Chemistry:Aplaviroc
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Short description: Chemical compound
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| Routes of administration | Oral |
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| Formula | C33H43N3O6 |
| Molar mass | 577.722 g·mol−1 |
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Aplaviroc (INN, codenamed AK602 and GSK-873140) is a CCR5 entry inhibitor that belongs to a class of 2,5-diketopiperazines[1] developed for the treatment of HIV infection.[2][3] It was developed by GlaxoSmithKline.
In October 2005, all studies of aplaviroc were discontinued due to liver toxicity concerns.[4][5] Some authors have claimed that evidence of poor efficacy may have contributed to termination of the drug's development;[6] the ASCENT study, one of the discontinued trials, showed aplaviroc to be under-effective in many patients even at high concentrations.[7]
See also
- CCR5 receptor antagonist
References
- ↑ "2,5-Diketopiperazines: synthesis, reactions, medicinal chemistry, and bioactive natural products". Chemical Reviews 112 (7): 3641–3716. July 2012. doi:10.1021/cr200398y. PMID 22575049.
- ↑ "Determination of binding sites of a unique CCR5 inhibitor AK602 on human CCR5". 11th conference on retroviruses and opportunistic infections. San Francisco, CA. 2004. http://www.retroconference.org/2004/cd/PDFs/540.pdf.
- ↑ "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". Journal of Virology 79 (4): 2087–2096. February 2005. doi:10.1128/jvi.79.4.2087-2096.2005. PMID 15681411.
- ↑ "Aplaviroc (GSK-873,140)". AIDSmeds.com. October 25, 2005. http://www.aidsmeds.com/drugs/aplaviroc.htm.
- ↑ "Hepatotoxicity observed in clinical trials of aplaviroc (GW873140)". Antimicrobial Agents and Chemotherapy 52 (3): 858–865. March 2008. doi:10.1128/aac.00821-07. PMID 18070967.
- ↑ "The Last Word on Aplaviroc: A CCR5 Antagonist With Poor Efficacy". The Body. December 19, 2006. http://www.thebody.com/content/treat/art39205.html.
- ↑ "Antiviral activity and safety of aplaviroc with lamivudine/zidovudine in HIV-infected, therapy-naive patients: the ASCENT (CCR102881) study". Antiviral Therapy 13 (2): 297–306. 2008. doi:10.1177/135965350801300204. PMID 18505181.
Further reading
- "Serious doubts on safety and efficacy of CCR5 antagonists : CCR5 antagonists teeter on a knife-edge". Infection 34 (2): 110–113. April 2006. doi:10.1007/s15010-006-6206-1. PMID 16703305.
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