Principal Scientist Merck & Co., Inc. West Point, Pennsylvania
NaV1.7 is an intriguing target for pharmaceutical intervention in various human pain conditions due to genetic evidence for its role in pain sensation. Identifying a molecule which can be effectively and safely administered in the clinic to test the hypothesis has proven quite challenging. This presentation will describe numerous hurdles along the path of discovery and preclinical development of NaV1.7 inhibitors, and navigation of these obstacles to progress a candidate to first in human studies.
Learning Objectives:
Describe challenges often faced in drug discovery and preclinical development.
Identify multifactorial considerations in establishing in vitro to in vivo potency relationship such as state dependence, isoform selectivity, species specificity, and biodistribution.
Discuss utility of PK-PD modeling to integrate in vitro and in vivo preclinical data for quantitative description of exposure-response relationships to enable translation between species.
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