Stampidine is a nucleoside analogue reverse transcriptase inhibitor (NRTI) developed by the Parker Hughes Institute. It is a derivative of d4T (stavudine, Zerit), and has been designed to avoid dependence on the rate limiting step of phosphorylation of stavudine to stavudine monophosphate. This is governed by the supply of thymidine kinase that is available, and stavudine is poorly phosphorylated to its monophosphate form in thymidine kinase-deficient cells, such as macrophages.

Laboratory studies show that stampidine is substantially more potent than stavudine, and active in thymidine-kinase deficient T-cells.

Toxicity has proved extremely rare in rodent studies even at very high doses.

Stampidine is approximately ten to 100 times more active than stavudine against non-B HIV-1 subtypes (A, C, F and G), and twice as active as AZT (zidovudine, Retrovir) against the same panel of non-B subtypes.

Stampidine is active against HIV isolates with five thymidine analogue mutations, at an average IC₅₀ of 2.8 to 3.2nM (Uckun 2002b).

References

Uckun FM et al. In vivo toxicity, pharmacokinetics and anti-human immunodeficiency virus activity of stavudine-5'-(p-bromophenyl methoxyalaninyl phosphate) (Stampidine) in mice. Antimicrob Agents Chemother 46: 3428-3436, 2002a.

Uckun FM et al. Stampidine is a potent inhibitor of zidovudine and nucleoside analog reverse transcriptase inhibitor-resistant primary clinical human immunodeficiency virus type 1 isolates with thymidine analog mutations. Antimicrob Agents Chemother 46: 3613-3616, 2002b.