Pharmaceutical Solid Form Selection: A Recent Review and Data Tapestry

Abstract

The selection of the “development” or “commercial” solid form during pharmaceutical development is a key milestone on the journey of a molecule into a medicine. The physicochemical properties that impact product performance are, to a great extent, influenced by the solid-state structure and particle attributes of the active pharmaceutical ingredient. Therefore, an understanding of the solid state and associated materials science of the new active ingredient is crucial at the interface of drug discovery and pharmaceutical sciences. In this paper, we will review and reflect on the solid forms that have been launched as medicines in the last two decades. The paper was inspired by a preliminary review presented at the 15-year celebration of the Crystal Form Consortium. The solid form nomination process in companies has been built upon linking academic progress in structural science to the best current industrial practices that pharmaceutical scientists apply in screening solid forms. An overview of how a collection of important data threads (community knowledge, structural sciences, screening landscapes) comes together in a tapestry of information will be highlighted. The review and key points will be accentuated through the use of examples, which will illuminate some of the scientific challenges and catalyze a perspective on a future state where solid form design allows acceleration of new chemical entities.