Anti-retroviral activity of GMP-grade stampidine against genotypically and phenotypically nucleoside reverse transcriptase inhibitor resistant recombinant human immunodeficiency virus. An in vitro study.
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.
Uckun
Fatih M
FM
Parker Hughes Institute, Roseville, MN, USA. fatih_uckun@tmo.blackberry.net
DuMez
Darin
D
Qazi
Sanjive
S
Tibbles
Heather
H
Venkatachalam
Taracad K
TK
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
D019380:Anti-HIV Agents; D002214:Capsules; D054306:Dideoxynucleotides; D018894:Reverse Transcriptase Inhibitors; C472384:stampidine; D013938:Thymidine Monophosphate; D018119:Stavudine