inSandwich. On 24 April 2007 the U.S.Food and Drug Administration advisory panel reviewing maraviroc'sNew Drug Application unanimously recommended approval for the new drug,[10] and the drug received full FDA approval on 6 August 2007 for use in treatment experienced patients.[11]
Two randomized, placebo-controlledclinical trials, compared 209 people receiving optimized therapy plus aplacebo to 426 people receiving optimized therapy plus 150 mg maraviroc once daily and 414 patients receiving optimized therapy plus 150 mg maraviroc twice daily. At 48 weeks, 55% of participants receiving maraviroc once daily and 60% of participants receiving the drug twice daily achieved aviral load of less than 400 copies/mL compared with 26% of those taking placebo; about 44% of the once-daily and 45% of the twice-daily maraviroc group had a viral load of less than 50 copies/mL compared with about 23% of those who received placebo. In addition, those who received theentry inhibitor had a mean increase inCD4+ cells of 110 cells/μL in the once-daily group, 106 cells/μL in the twice-daily group, and 56 cells/μL in the placebo group.[7][12][13] Maraviroc was approved for medical use in the European Union in September 2007.[3]
Maraviroc is theInternational nonproprietary name (INN).[14]
Maraviroc appears to reducegraft-versus-host disease in people treated withallogeneic bone marrow transplantation forleukemia, in a Phase I/II study.[15][16]
In addition to its established role in HIV treatment, maraviroc has been investigated for potential use in recovery fromstroke andtraumatic brain injury. Research led by neuroscientists at the University of California, Los Angeles, and collaborators in Israel and Canada identified the CCR5 receptor as a regulator ofneuroplasticity after brain injury. Animal studies and genetic analyses suggested that blocking CCR5 can extend the brain’s natural recovery window and improve outcomes. Since maraviroc is a CCR5 antagonist already approved for HIV therapy, it was repurposed for this purpose, with preclinical findings published inCell in 2019.[17] As of 2025, randomized clinical trials were underway in Canada to evaluate its effectiveness in human stroke patients.[18]
