Roche takes crystal-clear route to development

- Last updated on GMT

Related tags: Crystal, Pharmacology

Swiss drugmaker Roche has succeeded in developing a crystalline
form of one of its pipeline compounds with the help of a US
company, TransForm Pharmaceuticals, that is applying a
high-throughput approach to form and formulation.

Swiss drugmaker Roche has succeeded in developing a crystalline form of one of its pipeline compounds with the help of a US company, TransForm Pharmaceuticals, that is applying a high-throughput approach to form and formulation.

Finding a crystalline form of a drug candidate is generally considered a necessary prerequisite for its development as a pharmaceutical, both to ensure purity and to maximise the likelihood of the compound performing predictably in the formulation. However, an increasing number of compounds being discovered by the pharmaceutical industry are novel in structure and resistant to crystallisation.

"The ability to crystallise such compounds rapidly can therefore have a significant impact on R&D efficiency, as well as the commercial viability of those product candidates,"​ according to TransForm.

Whereas the conventional approach to form and formulation has been low-scale, with 10-20 variants typically being assessed over a two- to four-week period, TransForm's approach can amass data on 20,000 form experiments in two weeks. The firm's CrystalMax platform can grow crystal structures on a huge scale and is applicable to almost any compound that has a solid structure, from small molecules to proteins.

Allied to this is a series of in vitro​ proxies which can strip out the less promising crystal structures. For example, the firm has a system for mimicking the environment in the gut that could be used to weed out those forms whose bioavailability would not be suitable for oral dosing.

The successful crystallisation will assist Roche in advancing its unnamed compound into clinical development, and entitles TransForm​ to a milestone payment under the collaboration.

Under the terms of the partnership between the two companies, TransForm receives upfront research funding and success-based milestones from Roche for conducting comprehensive crystallisation studies on development-stage Roche compounds.

The company also has collaborations in place with Alza and Eli Lilly, and is planning to develop its own range of in-house drug candidates, with a focus on drugs that are already on sale but which have formulation difficulties that limit their potential.

Related topics: Preclinical Research, Ingredients

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