minesapride (DSP-6952) / Sumitomo Pharma - LARVOL DELTA

Pharmacokinetics, safety and metabolite profiling of minesapride, a novel 5-HT receptor partial agonist, in healthy elderly and young subjects. (PubMed, Drug Metab Pharmacokinet) - "No major metabolites exceeded 10% of unchanged minesapride, and results of the in vitro study suggested that there were no human-specific metabolites. From the viewpoints of PK and metabolite profiling, no dose adjustment of minesapride is warranted in elderly population without renal or hepatic impairment."

Clinical • Journal • PK/PD data • Constipation • Gastroenterology • Gastrointestinal Disorder • Immunology

Randomised clinical trial: minesapride vs placebo for irritable bowel syndrome with predominant constipation. (PubMed, Aliment Pharmacol Ther) - "Minesapride was safe and well-tolerated. Although the primary endpoint was negative, minesapride 40 mg is likely to improve the stricter composite endpoint and SBM frequency. Japan Pharmaceutical Information Center Number: Japic CTI-163459."

Clinical • Journal • Constipation • Immunology • Pain

Editorial: minesapride for irritable bowel syndrome with constipation. (PubMed, Aliment Pharmacol Ther) - No abstract available

Journal • Constipation • Gastroenterology • Gastrointestinal Disorder • Immunology

Editorial: minesapride for irritable bowel syndrome with constipation-authors' reply. (PubMed, Aliment Pharmacol Ther) - No abstract available

Journal • Constipation • Gastroenterology • Gastrointestinal Disorder • Immunology

"Study: DSP-6952 effective in IBS-C https://t.co/LvbX7jL6Ce @AmCollegeGastro" (@SWexner)

Efficacy and Safety of 5-HT4 Receptor Agonist Minesapride for Irritable Bowel Syndrome with Constipation in a Randomized Controlled Trial. (PubMed, Clin Gastroenterol Hepatol) - "In a phase 2 trial of patients with IBS-C in Japan, minesapride increased stool frequency (measured by CSBMs), reduced abdominal and overall IBS-C symptoms, and was well tolerated. Japan Pharmaceutical Information Center trial no: JapicCTI-122041."

Clinical • Journal

Thorough QT/QTc Study Shows That a Novel 5-HT Receptor Partial Agonist Minesapride Has No Effect on QT Prolongation. (PubMed, Clin Pharmacol Drug Dev) - "This was a randomized, placebo-controlled, 4-arm, 4-period, crossover study conducted in healthy adults, with administration of single oral doses of minesapride (40 mg and 120 mg), placebo, and moxifloxacin in the fasted state. Japanese subjects (48 total: 24 males and 24 females) were randomized, and 47 subjects completed all treatment periods. A review of other electrocardiographic data revealed that neither therapeutic (40 mg) nor supratherapeutic (120 mg) doses of minesapride were associated with increased risk of prolonged QT interval."

Journal

A 3-Part Phase 1 Study to Investigate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of DSP-6952 in Healthy Japanese Subjects and Those With ≤3 Spontaneous Bowel Movements per Week. (PubMed, Clin Pharmacol Drug Dev) - "In subjects with spontaneous bowel movements ≤3 times/wk, the median change in the frequency of bowel movements from baseline increased, although the difference did not reach statistical significance. DSP-6952 was well tolerated at single and multiple doses up to 120 mg/d, with a linear pharmacokinetic profile among all subjects."

Clinical • Journal • P1 data • PK/PD data