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Study aim: To prepare and evaluate CCK gastrin antagonists PNB-001 for a first in man clinical trial and to provide preclinical formulations, which can be used in later clinical studies. Methods: In vivo assay in rats, isolated tissue preparations, solid dosage forms, PK analysis to evaluate the anti-inflammatory analgesic PNB-001. Results: The arylated 5-hydroxy–pyrrol-2-one PNB-001 was prepared in 3 synthetic steps from furfural. The selective CCK2antagonist (PNB-001, IC50= 22nM) was fully evaluated to design a clinical trial. In vivo evaluation revealed analgesic activity for the gastrin CCK2 antagonist PNB-001 in the tail immersion test at a dose range by IP and oral administration. Plasma concentrations were analysed in rats and in vitro it was shown, that these concentrations, are efficient in vitro using isolated tissue preparations. Solid formulations were prepared and tested active in rats. Conclusion: From bench side to bed side, the preclinical development for PNB-001 is completed and data formed the foundations for a first in man trial, phase 1.

Pre-Clinical Evaluation of CCK2 Antagonist PNB-001 (4-Chloro-5-Hydroxy1-Phenylethyl-5-Phenyl-1,5-Dihydro-Pyrrol-2-One) Towards The Design For A First-In-Man Clinical Trial