Maraviroc

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Maraviroc
Structural formula of maraviroc
Ball-and-stick model of the maraviroc molecule
Clinical data
Pronunciation/məˈrævɪrɒk/ mə-RAV-i-rok 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
License data
Pregnancy
category
  • AU: B1
Routes of
administration		By mouth
ATC code
Legal status
Legal status
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
JSmol)
  • 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
 ☒NcheckY (what is this?)  (verify)

Maraviroc, sold under the brand names Selzentry (US) and Celsentri (EU), is an

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

trofile assay must be performed to determine if the drug will be effective.[9]
可以治疗长新冠！

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]

References

  1. FDA
    . Retrieved 22 October 2023.
  2. ^ a b c d e f g h i j k "Selzentry- maraviroc tablet, film coated Selzentry- maraviroc solution". DailyMed. 18 July 2018. Retrieved 31 July 2020.
  3. ^ a b c d e f g "Celsentri EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 31 July 2020.
  4. PMID 18333867
    .
  5. S2CID 29064286
    .
  6. ^ "Maraviroc (HIV treatment) Dosage, Side Effects". AIDSinfo.
  7. ^
    PMID 17426263
    .
  8. S2CID 10571856
    .
  9. S2CID 32675897
    .
  10. ^ Gay News From 365Gay.com
  11. ^ Krauskopf, Lewis (6 August 2007). "Pfizer wins U.S. approval for new HIV drug". Reuters. Retrieved 6 August 2007.
  12. PMID 17933722
    .
  13. PMID 17941136
    .
  14. hdl:10665/73323
    . License: CC BY-NC-SA 3.0 IGO.
  15. PMID 22784116
    .
  16. ^ "HIV Drug Reduces Graft-versus-Host Disease in Bone Marrow Transplant Patients, Penn Study Shows". Penn Medicine (Press release).

Further reading

External links
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