STEP7

Serotonergic analgesic therapy based on 5-HT7 receptor agonist (STEP7)

The aim of the project STEP7 is the development of a first-in-class 5-HT7 receptor agonist and its clinical evaluation as neuropathic pain therapy. Neuropathic pain is a serious clinical issue and huge socio-economic burden. The project will be implemented by a scientific consortium consisting of the pharmaceutical company Celon Pharma S.A. and the Maj Institute of Pharmacology PAS.

The project is based on results obtained for the AGH-194 compound (patent no. EP16461543). Preliminary in vitro experiments have shown very promising properties: high activity towards 5-HT7 receptor, high selectivity, good water solubility. Results from in vivo models indicated satisfactory bioavailability after oral administration in mice, strong and fast penetration from blood to brain as well as a strong analgesic effect of AGH-194. The project will be conducted for 49 months in 9 stages. The first 8 stages will consist of industrial research, i.e. physicochemical characterization of the compounds, ADMET, in vitro and in vivo activity studies, efficacy tests and exclusion of nonspecific mechanisms of action. Based on acquired results, the decision regarding further development of AGH-194 or the selection of a new lead compound will be made based on obtained results for lead and back-up compounds. In the next stages, formulation development for the lead compound, scale-up and synthesis of compounds in GMP standard and toxicological studies will be conducted. Development stages will consist of Phase I and IIa clinical trials in patients with neuropathic pain of various ethiologies. The successful finish of the STEP7 project will give the opportunity to commence Phase III studies, and in the case of success, to introduce an innovative neuropathic pain therapy to the market, based on a completely novel pharmaceutical drug.

Management team:

Manager

Mikołaj Matłoka (Celon Pharma)

Coordinator

Prof. Małgorzata Filip

R&D

Prof. Andrzej J. Bojarski

Main Executor

Adam S. Hogendorf, PhD

Executors in MedChem Team

Beata Duszyńska, PhD

Agata Hogendorf, Msc

Katarzyna Kaczorowska, Msc

Grzegorz Satała, PhD

Ryszard Bugno, PhD

Tomasz Lenda, Msc

Aneta Kozioł,

Krystyna Nędza.

The study is supported by a grant Szybka Ścieżka POIR.01.01.01-00-0887/19 financed by the National Centre for Research and Development.