asimadoline

Asimadoline is an orally administered, peripherally selective small molecule agonist of the kappa opioid receptor (KOR). It exhibits approximately 500-fold greater affinity for human kappa receptors compared to mu or delta opioid receptors. Due to its low penetration across the blood–brain barrier, asimadoline lacks central nervous system side effects typical of other KOR agonists. The drug was originally developed by Merck KGaA and later advanced by Tioga Pharmaceuticals for gastrointestinal indications. Asimadoline has been primarily investigated for the treatment of irritable bowel syndrome (IBS), where it demonstrated efficacy in reducing visceral pain and improving abnormal bowel function, particularly in diarrhea-predominant and alternating IBS subtypes. It has also been studied in functional dyspepsia and pruritus but has not received regulatory approval or reached the market[1][2][3][4][6][7].

Other names

asimadoline [INN]153205-46-0