Inflammation

Prostiazol

Researchers at Avidin have synthesized analogues of a novel prostaglandin with strong anti-inflammatory effects. Avidin is looking for partners for out-licensing/co-development/repurposing to other inflammatory diseases.

Chemistry Prostiazol is a semi-synthetic derivative of a naturally occurring prostaglandin derivate. The synthesis of the prostaglandin intermediate was quite long (22 chemical steps) but has been optimized (at present only 13 steps are needed). The full Prostiazol synthesis was optimized and in parallel the scale-up of the process to multi-hundred gram scale has been started. Avidin’s collaborator, Ubichem has the development and manufacturing capabilities to cover the chemistry development requirement during the preclinical and clinical development phase of the project and manufacture Prostiazol for the preclinical and clinical work under non-GMP and cGMP conditions.

Preclinical Results Prostiazol, the lead prostaglandin compound exerts strong anti-inflammatory action in vivo at very low doses (0.5-2 mg/kg). Its formulated form is orally active in vivo in IBD rat model at 1-2 mg/kg dose. Acute toxicology in mouse showed that Prostiazol is non-toxic up-to 60 mg/kg dose i.v. and up-to 200 mg/kg dose orally.

Market overview Gastrointestinal tract disorders and different forms of arthritis are a prominent component in the overall disease burden of the world’s most developed economies, and a lack of effective long-term treatments and limited etiological understanding is continuing to exacerbate the impact of such conditions. The global market for IBD drugs exceeded $5bn in 2009, with strong growth from the previous year. It is expected that the overall market for IBD drugs will expand from 2010 onwards.

IP position Avidin and Ubichem jointly submitted a patent for the therapeutic application of prostaglandin derivatives, as new compounds. Patent submitted in Hungary in June 2010, then PCT submission was initiated in July 2011. The basic prostaglandin was patented to use it in inflammatory diseases, while prostaglandin derivatives were patented as NCEs to use them in inflammatory diseases.