2. Academic Validation
  3. KP-1212/1461, a nucleoside designed for the treatment of HIV by viral mutagenesis

KP-1212/1461, a nucleoside designed for the treatment of HIV by viral mutagenesis

  • Antiviral Res. 2005 Jul;67(1):1-9. doi: 10.1016/j.antiviral.2005.03.004.
Kevin S Harris 1,  William Brabant,  Sheila Styrchak,  Alexander Gall,  Richard Daifuku
Affiliations

Affiliation

  • 1 Koronis Pharmaceuticals Inc., 12277 134th Ct. N.E. Redmond, WA 98052, USA. [email protected]
PMID: 15890415 DOI: 10.1016/j.antiviral.2005.03.004
Abstract

We report the activities of a novel nucleoside analog against HIV. This nucleoside (KP-1212) is not a chain terminator but exerts its Antiviral effects via mutagenesis of the viral genome. Serial passaging of HIV in the presence of KP-1212 causes an increase in the mutation rate of the virus leading to viral ablation. HIV strains resistant to KP-1212 have not yet been isolated. Quite to the contrary, virus treated with KP-1212 exhibited an increased sensitivity not only to KP-1212 but also to another nucleoside Reverse Transcriptase Inhibitor (NRTI), zidovudine. HIV strains resistant to Other NRTIs (e.g. zidovudine, lamivudine, stavudine, abacavir, etc.) exhibited no cross-resistance towards KP-1212. Multiple assays confirmed that KP-1212 has a favorable (low) genotoxicity profile when compared to some approved Antiviral nucleosides. In addition, KP-1212 is not toxic to mitochondria nor does it exhibit any inhibitory effects on mitochondrial DNA synthesis.

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