Chemical structure of stavudine.
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Zerit

Stavudine (2'-3'-didehydro-2'-3'-dideoxythymidine, d4T, brand name ZeritĀ®) is a nucleoside analog reverse transcriptase inhibitor (NARTI) active against HIV. more...

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History

Stavudine was approved by the Food and Drug Administration (FDA) in Jun 24, 1994 for adults and in Sep 6, 1996 for pediatric use and again as an extended-release version for once-a-day dosing in 2001. The fourth antiretroviral drug on the market, its patent will expire in the United States on 2008-06-25.

Mechanism of ation

Stavudine is an analog of thymidine. It is phosphorylated by cellular kinases into active triphosphate. Stavudine triphosphate inhibits the reverse transcriptase by competing with natural substrate, thymidine triphosphate. It also causes termination of DNA synthesis by incorporating into it.

The oral absorption rate of stavudine is over 80 %. Approximately half of stavudine is actively secreted unchanged into the urine and the other half is eliminated through endogenic pathways. Simultaneous use of AZT is not recommended, for AZT can inhibit the intracellular phosphorylation of stavudine. Other anti-HIV drugs do not possess this property. The main severe side effect is peripheral neuropathy, which can be corrected by reducing dosage. Stavudine has been shown in laboratory test to be genotoxic, but with clinical doses its carcinogenic effects are non-existent.

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Fourth AIDS drug approved - Bristol-Myers Squibb's Zerit product - Brief Article
From FDA Consumer, 9/1/94

A fourth drug has been approved by FDA for the treatment of HIV and AIDS. The anti-viral drug is specifically for adults with advanced HIV infection who no longer respond to or are intolerant of other anti-viral drugs.

Zerit (stavudine, also known as D4T) belongs to the nucleoside analog class, which includes previously approved Retrovir (zidovudine, also known as AZT), Videx (didanosine, also known as DDI), and HIVID (zalcitabine, also known as DDC). Nucleoside analogs are thought to slow the progression of AIDS by inhibiting HIV replication. Data indicate that drugs in this class may delay the onset of AIDS symptoms in HIV-infected individuals, and may extend patient survival.

The drug was approved under FDA's accelerated approval mechanism allowing the drug's effectiveness to be assessed by surrogate rather than clinical endpoints. The major surrogate endpoint in the Zerit trials is CD4 cell counts.

In an ongoing trial comparing Zerit with continued Retrovir treatment of HIV-infected adults, all participants had taken Retrovir for at least 24 weeks. Their CD4 cell counts, which reflect the strength of the immune system, were between 50 and 500. (Counts in healthy individuals are normally 1,000 or higher.) Twelve weeks into the trial with 359 patients, the mean CD4 cell count in patients receiving Zerit increased by 22 cells per milliliter of blood, while the mean count in patients continuing on Retrovir declined by 22.

FDA concluded that the increase in CD4 counts is a likely indicator of a meaningful clinical benefit. Accelerated approval applicants must continue studies after approval to evaluate the true clinical benefit of their drugs. If data do not verify a benefit, FDA may withdraw its approval.

Between 15 and 21 percent of patients in Zerit trials experienced the drug's major side effect, peripheral neuropathy, which causes pain and tingling or numbness in the hands and feet. This side effect appears to be dose-related and can usually be reversed by stopping treatment.

In October 1992, Zerit became the first drug FDA granted parallel track status, which allowed the agency to make the promising new drug available to patients before approval. Since then, about 11,000 patients have been treated with Zerit.

Zerit's manufacturer is Bristol-Myers Squibb Co., New York, N.Y.

COPYRIGHT 1994 U.S. Government Printing Office
COPYRIGHT 2004 Gale Group

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