Maraviroc
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Maraviroc
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| Systematic (IUPAC) name | |
| 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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| Identifiers | |
| CAS number | |
| ATC code | J05 |
| PubChem | |
| Chemical data | |
| Formula | C29H41F2N5O |
| Mol. mass | 513.666 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Licence data |
, |
| Pregnancy cat. |
B(US) |
| Legal status | |
| Routes | Oral |
Maraviroc (brand-named Selzentry, or Celsentri outside the U.S.) is a drug used in the treatment of HIV infection.
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Maraviroc is an entry inhibitor. Specifically, maraviroc blocks the chemokine receptor CCR5 which HIV uses as a coreceptor to bind and enter a human helper T cell. Because HIV can also use another coreceptor, CXCR4, an HIV tropism test such as a trofile assay must be performed to determine if the drug will be effective.[1]
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,[2] and the drug received full FDA approval on August 6, 2007 for use in treatment experienced patients.[3]
On September 24, 2007, Pfizer announced that the European Commission approved Maraviroc. Industry experts forecast annual Maraviroc sales of $500 million by 2011.[4]
Two randomized, placebo-controlled clinical trials, known as MOTIVATE 1 & 2, compared 209 patients receiving optimized therapy plus a placebo to 426 patients 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.[5][6][7]
The MOTIVATE trials showed no clinically relevant differences in safety between the maraviroc and placebo groups. However, researchers question the long-term safety of blocking CCR5, a receptor whose function in the healthy individual is not fully understood.[5]
- ^ Biswas P, Tambussi G, Lazzarin A (2007). "Access denied? The status of co-receptor inhibition to counter HIV entry". Expert Opin Pharmacother 8 (7): 923–33. doi:. PMID 17472538. http://www.expertopin.com/doi/abs/10.1517/14656566.8.7.923.
- ^ Gay News From 365Gay.com
- ^ "Pfizer wins U.S. approval for new HIV drug". Retrieved on 2007-08-06.
- ^ Reuters, Europe gives final approval to Pfizer HIV drug
- ^ a b Stephenson J (2007). "Researchers buoyed by novel HIV drugs: will expand drug arsenal against resistant virus". JAMA 297 (14): 1535–6. doi:. PMID 17426263. http://jama.ama-assn.org/cgi/pmidlookup?view=long&pmid=17426263.
- ^ Emmelkamp JM, Rockstroh JK (2007). "CCR5 antagonists: comparison of efficacy, side effects, pharmacokinetics and interactions--review of the literature". Eur. J. Med. Res. 12 (9): 409–17. PMID 17933722.
- ^ "Maraviroc reduces viral load in naive patients at 48 weeks". AIDS Patient Care STDS 21 (9): 703–4. 2007. PMID 17941136.
- BBC News story: Drug 'stops HIV's entry to cells'
- Maraviroc data at aidsmap
- Maraviroc early access program
- New HIV Drug Recommended for Approval
- MeSH maraviroc
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