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Novel PAR1 Antagonist Has Promising Results in Early IC Study

Monjotin N, Gillespie J, Farrie M, Le Grand B, Junquero D, Vergnolle N. F16357, a novel PAR1 antagonist improves urodynamic parameters in a rat model of Interstitial Cystitis. Br J Pharmacol. 2016 Apr 25. doi: 10.1111/bph.13501. [Epub ahead of print]

Researchers in this preclinical study sought to characterize the potential benefits of F16357, a novel agent that may have anti-inflammatory effects or other potential benefits in the setting of interstitial cystitis (IC). The agent is one of a class of several agents, known as PAR1 antagonists, that are under investigation in preclinical studies for a variety of conditions. To test F16357, the researchers delivered the compound directly to bladder of rats with an induced form of IC. After exposure to the compound, the rats were found to be virtually free of any damage to the bladder lining. The level of immune reaction to PAR1 was no higher in the bladder tissue of the IC-induced rats than in normal rat bladder tissue. Furthermore, F16357 seemed to block an increase of urine production and voiding frequency. Based on these early but promising results, investigators from this trial think F16357 could be an interesting candidate for further evaluation as treatment for IC.