(262d) Making Molecules into Medicines: Engineering in Materials Properties

Over the last 3-4 decades since the development of biochemical understanding of disease, the pharmaceutical industry has been driven by identifying molecular targets and creating new molecular entities that inhibit, activate, agonize or antagonize the target to produce a desired pharmacologic response in the patient. In general the focus has been on finding very potent and selective compounds by employing novel technologies including high throughput genomics, chemistry and biochemical screening. The resultant molecules are interesting pharmacological agents, but in many cases lack the requisite physical properties to make them effective drugs. In a parallel process, there has been an evolution in materials science expanding from inorganic materials to small molecular weight organic compounds and polymeric structures. Here too, scientists and engineers have availed themselves of high throughput technologies to explore large experimental spaces in the search for novel structural forms whose properties enable performance commensurate with delivery of the molecules to the patient. This presentation will use industry examples to demonstrate the importance of understanding and controlling materials properties and will proceed to discuss techniques to rapidly identify and evaluate novel solid state forms as drug development candidates. In particular, the presentation will emphasize the value of designing co-crystal structures in which the active drug molecule shares the crystalline structure with other pharmaceutically acceptable components whose presence significantly improve the pharmaceutical properties of the material. Furthermore, the importance of the formulation components in controlling the delivery characteristics of the drug will be highlighted.