Maraviroc

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Maraviroc
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Clinical data
Pronunciation/məˈrævɪrɒk/ Script error: No such module "Respell". Selzentry: /sɛlˈzɛntri/
Trade namesSelzentry, Celsentri
Other namesUK-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.comMonograph
MedlinePlusa607076
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Pregnancy
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  • AU: B1
Routes of
administration		By mouth
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Legal status
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Pharmacokinetic data
Bioavailability23%[4]
Protein binding~76%[2]
MetabolismLiver (CYP, predominantly CYP3A)[2]
MetabolitesSecondary amine formed by N-dealkylation (major)
Elimination half-life14–18 hours[2] (mean 16 hours)[5]
ExcretionFeces (76%), urine (20%)[2]
Identifiers
  • 4,4-Difluoro-N-{(1S)-3-[3-(3-isopropyl- 5-methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]oct-8-yl]-1-phenylpropyl}cyclohexanecarboxamide
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Chemical and physical data
FormulaC29H41F2N5O
Molar mass513.678 g·mol−1
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  • Cc5nnc(n5[C@@H]1C[C@H]4CC[C@@H](C1)N4CC[C@H](NC(=O)C2CCC(F)(F)CC2)c3ccccc3)C(C)C
  • InChI=1S/C29H41F2N5O/c1-19(2)27-34-33-20(3)36(27)25-17-23-9-10-24(18-25)35(23)16-13-26(21-7-5-4-6-8-21)32-28(37)22-11-14-29(30,31)15-12-22/h4-8,19,22-26H,9-18H2,1-3H3,(H,32,37)/t23-,24+,25-,26-/m0/s1 ☒N
  • Key:GSNHKUDZZFZSJB-QYOOZWMWSA-N ☒N
Data page
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Maraviroc, sold under the brand names Selzentry (US) and Celsentri (EU), is an antiretroviral medication used to treat HIV infection.[2][3] It is taken by mouth.[2][3] It is in the CCR5 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]

Medical uses

Maraviroc is indicated, in combination with other antiretroviral medications, for the treatment of only CCR5-tropic HIV-1 infection.[2][3]

Side effects

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 has black box warning for hepatotoxicity.[2] The MOTIVATE trials showed no clinically relevant differences in safety between the maraviroc and placebo groups.[7]

Mechanism of action

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.[8] 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.[9]

History

Maraviroc, originally designated UK-427857, was developed by the drug company Pfizer in its UK labs located in Sandwich. On 24 April 2007 the U.S. Food and Drug Administration advisory panel reviewing maraviroc's New 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-controlled clinical trials, compared 209 people receiving optimized therapy plus a placebo 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 a viral 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 the entry inhibitor had a mean increase in CD4+ 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]

Names

Maraviroc is the International nonproprietary name (INN).[14]

Research

Maraviroc appears to reduce graft-versus-host disease in people treated with allogeneic bone marrow transplantation for leukemia, 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 from stroke and traumatic 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 of neuroplasticity 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 in Cell in 2019.[17] As of 2025, randomized clinical trials were underway in Canada to evaluate its effectiveness in human stroke patients.[18]

References

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  1. ^ Page Module:Citation/CS1/styles.css has no content."Maraviroc Waymade (Waymade Australia Pty Limited)". Therapeutic Goods Administration (TGA). 14 January 2025. Retrieved 20 January 2025.
  2. ^ a b c d e f g h i j k Page Module:Citation/CS1/styles.css has no content."Selzentry- maraviroc tablet, film coated Selzentry- maraviroc solution". DailyMed. 18 July 2018. Retrieved 31 July 2020.
  3. ^ a b c d e f g Page Module:Citation/CS1/styles.css has no content."Celsentri EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 31 July 2020.
  4. ^ Page Module:Citation/CS1/styles.css has no content.Abel S, Russell D, Whitlock LA, Ridgway CE, Nedderman AN, Walker DK (April 2008). "Assessment of the absorption, metabolism and absolute bioavailability of maraviroc in healthy male subjects". British Journal of Clinical Pharmacology. 65 Suppl 1 (Suppl 1): 60–67. doi:10.1111/j.1365-2125.2008.03137.x. PMC 2311408. PMID 18333867.
  5. ^ Page Module:Citation/CS1/styles.css has no content.Abel S, Back DJ, Vourvahis M (2009). "Maraviroc: pharmacokinetics and drug interactions". Antiviral Therapy. 14 (5): 607–618. doi:10.1177/135965350901400514. PMID 19704163. S2CID 29064286.
  6. ^ Page Module:Citation/CS1/styles.css has no content."Maraviroc (HIV treatment) Dosage, Side Effects". AIDSinfo. Archived from the original on 20 February 2020. Retrieved 6 June 2019.
  7. ^ a b Page Module:Citation/CS1/styles.css has no content.Stephenson J (April 2007). "Researchers buoyed by novel HIV drugs: will expand drug arsenal against resistant virus". JAMA. 297 (14): 1535–1536. doi:10.1001/jama.297.14.1535. PMID 17426263.
  8. ^ Page Module:Citation/CS1/styles.css has no content.JA L (January 2009). "HIV pathogenesis: 25 years of progress and persistent challenges". AIDS. 23 (2): 147–160. doi:10.1097/QAD.0b013e3283217f9f. PMID 19098484. S2CID 10571856.
  9. ^ Page Module:Citation/CS1/styles.css has no content.Biswas P, Tambussi G, Lazzarin A (May 2007). "Access denied? The status of co-receptor inhibition to counter HIV entry". Expert Opinion on Pharmacotherapy. 8 (7): 923–933. doi:10.1517/14656566.8.7.923. PMID 17472538. S2CID 32675897.
  10. ^ Gay News From 365Gay.com
  11. ^ Page Module:Citation/CS1/styles.css has no content.Krauskopf L (6 August 2007). "Pfizer wins U.S. approval for new HIV drug". Reuters. Retrieved 6 August 2007.
  12. ^ Page Module:Citation/CS1/styles.css has no content.Emmelkamp JM, Rockstroh JK (October 2007). "CCR5 antagonists: comparison of efficacy, side effects, pharmacokinetics and interactions--review of the literature". European Journal of Medical Research. 12 (9): 409–417. PMID 17933722.
  13. ^ Page Module:Citation/CS1/styles.css has no content."Maraviroc reduces viral load in naive patients at 48 weeks". AIDS Patient Care and STDs. 21 (9): 703–704. September 2007. PMID 17941136.
  14. ^ Page Module:Citation/CS1/styles.css has no content.World Health Organization (2005). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 53". WHO Drug Information. 19 (1): 84–85. hdl:10665/73323. License: CC BY-NC-SA 3.0 IGO.
  15. ^ Page Module:Citation/CS1/styles.css has no content.Reshef R, Luger SM, Hexner EO, Loren AW, Frey NV, Nasta SD, et al. (July 2012). "Blockade of lymphocyte chemotaxis in visceral graft-versus-host disease". N. Engl. J. Med. 367 (2): 135–145. doi:10.1056/NEJMoa1201248. PMC 3568501. PMID 22784116.
  16. ^ Page Module:Citation/CS1/styles.css has no content."HIV Drug Reduces Graft-versus-Host Disease in Bone Marrow Transplant Patients, Penn Study Shows". Penn Medicine (Press release).
  17. ^ Page Module:Citation/CS1/styles.css has no content.Joy MT, Assayag EB, Shabashov-Stone D, Liraz-Zaltsman S, Mazzitelli J, Arenas M, et al. (21 February 2019). "CCR5 Is a Therapeutic Target for Recovery after Stroke and Traumatic Brain Injury". Cell. 176 (5): 1143–1157.e13. doi:10.1016/j.cell.2019.01.044. ISSN 0092-8674. PMC 7259116. PMID 30794775.
  18. ^ Page Module:Citation/CS1/styles.css has no content."Could a Pill Fix the Brain?". 4 September 2025. Retrieved 4 September 2025.

Further reading

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