Steven R. LaPlante

TL;DR: Administration of BILN 2061 to patients infected with HCV genotype 1 for 2 days resulted in an impressive reduction of HCV RNA plasma levels, and established proof-of-concept in humans for an HCV NS3 protease inhibitor, illustrating the potential of the viral-enzyme-targeted drug discovery approach for the development of new HCV therapeutics.

TL;DR: This Minireview brings together the various strategies that have been adopted and proposes a general approach to handling an aspect of stereochemistry which has received little attention from drug regulatory agencies.

TL;DR: Assessing Atropisomer Axial Chirality in Drug Discovery and Development Steven R. F. Fandrick, Oliver Hucke, Ray Kemper, Stephen P. Miller, and Paul J. Edwards assess the importance of chiral consistency in drug discovery and development.

TL;DR: A strategy to reveal and classify compounds that have atropisomeric chirality is introduced and decisions can be made during early discovery stages such as “hit‐to‐lead” and “lead optimization,” to foresee and validate the presence ofAtropisomers and to exercise options of removing, further stabilizing, or rendering the chiral axis of interest more freely rotatable via SAR design, thereby decreasing this potential liability within a compound series.