Maraviroc
From Wikipedia, the free encyclopedia
 |
|
|
Maraviroc
|
|
| 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 |
|
| 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.
Contents |
[edit] Mechanism of action
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]
[edit] Development and approval
Maraviroc, originally designated UK-427857, was developed by the drug company Pfizer in its UK labs located in Sandwich,_Kent. 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]
[edit] Efficacy
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]
[edit] Safety
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]
[edit] References
- ^ 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.
- ^ 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.
- ^ 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" (2007). AIDS Patient Care STDS 21 (9): 703–4. PMID 17941136.
[edit] External links
- 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
|
|||||||||||||||||||||||||||||
 |
This antimicrobial-related article is a stub. You can help Wikipedia by expanding it. |
