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 | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | ? |
| Identifiers | |
| CAS number | 461023-63-2  |
| ATC code | None |
| PubChem | CID 3001322 |
| ChemSpider | 2272720 |
| UNII | 98B425P30V |
| KEGG | D06557 |
| Chemical data | |
| Formula | C33H43N3O6 |
| Mol. mass | 577.711 g/mol |
| SMILES | eMolecules & PubChem |
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Aplaviroc (INN, codenamed AK602 and GSK-873140) is 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 under-effective in many patients even at high concentrations.[6]
[edit] See also
[edit] References
- ^ 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 - Nakata et al. 79 (4): 2087 - The Journal of Virology
- ^ "Aplaviroc (GSK-873,140)". AIDSmeds.com. October 25, 2005. http://www.aidsmeds.com/drugs/aplaviroc.htm. Retrieved 2008-09-05.[dead link]
- ^ Nichols WG, Steel HM, Bonny T et al (March 2008). "Hepatotoxicity Observed in Clinical Trials of Aplaviroc (GW873140)". Antimicrob Agents Chemother 52 (3): 858–65. doi:10.1128/AAC.00821-07. PMC 2258506. PMID 18070967. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2258506.
- ^ Moyle, Graeme (December 19, 2006). "The Last Word on Aplaviroc: A CCR5 Antagonist With Poor Efficacy". The Body. http://www.thebody.com/content/treat/art39205.html. Retrieved 2008-09-05.
- ^ 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. http://www.intmedpress.com/serveFile.cfm?sUID=176d0ac2-96c4-4498-97dc-f19874756f4e.
[edit] Further reading
- Horster S, Goebel FD (April 2006). "Serious doubts on safety and efficacy of CCR5 antagonists : CCR5 antagonists teeter on a knife-edge". Infection 34 (2): 110–3. doi:10.1007/s15010-006-6206-1. PMID 16703305.
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