title: Anti-retroviral activity of GMP-grade stampidine against genotypically and phenotypically nucleoside reverse transcriptase inhibitor resistant recombinant human immunodeficiency virus. An in vitro study.
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 159I0601) 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.
authors.affiliation: Parker Hughes Institute, Roseville, MN, USA. fatih_uckun@tmo.blackberry.net
authors.forename: Fatih M
authors.initials: FM
authors.lastname: Uckun
authors.forename: Darin
authors.initials: D
authors.lastname: DuMez
authors.forename: Sanjive
authors.initials: S
authors.lastname: Qazi
authors.forename: Heather
authors.initials: H
authors.lastname: Tibbles
authors.forename: Taracad K
authors.initials: TK
authors.lastname: Venkatachalam
mesh_terms: D019380:Anti-HIV Agents / Q000494:pharmacology*; D002214:Capsules; D002626:Chemistry, Pharmaceutical; D003001:Cloning, Molecular; D003588:Cytopathogenic Effect, Viral; D054306:Dideoxynucleotides; D024882:Drug Resistance, Viral / Q000187:drug effects / Q000235:genetics; D006678:HIV / Q000187:drug effects; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D009154:Mutation; D012044:Regression Analysis; D018894:Reverse Transcriptase Inhibitors / Q000494:pharmacology*; D018119:Stavudine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D013938:Thymidine Monophosphate / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D019380:Anti-HIV Agents; D002214:Capsules; D054306:Dideoxynucleotides; D018894:Reverse Transcriptase Inhibitors; C472384:stampidine; D013938:Thymidine Monophosphate; D018119:Stavudine