- Aplaviroc
Drugbox
IUPAC_name = 4-(4-{ [(3"R")-1-butyl-3- [("R")-cyclohexylhydroxymethyl] -2,5-dioxo- 1,4,9-triazaspiro [5.5] undecan-9-yl] methyl}phenoxy)benzoic acid
width = 300
CAS_number = 461023-63-2
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PubChem = 3001322
DrugBank =
C=33|H=43|N=3|O=6
molecular_weight = 577.711 g/mol
smiles = CCCCN1C(=O) [C@H] (NC(=O)C12CCN(CC2)CC3=CC=C(C=C3)OC4=CC=C(C=C4)C(=O)O) [C@@H] (C5CCCCC5)O
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routes_of_administration =Aplaviroc (INN, codenamed AK602 and GSK-873140) was a
CCR5 entry inhibitor developed for the treatment ofHIV infection. [http://www.retroconference.org/2004/cd/PDFs/540.pdf] [ [http://jvi.asm.org/cgi/content/abstract/79/4/2087 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 ] ]In October 2005, all studies of aplaviroc were discontinued due to liver toxicity concerns. [cite web |url=http://www.aidsmeds.com/drugs/aplaviroc.htm |title=Aplaviroc (GSK-873,140) |date=October 25, 2005 |publisher=AIDSmeds.com |accessdate=2008-09-05] [cite journal |author=Nichols WG, Steel HM, Bonny T, "et al" |title=Hepatotoxicity observed in clinical trials of aplaviroc (GW873140) |journal=Antimicrob Agents Chemother |volume=52 |issue=3 |pages=858–65 |year=2008 |month=March |pmid=18070967 |pmc=2258506 |doi=10.1128/AAC.00821-07 |url=] Some authors have claimed that evidence of poor efficacy may have contributed to termination of the drug's development; [cite web |url=http://www.thebody.com/content/treat/art39205.html |title=The Last Word on Aplaviroc: A CCR5 Antagonist With Poor Efficacy |date=December 19, 2006 |author=Moyle, Graeme |publisher=The Body |accessdate=2008-09-05] the ASCENT study, one of the discontinued trials, showed aplaviroc to be inferior to
efavirenz as the third component of a three-drug regimen. [cite journal |author=Currier J, Lazzarin A, Sloan L, "et al" |title=Antiviral activity and safety of aplaviroc with lamivudine/zidovudine in HIV-infected, therapy-naive patients: the ASCENT (CCR102881) study |journal=Antivir Ther (Lond.) |volume=13 |issue=2 |pages=297–306 |year=2008 |pmid=18505181 |doi= |url=]References
Further reading
*cite journal |author=Horster S, Goebel FD |title=Serious doubts on safety and efficacy of CCR5 antagonists : CCR5 antagonists teeter on a knife-edge |journal=Infection |volume=34 |issue=2 |pages=110–3 |year=2006 |month=April |pmid=16703305 |doi=10.1007/s15010-006-6206-1 |url=
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