In vitro Activity of Stampidine against Primary Clinical Human Immunodeficiency Virus Isolates

Uckun, Fatih M.; Pendergrass, Sharon; Qazi, Sanjive; Venkatachalam, Taracad K.
January 2004
Drug Research / Arzneimittel-Forschung (Editio Cantor Verlag fur;Jan2004, Vol. 54 Issue 1, p69
Academic Journal
The in vitro activity profile of stampidine (CAS 217178-62-6, STAMP) was examined against clinical isolates of HIV-1. In a side-by-side comparison against 10 zidovudine-sensitive clinical HIV-1 isolates, STAMP was 100-fold more potent than stavudine (CAS 3056-17-5) and twice as effective as zidovudine (CAS 305 16-87-1). STAMP was also active against pheno-typically and/or genotypically NRTI (nucleoside analog inhibitors of reverse transcriptase) - resistant HIV and inhibited the replication of 20 zidovudine-resistant clinical 11EV-i isolates with low nanomolar to subnanomolar IC[sub50] values. Similarly, STAMP inhibited the replication of 9 genotypically NNRTI (non-nucleoside analog inhibitors of reverse transcriptase) -resistant clinical HIV-1 isolates (n = 9) with an average IC[sub50] value of 11.2 ± 6.5 nmol/L. The remarkable potency of STAMP against clinical HIV-1 isolates with NRTI- or NNRTI -resistance warrants the further development of this promising new antiviral agent.


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