Boehringer Ingelheim to Leverage Philogen's DNA-Encoded Library Platform

July 21, 2017
Boehringer Ingelheim to Leverage Philogen's DNA-Encoded Library Platform
Boehringer Ingelheim will apply Philogen’s Encoded Self-Assembling Chemical (ESAC) Library Technology in the companies' second drug discovery collaboration. [Theasis/iStock Photos]

Boehringer Ingelheim will apply Philogen’s proprietary Encoded Self-Assembling Chemical (ESAC) library technology platform to discover and optimize novel small-molecule–based therapeutics, through a collaboration whose value was not disclosed.

ESAC enables Philogen to construct and screen DNA-encoded chemical libraries that according to the company are of unprecedented size and quality. Philogen owns or has exclusive rights to four human antibody libraries that contain more than 50 billion different binding specificities—ETH-2, PHILO-1, PHILO-2 and PHILO-DIAMOND—as well as a mouse antibody library, PHILO-TOP.

The company says its human antibody libraries have been used to generate high-quality binding specificities against more than 100 different antigens, including human monoclonal antibodies (mAbs) now being developed in clinical trials by Philogen.

The antibody libraries contain mAbs in scFv format. Once mAbs specific to the target antigen of choice are isolated, Philogen says, they can be easily reformatted into other recombinant antibody formats such as IgG, Fab, mini-antibody, Fc-fusion.

Philogen’s ESAC platform and DNA-Encoded Chemistry technology were developed by company researchers with the group of Prof. Dario Neri, Ph.D., at ETH Zurich during the past decade. The two technologies allow for screening of billions of small molecules, as well as for further optimization of “hit” compounds in a fully automatic, DNA-tagged, fragment-based drug-discovery manner.

“We are very excited about the opportunity to apply Philochem’s DNA-encoded library technology to drugging intractable proteins,” Darryl McConnell, vice president and head, Boehringer Ingelheim Research Site, Austria, said in a statement. “We believe that Philochem’s unique chemistry combined with Boehringer Ingelheim’s capabilities in discovering novel drugs could accelerate the optimization of chemical starting points to potent drug candidates.”

The collaboration is the companies’ second in nearly two years. In October 2015, Boehringer and Philogen committed to carrying out an exploratory trial investigating novel immunotherapy concepts for relapsed acute myeloid leukemia (AML) patients, as part of a partnership aimed at investigating novel treatment approaches for the disease.

Philogen’s pipeline includes a Boehringer-partnered undisclosed AML treatment that has concluded Phase I. Nearly all of Philogen’s pipeline treatments are in oncology, though the company is also developing a rheumatoid arthritis candidate, Dekavil (F8-IL10), in partnership with Pfizer.

This time, the companies have not specified what therapeutic areas they will focus on. Boehringer’s areas of focus include oncology, cardiometabolic diseases, central nervous system diseases, and immunology and respiratory diseases.

“We are both committed to the creation of new pharmaceutical agents, which may help treat serious unmet medical needs and provide a benefit to patients,” Dr. Neri, who is also cofounder and president of Philogen’s scientific advisory board, said in a statement. “ESAC technology is ideally suited for the identification of synergistic chemical fragments, which recognize adjacent binding sites on the surface of the target protein of interest.

“We are confident that ESAC technology will facilitate hit and lead discovery activities, complementing the strong medicinal chemistry technologies already established at Boehringer Ingelheim,” Dr. Neri added.

Founded in 1996, Philogen is headquartered in Siena, Italy, with research activities conducted at its subsidiary Philochem in Zürich, Switzerland.