In the preclinical development of kinase inhibitors, it is important to employ a sequential process — selecting only the best compounds at each stage, with the goal of retaining only one or two optimized leads by the end of the process.
TORONTO (PRWEB) May 25, 2023
Protein kinases act as master regulators of multiple key processes within the cell cycle, and aberrant regulation of their activity has been associated with a large number of pathological conditions, including inflammatory diseases. Therefore, protein kinases constitute promising targets for drug development, and numerous preclinical and clinical programs for kinase inhibitors are ongoing.
In this webinar, the featured speaker will examine the challenges associated with the preclinical development of kinase inhibitors. They will provide insights into the strategies used to screen new chemical entities, as well as the key steps, checkpoints and custom tools used throughout the hit-to-lead and lead optimization phases.
In the preclinical development of kinase inhibitors, it is important to employ a sequential process — selecting only the best compounds at each stage, with the goal of retaining only one or two optimized leads by the end of the process.
The first step consists in developing and performing in vitro assays for direct kinase inhibition testing. Active compounds can then progress to a phenotypic cell assay and undergo inhibitor selectivity testing. Lastly, interferences with blood components should be evaluated by performing inhibition tests in a whole blood system.
Once active and selective inhibitors have been selected, drug metabolism and pharmacokinetics (DMPK) steps enable a rigorous selection of compounds with suitable absorption, distribution, metabolism and excretion profiles. Mathematical models, when provided with the in vivo and in vitro DMPK data from rodent systems, can extrapolate probable in vivo parameters in humans from in vitro assays performed on human samples, helping with future dose calculations.
Although in vivo activity should be relatively predictable using the combination of in vitro activity and PK parameters, it is still necessary to test compound activity in vivo to validate the PK/PD model. In parallel, target validation may be documented using clinically relevant disease models.
Join this webinar to learn about the preclinical development of kinase inhibitors for the treatment of inflammatory diseases.
Join Dr. Pauline Bornert, Study & Research Director, Oncodesign Services, for the live webinar on Thursday, June 15, 2023, at 11am EDT (4pm BST/UK).
For more information, or to register for this event, visit Kinase Inhibitors for Inflammatory Diseases: Preclinical Development.
ABOUT XTALKS
Xtalks, powered by Honeycomb Worldwide Inc., is a leading provider of educational webinars to the global life science, food and medical device community. Every year, thousands of industry practitioners (from life science, food and medical device companies, private & academic research institutions, healthcare centers, etc.) turn to Xtalks for access to quality content. Xtalks helps Life Science professionals stay current with industry developments, trends and regulations. Xtalks webinars also provide perspectives on key issues from top industry thought leaders and service providers.
To learn more about Xtalks visit http://xtalks.com
For information about hosting a webinar visit http://xtalks.com/why-host-a-webinar/
Contact:
Vera Kovacevic
Tel: +1 (416) 977-6555 x371
Email: vkovacevic@xtalks.com
