Abstract
Identification of an optimal crystalline phase of a preclinical drug candidate plays a critical role in drug development, impacting bioavailability, solubility, stability, and physicochemical properties. Historically, drug candidate phase optimization was delayed until the development stage. More recently, however, these efforts have been moved earlier during the discovery stage. As such, an early understanding of a drug candidate’s phase behavior can clarify development liabilities and allow for more rapid development. This chapter begins with a rational for early phase optimization and describes critical attributes of an optimal development phase that impact scale-up and formulation design and performance. As detailed discussion on methods of phase screening, preparation and characterization is presented along with a brief section on preclinical formulation as it pertains to the selected solid state phase.
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McNevin, M., Higgins, J. (2015). Strategies and Methods for Drug Candidate Phase Optimization in Discovery Space. In: Templeton, A., Byrn, S., Haskell, R., Prisinzano, T. (eds) Discovering and Developing Molecules with Optimal Drug-Like Properties. AAPS Advances in the Pharmaceutical Sciences Series, vol 15. Springer, New York, NY. https://doi.org/10.1007/978-1-4939-1399-2_7
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DOI: https://doi.org/10.1007/978-1-4939-1399-2_7
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