Aplaviroc

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Aplaviroc
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Systematic (IUPAC) name
4-(4-{[(3R)-1-butyl-3-[(R)-cyclohexylhydroxymethyl]-2,5-dioxo- 1,4,9-triazaspiro[5.5]undecan-9-yl]methyl}phenoxy)benzoic acid
Identifiers
CAS Number 461023-63-2
ATC code none
PubChem CID 3001322
Chemical data
Formula C33H43N3O6
Molar mass 577.711 g/mol[[Script error: No such module "String".]]
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Aplaviroc (INN, codenamed AK602 and GSK-873140) was a CCR5 entry inhibitor developed for the treatment of HIV infection.[1][2] It is developed by GlaxoSmithKline

In October 2005, all studies of aplaviroc were discontinued due to liver toxicity concerns.[3][4] Some authors have claimed that evidence of poor efficacy may have contributed to termination of the drug's development;[5] the ASCENT study, one of the discontinued trials, showed aplaviroc to be inferior to efavirenz as the third component of a three-drug regimen.[6]

See also

References

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Further reading

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  1. http://www.retroconference.org/2004/cd/PDFs/540.pdf
  2. Potent Anti-R5 Human Immunodeficiency Virus Type 1 Effects of a CCR5 Antagonist, AK602/ONO4128/GW873140, in a Novel Human Peripheral Blood Mononuclear Cell Nonobese Diabetic-SCID, Interleukin-2 Receptor {gamma}-Chain-Knocked-Out AIDS Mouse Model - Nakata et al. 79 (4): 2087 - The Journal of Virology
  3. "Aplaviroc (GSK-873,140)". AIDSmeds.com. October 25, 2005. Retrieved 2008-09-05. 
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  5. Moyle, Graeme (December 19, 2006). "The Last Word on Aplaviroc: A CCR5 Antagonist With Poor Efficacy". The Body. Retrieved 2008-09-05. 
  6. Currier J, Lazzarin A, Sloan L; et al. (2008). "Antiviral activity and safety of aplaviroc with lamivudine/zidovudine in HIV-infected, therapy-naive patients: the ASCENT (CCR102881) study". Antivir Ther (Lond.). 13 (2): 297–306. PMID 18505181.