Discovery Formulations : Approaches and Practices in Early Preclinical Development

Reduced portfolio attrition and faster development of high quality drugs that address unmet medical needs is an established imperative within the pharmaceutical industry. Given the complexity of modern drug discovery, this goal can only be achieved through well-designed pharmacology, pharmacokinetic, and toxicology studies resulting in the identification of exceptional development candidates. Pivotal to the success of these studies is the use of appropriate formulations designed to deliver the compound to the desired site via the desired route, in a consistent and acceptable manner. It is also essential that the formulations are developed with a clear understanding of the goals of the studies, future application of the formulations, and/or the data from the studies. However, the development of an appropriate discovery formulation can be challenging due to a myriad of factors that include suboptimal biopharmaceutical properties, dose, compound purity, compound availability, and aggressive timelines. This chapter will cover formulations used in the discovery setting from conventional vehicles to solubilizing systems and alternate delivery approaches. The application of the appropriate formulation approach to meet the study goals and efficient development timelines will also be discussed.