CYP26B1 inhibitors for oral administration

Purpose and goal

Around 600 million people suffer from acne. Current treatment with externally supplied Vitamin A has several adverse effects, including teratogenicity. The market asks for pharmaceuticals with new modes of action. Our compound restores the levels of Vitamin A in the tissue by inhibiting the enzyme CYP26B1. The analoges that have been developed during last year have the potential to be utilized through different means of administration, and have in a range of tests shown very benign results.

Expected results and effects

We have conducted synthetic design, developed analogous compounds, scaled up synthesis and performed various tests. We have benchmarked against competing substances. Our compounds are designed to target CYP26B1, which is up-regulated in skin disorders such as acne. The tests have shown very positive data on a range of parameters for drug candidates, which enables us to take the next step in the development of our compounds, and opens for dialoges with investors and pharmaceutical industry.

Planned approach and implementation

Based on earlier vitrual screening, synthetic design and know-how, analoges of CYP26B1 inhibitors were synthesized, scaled up, and tested in enzymatic assays and ADMET profiling. BeePCo and LIOS were hired for chemistry, and CROs HepaPredict, Eurofins and ADMEYT AB for tests. Some delays arose due to late delivery of reagents and feedback from consultants, but the project could nonetheless be performed as planned and has generated very promising data for the next steps in the drug development process.