István Greiner MSc. PhD. MBA
Deputy of Research Director Gedeon Richter Plc.

Abstract:

Gedeon Richter Plc. (www.richter.hu) has a long track back record regarding development of CNS active compounds. Two most successful products are vinpocetine and tolperisone, which are marketed even today by the company. As a continuation of this activity during the last 20 years company invested in NCE R&D heavily and from 2000 updated its structure and research strategy according to the newest requirements. But it did not mean that forget everything from the past. Knowledge generated previously had a big impact of the new start.

Due to the fact that the research of dopaminergic system was well established we tried to find a new active compound with a promise of therapeutic value. At the beginning focus was made on D3 receptors but further experiments revealed necessity of D2 as well. Reanalyzing all of our knowledge in chemistry and SAR on this field several new classes of compounds were identified as a source of potential development candidates. Well established and new approaches were used to analyse inherent pharmacokinetic and pharmacodynamic features of selected compounds. RGH-188 (INN: cariprazine) was finally selected for clinical development while other two relatives were nominated as back-ups. New and highly effective high scale synthetic process was also developed and used to produce materials for clinical trials.

Gedeon Richter Plc., as a medium size company is not dedicated to pursue a worldwide development alone. As a result of our partnering activity in year 2004 Mitsubishi Pharma Co. and later Forest Laboratories entered into two development agreements with the company for Asian and North American territories respectively. From that time the clinical activities were cross organised and included couple of PI and several PII studies, both having positive final outcomes. Due to these successes in human further clinical studies were started to investigate further therapeutic possibilities. Based on the presentation audience will be familiar with experiences gained during the R&D process of Cariprazine, a promising CNS active compound which is on the right track to be a successful product marketed worldwide.