Stavudine-13C-d3

Stavudine-¹³C-d₃ is intended for use as an internal standard for the quantification of stavudine by GC- or LC-MS. Stavudine is an inhibitor of HIV reverse transcriptase and a derivative of the nucleoside thymidine .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.

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 virusBiochem. 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 virusAntimicrob. 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 macaquesAIDS Res. Hum. Retroviruses13(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 methodsInflammopharmacology27(2)387-396(2019)