Stavudine

Stavudine is an inhibitor of HIV reverse transcriptase and a derivative of the nucleoside thymidine (Item No. 20519).¹ It inhibits HIV-1 replication in human peripheral blood mononuclear cells (PBMCs; EC₅₀ = 8.8 nM). Stavudine reduces the synthesis of HIV-specific antigen in MT-4 cells when used at concentrations ranging from 0.1 to 10 µg/ml and reduces HIV-induced plaque formation in MT-4 cells at 0.05 µg/ml.² It reduces plasma- and cell-associated viral load in macaques infected with a highly pathogenic isolate of HIV-2.³ Stavudine induces sustained hind paw mechanical allodynia in a rat model of antiretroviral toxic neuropathy (ATN) when administered at a dose of 75 mg/kg twice weekly for five consecutive doses for a cumulative dose of 375 mg/kg.⁴ Formulations containing stavudine, in combination with other antiretrovirals, have been used in the treatment of HIV-1 infection.

WARNING This product is not for human or veterinary use.

1. Lin, T.-S., Schinazi, R.F., and Prusoff, W.H. Potent and selective in vitro activity of 3'-deoxythymidin-2'-ene (3'-deoxy-2',3'-didehydrothymidine) against human immunodeficiency virus. Biochem. Pharmacol. 36(17), 2713-2718 (1987).

2. Hamamoto, Y., Nakashima, H., Matsui, T., et al. Inhibitory effect of 2',3'-didehydro-2',3'-dideoxynucleosides on infectivity, cytopathic effects, and replication of human immunodeficiency virus. Antimicrob. Agents Chemother. 31(6), 907-910 (1987).

3. Watson, A., McClure, J., Ranchalis, J., et al. Early postinfection antiviral treatment reduces viral load and prevents CD4⁺ cell decline in HIV type 2-infected macaques. AIDS Res. Hum. Retroviruses 13(16), 1375-1381 (1997).

4. Kuo, A., Nicholson, J.R., Corradini, L., et al. Establishment and characterisation of a stavudine (d4T)-induced rat model of antiretroviral toxic neuropathy (ATN) using behavioural and pharmacological methods. Inflammopharmacology 27(2), 387-396 (2019).