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Arzneimittelforschung 2007; 57(2): 112-121
DOI: 10.1055/s-0031-1296592
Antibiotics · Antiviral Drugs · Chemotherapeutics · Cytostatics
Editio Cantor Verlag Aulendorf (Germany)

Anti-retroviral Activity of GMP-Grade Stampidine against Genotypically and Phenotypically Nucleoside Reverse Transcriptase Inhibitor Resistant Recombinant Human Immunodeficiency Virus

Fatih M. Uckun
1   Parker Hughes Institute, Roseville, MN, USA
2   Paradigm Pharmaceuticals, White Bear Lake, MN, USA
3   Ikaros Enterprises, Inc., Hudson, WI, USA
,
Darin DuMez
3   Ikaros Enterprises, Inc., Hudson, WI, USA
,
Sanjive Qazi
1   Parker Hughes Institute, Roseville, MN, USA
2   Paradigm Pharmaceuticals, White Bear Lake, MN, USA
,
Heather Tibbies
1   Parker Hughes Institute, Roseville, MN, USA
2   Paradigm Pharmaceuticals, White Bear Lake, MN, USA
,
Taracad K. Venkatachalam
2   Paradigm Pharmaceuticals, White Bear Lake, MN, USA
› Author Affiliations
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Publication History

Publication Date:
21 December 2011 (online)

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Abstract

The in vitro potency of GMP-grade stampidine (CAS 217178-62-6) was examined against 3 clinical HIV-1 isolates and 6 recombinant HIV-1 clones with multi-NRTI resistance (NRTI: nucleoside reverse transcriptase inhibitors). GMP-grade stampidine active drug substance (Lot #'s MPR-M0008.00-01 and MPR-M0008.01-01) as well as GMP-grade stampidine extracted from the clinical stampidine capsules (GMP-Grade Clinical Batch, Pharmaceutical Service Lot Number 15910601) were highly potent and exhibited nanomolar IC50 values against clinical HIV-1 isolates as well as recombinant HIV-1 clones with multi-NRTI resistance containing common patterns of reverse transcriptase mutations responsible for NRTI resistance.

Key words

AIDS - CAS 217178-62-6 - Human immunodeficiency virus - Nucleoside reverse transcriptase inhibitors - Stampidine, antiretroviral activity, GMP-grade, in vitro study