Drug Discovery

Phenex uses its technology and its in-depth knowledge of Nuclear Receptor biology not only for drug discovery services, but also for its own drug discovery programs.

The company is currently engaged in three proprietary drug discovery programs on the emerging drug targets FXR, LXR and ERRα.

 

FXR Program

FXR (NR1H4, synonyms: BAR = bile acid receptor) is proposed to be a nuclear bile acid sensor. As a result, it modulates both, the synthetic output of bile acids in the liver and their recycling in the intestine (by regulating bile acid binding proteins). But beyond bile acid physiology, FXR seems to be involved in the regulation of many diverse physiological processes which are relevant in the etiology of and for the treatment of diseases as diverse as cholesterol gallstones, metabolic disorders such as Type II Diabetes, dyslipidemias or obesity, chronic inflammatory diseases such as Inflammatory Bowel Diseases or chronic intrahepatic forms of cholestasis.

Phenex focuses in its program on the discovery of novel proprietary FXR agonists with anti-diabetic properties. FXR is well suited as a drug target for orally available small molecular Type II Diabetes drugs because

1. It binds natural small molecule ligands (bile acids).

2. Activation of FXR increases insulin sensitivity, lowers triglycerides, increases liver glycogen and potentially reduces body weight in relevant animal models.

3. FXR shows no obvious liability as compared to other oral insulin sensitizers such as PPARγ (Rosi- and Pioglitazone) or dual PPARα/PPARγ targeted drugs (e.g."Glitazars").

Phenex has filed several patent applications on novel chemical matter and was already granted some patents in this field. The project is at preclinical proof-of-concept stage.