Aplaviroc

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Aplaviroc
300px
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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Antiviral drugs: antiretroviral drugs used against HIV (primarily J05)
Entry/fusion inhibitors
(Discovery & development)
Reverse transcriptase
inhibitors (RTIs)
(1st gen) Efavirenz°# · Nevirapine#  · Loviride◊ · Delavirdine◊ ·
(2nd gen) diarylpyrimidines (Etravirine, Rilpivirine†)  · Lersivirine†
Integrase inhibitors
Raltegravir · Elvitegravir† · Globoidnan A (experimental)  · MK-2048†  · GSK-572†
Maturation inhibitors
Bevirimat† · Vivecon†
Protease Inhibitors (PI)
(Discovery and development)
Combined formulations
Experimental agents
TRIM5alpha (gene)
Other
Failed agents
°DHHS preferred first-line agent. ◊Formerly or rarely used agent.
  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. 
  4. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  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. 
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