ABSTRACT
Stavudine (2′,3′-didehydro-2′3′-deoxythymidine, d4T) is a potent inhibitor of HIV reverse transcriptase in vitro. Stavudine is an odorless, relatively water-soluble white crystalline solid with a molecular weight of 224 and formula of C10H12N2O4, with the chemical structure shown in Figure 229.1. Drug concentrations are described in micromols or micrograms per milliliter (1 μ? is approximately equivalent to 0.2 μg/ml). Stavudine was first synthesized in 1966 by Horwitz and co-workers (1966), who were also responsible for the synthesis of zidovudine (AZT) (see Chapter 225, Zidovudine) and zalcitabine (ddC) (see Chapter 227, Zalcitabine) as well as early antiretroviral therapies against HIV. Stavudine has activity against both HIV-1 and HIV-2 and was the fourth nucleoside reverse transcriptase inhibitor to become commercially available, marketed as Zerit by Bristol-Myers Squibb. Stavudine was licensed for adults by the US FDA in 1994, and for children in 1996. Chemical structure of stavudine. https://s3-euw1-ap-pe-df-pch-content-public-p.s3.eu-west-1.amazonaws.com/9781315152110/08d8042d-9481-4a8d-8c27-9bd589f6de6b/content/fig229_1.tif" xmlns:xlink="https://www.w3.org/1999/xlink"/>
