XEN-D0501

XEN-D0501 is a selective, synthetic, orally active small molecule that acts as a potent antagonist of the transient receptor potential vanilloid 1 (TRPV1) receptor. It was originally developed by Xention and is currently being developed by Pila Pharma for the treatment of erythromelalgia, type 2 diabetes mellitus, and obesity. The drug has received orphan drug status in the United States for erythromelalgia. Mechanistically, it blocks TRPV1 channels involved in neurogenic inflammation and pain signaling pathways. Clinical studies have shown that XEN-D0501 enhances endogenous insulin response to oral glucose and reduces cardiovascular biomarkers such as ANP in people with type 2 diabetes and obesity. Development for overactive bladder and cough has been discontinued due to lack of efficacy or safety concerns[3][4][7][8].

Other names

Ion channel modulator 1 (overactive bladder)TRPV1 antagonist (overactive bladder)VR1 antagonist (overactive bladder)Vanilloid receptor-1 antagonist (overactive bladder)