Aplaviroc

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 category	?
Legal status	?
Routes of administration	Oral
Identifiers
CAS Number	461023-63-2 Y
ATC code	none
PubChem	CID: 3001322
IUPHAR/BPS	805
ChemSpider	2272720 Y
UNII	98B425P30V Y
KEGG	D06557 Y
ChEMBL	CHEMBL1255794
Chemical data
Formula	C33H43N3O6
Molecular mass	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
InChI InChI=1S/C33H43N3O6/c1-2-3-19-36-30(38)28(29(37)24-7-5-4-6-8-24)34-32(41)33(36)17-20-35(21-18-33)22-23-9-13-26(14-10-23)42-27-15-11-25(12-16-27)31(39)40/h9-16,24,28-29,37H,2-8,17-22H2,1H3,(H,34,41)(H,39,40)/t28-,29-/m1/s1 Y Key:GWNOTCOIYUNTQP-FQLXRVMXSA-N Y
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Aplaviroc (INN, codenamed AK602 and GSK-873140) is a CCR5 entry inhibitor developed for the treatment of HIV infection. It was developed by GlaxoSmithKline.

In October 2005, all studies of aplaviroc were discontinued due to liver toxicity concerns. Some authors have claimed that evidence of poor efficacy may have contributed to termination of the drug's development; the ASCENT study, one of the discontinued trials, showed aplaviroc to be under-effective in many patients even at high concentrations.

See also

• CCR5 receptor antagonist