Maraviroc
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| Pronunciation | mə-RAV-i-rok |
| Trade names | Selzentry, Celsentri |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a607076 |
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By mouth (tablets, oral solution) |
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| Pharmacokinetic data | |
| Bioavailability | 23% |
| Protein binding | ~76% |
| Metabolism | Liver (, predominantly CYP3A) |
| Metabolites | Secondary amine formed by N-dealkylation (major) |
| Biological half-life | 14–18 hours (mean 16 hours) |
| Excretion | Feces (76%), urine (20%) |
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| Synonyms | 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 |
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| ECHA InfoCard | 100.124.927 |
| Chemical and physical data | |
| Formula | C29H41F2N5O |
| Molar mass | 513.666 g/mol |
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Maraviroc (INN, brand-named Selzentry sel-ZEN-tree, or Celsentri outside the U.S.) is an antiretroviral drug in the CCR5 receptor antagonist class used in the treatment of HIV infection. It is also classed as an entry inhibitor. It also appeared to reduce graft-versus-host disease in patients treated with allogeneic bone marrow transplantation for leukemia, in a phase 1/2 study.
Maraviroc is an entry inhibitor. Specifically, maraviroc is a negative allosteric modulator of the CCR5 receptor, which is found on the surface of certain human cells. The chemokine receptor CCR5 is an essential co-receptor for most HIV strains and necessary for the entry process of the virus into the host cell. The drug binds to CCR5, thereby blocking the HIV protein gp120 from associating with the receptor. HIV is then unable to enter human macrophages and T cells. Because HIV can also use other coreceptors, such as CXCR4, an HIV tropism test such as a trofile assay must be performed to determine if the drug will be effective.
Maraviroc, originally designated UK-427857, was developed by the drug company Pfizer in its UK labs located in Sandwich. On April 24, 2007 the U.S. Food and Drug Administration advisory panel reviewing maraviroc's New Drug Application unanimously recommended approval for the new drug, and the drug received full FDA approval on August 6, 2007 for use in treatment experienced patients.
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