Aplaviroc (
INN
Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...
, codenamed AK602 and GSK-873140) is a
CCR5
C-C chemokine receptor type 5, also known as CCR5 or CD195, is a protein on the surface of white blood cells that is involved in the immune system as it acts as a receptor for chemokines.
In humans, the ''CCR5'' gene that encodes the CCR5 pro ...
entry inhibitor
Entry inhibitors, also known as fusion inhibitors, are a class of antiviral drugs that prevent a virus from entering a cell, for example, by blocking a receptor. Entry inhibitors are used to treat conditions such as HIV and hepatitis D.
HIV entr ...
that belongs to a class of
2,5-diketopiperazines developed for the treatment of
HIV
The human immunodeficiency viruses (HIV) are two species of ''Lentivirus'' (a subgroup of retrovirus) that infect humans. Over time, they cause acquired immunodeficiency syndrome (AIDS), a condition in which progressive failure of the immune ...
infection. It was developed by
GlaxoSmithKline
GSK plc, formerly GlaxoSmithKline plc, is a British multinational pharmaceutical and biotechnology company with global headquarters in London, England. Established in 2000 by a merger of Glaxo Wellcome and SmithKline Beecham. GSK is the ten ...
.
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
CCR5 receptor antagonists are a class of small molecules that antagonize the CCR5 receptor. The C-C motif chemokine receptor CCR5 is involved in the process by which HIV, the virus that causes AIDS, enters cells. Hence antagonists of this rec ...
References
Further reading
*
Abandoned drugs
Benzoic acids
Diketopiperazines
Entry inhibitors
Hepatotoxins
Spiro compounds
Diphenyl ethers
Butyl compounds
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