2. Academic Validation
  3. Discovery of ANA975: an oral prodrug of the TLR-7 agonist isatoribine

Discovery of ANA975: an oral prodrug of the TLR-7 agonist isatoribine

  • Nucleosides Nucleotides Nucleic Acids. 2007;26(6-7):635-40. doi: 10.1080/15257770701490472.
Alan X Xiang 1,  Stephen E Webber,  Bradley M Kerr,  Erik J Rueden,  Joseph R Lennox,  Gregory J Haley,  Tingmin Wang,  John S Ng,  Mark R Herbert,  David L Clark,  Virginia N Banh,  Wei Li,  Simon P Fletcher,  Kevin R Steffy,  Darian M Bartkowski,  Leonid I Kirkovsky,  Lisa A Bauman,  Devron R Averett
Affiliations

Affiliation

  • 1 Anadys Pharmaceuticals, Inc., San Diego, California 92121, USA. axiang@anadyspharma.com
PMID: 18066870 DOI: 10.1080/15257770701490472
Abstract

ANA975, a 5-amino-3-beta -D-ribofuranosyl-3H-thiazolo[4,5-d]pyrimidin-2-one derivative, was synthesized in the search of an oral prodrug of isatoribine, a small molecule Toll-like Receptor 7 (TLR-7) agonist. Several strategies were studied to enable the kilogram-scale synthesis of ANA975. Three general total syntheses are described. In the phase I clinical study of ANA975 against hepatitis C virus (HCV), conversion to isatoribine in plasma was rapid and effective, delivering levels of isatoribine that have been shown to be clinically relevant.

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