Chemical structure of abacavir.
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Abacavir

Abacavir (ABC) is the most powerful nucleoside analog reverse transcriptase inhibitor (NARTI) used to treat HIV and AIDS. It has been well tolerated, its main side effect being hypersensitivity reactions, which can be dangerous. It is available under the trade name Ziagen™ by GlaxoSmithKline and the combination drug Trizivir™. more...

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Abacavir is one of the most deadly NARTIs, due its ability to trigger to hypersensitivity reactions that lead to sudden death in certain individuals. However, a genetic test is now available that, while not perfect, has reasonable accuracy in predicting whether an individual will be hypersensitive. Over 90% of patients can safely take abacavir.

Strains that are resistant to zidovudine (AZT) or lamivudine (3TC) are generally sensitive to abacavir, whereas strains that are resistant to AZT and 3TC are not as sensitive to abacavir.

History

Abacavir was approved by the Food and Drug Administration (FDA) on December 18, 1998 and is thus the fifteenth approved antiretroviral drug in the United States. Its patent will expire in the United States on 2009-12-26.

Mechanism of action

ABC is an analog of guanosine. It is capable of crossing the blood-brain barrier.

Abacavir is given orally and has a high bio-availability of 83%. It is metabolised primarily through alcohol dehydrogenase or gluconyl transferase.

Read more at Wikipedia.org


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Gene predicts dangerous drug reaction - HIV Digest - Brief Article
From Men's Fitness, 8/1/02

A genetic test can help predict whether a patient will have a perilous reaction to a widely prescribed AIDS medication.

Between 5 percent and 10 percent of patients who take abacavir (brand name Ziagen), a highly potent nucleoside reverse transcriptase inhibitor, suffer severe side effects approximately two to six weeks after starting on the drug.

Most people at risk for adverse reactions have the gene in question, designated as HLA-B5701. The discovery of this "genetic fingerprint," made by researchers at Royal Perth Hospital in Australia, will allow patients to be prescreened and the potential dangers to be markedly reduced.

"It's an astonishing connection between a genetic marker and the risk of a potentially fatal drug reaction," says Charles Flexner, M.D., associate professor of pharmacology and molecular biology at Johns Hopkins University School of Medicine.

Abacavir, manufactured by GlaxoSmithKline, is also sold as Trizivir, which combines it with the drugs AZT and 3TC.

The Australian study was published in the Lancet.

COPYRIGHT 2002 Weider Publications
COPYRIGHT 2002 Gale Group

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