Safety Considerations in Early Chemical Design

Sygnature Discovery recently hosted a lecture by Professor Ruth Roberts and Dr Michael Morton from ApconiX.  Based at BioCity in Nottingham, Sygnature Discovery is the UK’s largest independent provider of integrated drug discovery resource and expertise.  The theme of the lecture and subsequent debate with the attendees was ‘Safety considerations in early chemical design: Challenges and opportunities’.   

Ruth introduced the top of drug attrition. She explained that the reason most drugs fail pre-clinically is due to safety considerations, as opposed to a lack of efficacy or poor PK/PD. Top of the list is cardiovascular safety!  To address this, the 3 key aspects of Target-Chemistry-Patient should be considered individually as part of the strategy to evaluate and mitigate risk. An important part of this is testing in vitro for unwanted ion channel activity. Mike explained how this activity can be measured, its translation in humans, and how this activity can be designed out by expert and timely collaboration with the chemist. The audience were keen to explore these ideas and the value of other in vitro assays as a basis for future collaboration as well as asking how this integrated approach might apply both to small molecules and to new modalities.

By | 2018-06-06T14:50:30+00:00 April 20th, 2017|Events|Comments Off on Safety Considerations in Early Chemical Design

About the Author:

Professor Ruth A Roberts, PhD, ATS, FBTS, ERT, FRSB, FRCPath Director and Cofounder, ApconiX, UK and Chair and Director of Drug Discovery, University of Birmingham, UK Ruth is chair of drug discovery at Birmingham University, UK and Cofounder of ApconiX, an integrated toxicology and ion channel company that brings together a team of world-renowned nonclinical safety experts with over 400 years of drug discovery and development experience. Previously, Ruth was Global Head of Regulatory Safety at AstraZeneca and Director of Toxicology for Aventis. Ruth is an established science professional bringing rigorous expert thinking to toxicology, drug discovery and drug development. With >140 publications in peer reviewed journals, she is focused on reducing attrition attributable to safety and toxicity. A former president of the British Toxicology Society, former president of EUROTOX, former secretary to SOT and president elect of the Academy of Toxicological Sciences, Ruth was the recipient of the SOT Achievement award in 2002, the EUROTOX Bo Holmstedt Award in 2009 and the SOT Founders award in 2018 for outstanding leadership in toxicology.