Cocrystals a New Class of Drugs

Will the latest FDA draft attract more interests from industry?

Cocrystals, a relatively new class of multicomponent systems, attracted in the last years both the interest of industrial as well as academic researchers. Several definitions and classifications are available within the scientific world. Often referred to as co-crystals or cocrystals, these multicomponent systems managed to initiate challenging discussions. Co-crystallization has emerged over the past decade as an attractive technique for modification of the physicochemical properties of organic compounds, such as modifying the aqueous solubility and/or dissolution rate, stability, and bioavailability. Cocrystals are a feasible solution for those compounds which do not show to have another form with the required physicochemical properties.

In 2013 the FDA’s view on the topic referred to cocrystals as dissociable “API—excipient molecular complexes". This guidance created a lot of controversy from both industry and academia.

3 years later, the agency comes back with a different perspective. "Pharmaceutical co-crystals have opened up opportunities for engineering solid-state forms beyond conventional solid-state forms of an active pharmaceutical ingredient (API), such as salts and polymorphs. From a physical chemistry perspective, co-crystals can be viewed as a special case of solvates and hydrates, wherein the second component, the coformer, is nonvolatile. Therefore, co-crystals are classified as a special case of solvates in which the second component is nonvolatile."

Would this ease the embrace of cocrystals by pharmaceutical companies? Would Agrochemical industry and other markets easier adopt cocrystals as a strategy for development? How would this impact the development timelines, manufacturing process or IP strategy? Something to be certainly evaluated in the future.

Experts' opinion

Dr. Michael Gruß is a professional with more than 14 years’ experience in process development as head of laboratory at Grünenthal and currently leading Solid State Concepts. Named inventor/co-inventor in more than 15 patent applications, has a wide expertise and experience in solid state chemistry, crystallization, analytical chemistry, drug development, scale-up/scale-down, and CMC.

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Prof. Dr. Joop H. ter Horst leads an application driven fundamental research group at the University of Strathclyde in Glasgow. His group is focused on various crystallization related topics such as crystallization control, continuous crystallization and chiral resolution.

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Dr. Martin Viertelhaus is Research Scientist Crystalline Materials and Polymorphism at BASF SE, Ludwigshafen, Germany. His expertise is in the field of solid state development and physicochemical characterization of active ingredients: e.g. agrochemical, pharmaceutical and performance chemicals. During his professional career, he worked for pharmaceutical and chemical companies as well as for a service provider.

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