RIP2 kinase has been identified as a key signal transduction partner in the NOD2 pathway contributing to a variety of human disease pathologies, including immune-mediated inflammatory diseases such as Crohn’s Disease and ulcerative colitis. At GSK, we have successfully targeted small molecule inhibitors of RIP2 kinase to block this pathway in the hope of leading to positive clinical outcomes as highlighted in previous publications. In this presentation we will focus on the methodologies and approaches we took to translate preclinical coherent pharmacology, drug metabolism and pharmacokinetics into early human dose estimates, facilitating more effective SAR generation on a number of different molecular series. These early estimates of human dose were then expanded to generate more complete dose predictions leading to the successful identification and selection of drug candidates for progression into clinical development.

Application of early human dose predictions to the RIP2 Kinase project

ACS Spring Meeting 2021

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.