Translational Pharmacokinetic-Pharmacodynamic Modeling of NaV1.7 Inhibitor MK-2075 to Inform Human Efficacious Dose

• Main Authors: Jeanine E. Ballard (Author), Parul S. Pall (Author), Joshua Vardigan (Author), Fuqiang Zhao (Author), Marie A. Holahan (Author), Xiaoping Zhou (Author), Nina Jochnowitz (Author), Richard L. Kraus (Author), Rebecca M. Klein (Author), Darrell A. Henze (Author), Andrea K. Houghton (Author), Christopher S. Burgey (Author), Christopher Gibson (Author), Arie Struyk (Author)
• Format: Book
• Published: Frontiers Media S.A., 2021-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

MK-2075 is a small-molecule selective inhibitor of the NaV1.7 channel investigated for the treatment of postoperative pain. A translational strategy was developed for MK-2075 to quantitatively interrelate drug exposure, target modulation, and the desired pharmacological response in preclinical anima...