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Bicoll GmbH Announces a Fast Small Molecule Ligand Validation Method for Orphan Targets



8/29/2013 9:12:29 AM

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Munich (Germany) – August-29, 2013 – BICOLL Group announces today the successful application of its technology for the identification of ligands of a specific orphan target. As described in a new publication in the Journal of Biomolecular Screening1, a class of potent and bioavailable RAR-related orphan receptor alpha (RORa) agonists has been identified in a plant extract library from BICOLL. The findings were generated in collaboration with Genfit, a biopharmaceutical company at the forefront of drug discovery and development, focusing on the early diagnosis and preventive treatment of cardiometabolic and associated disorders. The successful joint program demonstrates the general effectiveness of BICOLL's small molecule approach on orphan targets as a case study. Indeed, the use of BICOLL's technology of fractionated plant extracts (Profiles™) has led to a timely identification of potent ligands and enabled target validation studies in vivo within a period of 9-months from the start of the initial screening.

BICOLL's plant Profiles™ is a fast-track validation tool for any small molecule screening program. It gives partners the opportunity to obtain essential target validation data in animal model(s) with an unprecedented rapidity. Classically, the identification of such ligands may take between 18 and 24 months or even longer. The disclosed plant ProfilesTM-approach brings together two important aspects that help to overcome usual drug discovery program difficulties, i.e. an enormous chemical diversity (up to 100.000 relevant, chemical entities in a typical screening campaign) and a relative ease of operations with respect to screening procedures, since the full set of this diversity can be leveraged without explicit purification.

"Any medicinal chemistry program will profit from employing plant Profiles™ in drug discovery - either as a jump starting point, benchmarking, or inspiration for chemists" stated Dr. Kai Lamottke, managing director of BICOLL and co-author of the publication. "Valid data from animal models can be quickly produced and "go" or "no-go" decisions can be done without any big investment or set-up of a compound library of highly pure and initially defined small molecules. Our partner Genfit is highly experienced in evaluating the suitability of difficult orphan targets for drug discovery programs. Genfit's drug discovery team led by Dr. Robert Walczak leveraged the whole set of information generated by our technology and translated the findings rapidly into animal studies. In principle, ProfilesTM technology can be used in any classical drug discovery program, even on a difficult target, as a ready to go solution".

About BICOLL:

BICOLL is a biopharmaceutical company, offering pre-clinical support in the area of Drug Discovery from Natural Products and Medicinal Chemistry. Dedicated to the discovery and optimization of the highest quality lead compounds, BICOLL provides an efficient, multi-disciplinary approach to drug discovery. With outstanding expertise in high tech natural product chemistry and validated experience in medicinal chemistry, BICOLL increases quality and quantity of the drug discovery pipeline of its partner's candidates portfolio.

The BICOLL Group provides its services to a number of international clients of various fields of interest, e.g. pharmaceutical and agrochemical industry. The BICOLL Group comprises two legal entities: BICOLL GmbH in Munich, Germany and BICOLL Biotechnology (Shanghai) Co. Ltd., P.R. China. Technology development, cooperation management and marketing are functions in Munich, while facilities for research and development are located in Shanghai.

BICOLL currently employs 40 people at both locations.

www.bicoll-group.com

Contact BICOLL:

Dr. Nicole Feling, Public Relations Management

+49 (0) 89 / 82010630,

nicole.feling@bicoll-group.com

About GENFIT:

GENFIT is a biopharmaceutical company focused on the Discovery and Development of drug candidates in therapeutic fields linked to cardiometabolic disorders (prediabetes/diabetes, atherosclerosis, dyslipidemia, inflammatory diseases…). GENFIT uses a multi-pronged approach based on early diagnosis, preventive solutions, and therapeutic treatments and advances therapeutic research programs, either independently or in partnership with leading pharmaceutical companies, including Sanofi, to address these major public health concerns and their unmet medical needs.

GENFIT's research programs have resulted in the creation of a rich and diversified pipeline of drug candidates at different stages of development, including GENFIT's lead proprietary compound, GFT505 that is currently in Phase IIb. With facilities in Lille, France, and Cambridge, MA (USA), the Company has approximately 80 employees. GENFIT is a public company listed on the Alternext trading market by Euronext™ Paris (Alternext: ALGFT; ISIN: FR0004163111). www.genfit.com

Contact GENFIT

Jean-François Mouney – CEO & Chairman of the Management Board

+333 2016 4000

MILESTONES – Press Relations

Bruno Arabian

+331 7544 8740 / +336 8788 4726

barabian@milestones.fr

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