The efficacy and safety of the peripheral kappa agonist fedotozine was evaluated In a double-blind, multicenter study involving 238 patients with the irritable bowel syndrome. According to the investigators, the highest dose of fedotozine markedly reduced overall disease severity (P = 0.003) and the pain component of the symptomatic profile (P = 0.009). Clinical and laboratory safety was very good.1
In a randomized, double blind manner, the peripherally selective KOR agonist ADL 10-0101 or placebo was infused into six patients with chronic pancreatitis and ongoing abdominal pain despite mu-opioid agonist therapy. One patient receiving placebo and one receiving ADL 10-0101 experienced a mild headache during the study. One patient receiving ADL 10-0101 experienced restlessness and another had assymptomatic transient dysrhythmia upon standing after the 4 h study. Neither of the treatments affected blood pressure, heart rate, respiratory rate, or oxyhemoglobin saturation, and no patient experienced nausea during the study.2
In a study to evaluate the analgesic efficacy and safety of peripherally-restricted and highly selective kappa opioid receptor agonist CR845 when dosed preoperatively and postoperatively in women undergoing elective laparoscopic hysterectomy, the drug was found to be safe and well-tolerated when administered perioperatively, before and/or after surgery, and patients reported higher levels of satisfaction after being treated. The incidence of opioid-related treatment-emergent adverse events was lower in patients treated than in patients treated only with placebo.3
