Solid Form Optimization

Evotec boasts an experienced team with extensive pharmaceutical expertise dedicated to identifying optimal solid forms and biopharmaceutical properties for further development. Over the past decade, the team has successfully completed more than 300 solid form screening processes.

To facilitate this process, we have developed a customized robotic screening platform capable of identifying salts, co-crystals, and polymorphs. This platform offers flexible and modifiable screening conditions to optimize the properties of the active pharmaceutical ingredient (API). Scientific approaches, including considerations of pKa differences, molecular diversity, and sophisticated models involving surface electronic density interaction and mixture enthalpy calculations, support the selection of guest molecules.

The newly identified API solid forms undergo manual confirmation at a ten milligram scale, while simultaneously developing a preliminary crystallization process to pre-select the most promising forms for scale-up. Following a larger upscale (hundred milligrams scale) led by our process chemistry team, each pre-selected API form undergoes an in-depth Solid State/PhysChem analytical package.

This efficient and successful process has been applied to more than 150 preclinical candidates over the past decade, with each case accompanied by a CMC risk assessment document that provides a clear recommendation for the most suitable form for future human clinical trials.

Our platform provides a wealth of information related to the identified solid forms, including solid-state profiling (crystalline nature, thermal behavior, hygroscopicity data, particle characterization, spectroscopy), PhysChem profiling (pKa and dissociation equilibrium, LogP and Log D, solubility profiling in aqueous or biorelevant media, accelerated physical and chemical stability, chemical stability), and in-silico PhysChem profiling (XRPD indexation for crystalline purity and crystal structure determination, ab-initio prediction from structure of NMR, Raman, FTRIR spectra, LogP, Log DpH partition coefficient, screening of organic/organic or water/organic Liquid-Liquid extraction coefficient, ab-initio prediction of API solubility, UV coefficient response, and chemical degradation pathway).

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Ashley Jarvis

Ashley Jarvis, PhD, FRSC

EVP Head of Drug Discovery Chemistry

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Evotec has the right technologies & disease understanding to meet our partners' evolving needs: a comprehensive disease knowledge at the molecular level, cutting-edge technologies & platforms to translate this expertise into effective precision medicines.