Progressing preclinical drug candidates: strategies on preclinical safety studies and the quest for adequate exposure

Drug discovery lead optimization teams face many diverse challenges in the search for drug development candidates. This includes understanding the toxicology profile of a candidate, and some strategies call for in vivo preclinical safety studies to be moved increasingly earlier in the discovery phase to increase the likelihood of success in development. One of the final hurdles in these pursuits is achieving adequate exposure to support safety margins for human clinical trials. In this article, we describe several strategies on early toxicology studies along with various enabling formulation methods that can be employed to achieve optimal oral absorption. These two elements of research together can significantly increase the speed preclinical drug candidates can move through development, and the overall probability of success in identifying viable new drugs.

► There is increasing emphasis in drug discovery on understanding a drug candidate's safety profile, and many pre-clinical toxicology studies are being executed at earlier stages.
► Significantly high exposure in pre-clinical species is often required in order to achieve adequate safety margins for clinical development.
► There are various strategies and enabled pre-clinical formulation technologies now available for application in the drug discovery stage in order to maximize exposure.