Bayer and X-Chem Pharmaceuticals have expanded a global drug discovery collaboration launched in 2012 across multiple therapeutic areas and target classes. The expanded partnership could generate up to $528 million-plus for X-Chem.

The companies agreed to extend Bayer's access to X-Chem's DNA-Encoded X-Chem (DEX™) technology, which is based on DNA-encoded libraries of small molecules with more than 120 billion molecules. The new multiyear agreement will significantly expand the scope and duration of the collaboration, which aims to discover innovative lead structures for complex drug targets in areas of high unmet medical need.

Through the DEX library, X-Chem says, it can discover multiple series of novel, potent, and selective lead compounds at an unprecedented rate of success against a wide range of targets, including some that previously failed using conventional screening methods.

The company says its proprietary library design, screening methodology, and bioinformatics, as well as its approach to library construction, allow for additional chemical reactions to become usable in DNA-encoded library synthesis. These features, according to X-Chem, yield a much greater repertoire of diversity for small molecules, covering categories that include fragment molecules, small-molecular-weight heterocyclic compounds, and macrocyclic structures.

“We have identified the DEX platform as a highly valuable extension for our drug discovery efforts. We are looking forward to working with X-Chem on some of our highest-priority targets, for which X-Chem's platform is ideally suited,” Professor Andreas Busch, member of the Executive Committee of Bayer's Pharmaceuticals Division and head of drug discovery, said in a statement.

Bayer has an exclusive option to license any programs generated through the collaboration.

In return, Bayer agreed to pay X-Chem an upfront payment, R&D funding, as well as potential preclinical, clinical, and regulatory milestone payments totaling up to $528 million. Bayer also agreed to pay X-Chem royalties and sales milestones for each successfully commercialized drug that results from a licensed collaboration program.

Bayer previously licensed two programs for multiple series of small molecules from X-Chem that address complex target structures such as protein–protein interactions. In February 2014, X-Chem licensed to Bayer an early-stage drug discovery program directed against an epigenetic drug target, after achieving an unspecified success milestone. Later that year, X-Chem licensed a second program consisting of several series of small molecule compounds against a cardiovascular drug target.

Bayer is among several pharma giants that have inked collaborations with privately-held X-Chem; others include AstraZeneca, Pfizer, and Roche. “With multiple successes across our partnerships, the DEX™ platform has been broadly validated to deliver novel chemical entities against a wide array of targets, including difficult targets,” added X-Chem CEO Rick Wagner, Ph.D.

Founded in 2009, X-Chem formed a strategic partnership, including an investment, a year later with Pharmaceutical Product Development, LLC.  PPD acquired all remaining interests in X-Chem in 2014.

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