tetomilast (OPC-6535) / Otsuka - LARVOL DELTA

Research progress of phosphodiesterase inhibitors in inflammatory bowel disease treatment. (PubMed, Zhejiang Da Xue Xue Bao Yi Xue Ban) - "In recent years, a series of researches suggest that PDE inhibitors such as several PDE4 inhibitors, PDE5 inhibitors (sildenafil, tadalafil and vardenafil), PDE3 inhibitors (cilostazol), PDE9 inhibitor (PF-04447943) and PDE3/PDE4 double inhibitor (pumafentrine) have ameliorating effect on experimental colitis in animals. In clinical trials, PDE4 inhibitor apremilast showed more therapeutic advantage than tetomilast. This article reviews the recent research progress of PDE inhibitors in treatment of inflammatory bowel disease."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease

A Dose-finding Study of OPC-6535 in Patients With Active Ulcerative Colitis (clinicaltrials.gov) - P2; N=43; Terminated; Sponsor: Otsuka Pharmaceutical Co., Ltd.; N=160 ➔ 43

Clinical • Enrollment change • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

A Dose-finding Study of OPC-6535 in Patients With Active Crohn's Disease (clinicaltrials.gov) - P2; N=29; Terminated; Sponsor: Otsuka Pharmaceutical Co., Ltd.; N=60 ➔ 29

Clinical • Enrollment change • Crohn's disease • Gastroenterology • Genetic Disorders • Immunology • Inflammatory Bowel Disease • CRP

Phosphodiesterase-4 inhibitors for chronic obstructive pulmonary disease. (PubMed, Cochrane Database Syst Rev) - "For this current update, five new studies from the 2020 search contributed to existing findings but made little impact on outcomes described in earlier versions of this review. PDE₄ inhibitors offered a small benefit over placebo in improving lung function and reducing the likelihood of exacerbations in people with COPD; however, they had little impact on quality of life or on symptoms. Gastrointestinal adverse effects and weight loss were common, and the likelihood of psychiatric symptoms was higher, with roflumilast 500 µg. The findings of this review provide cautious support for the use of PDE₄ inhibitors in COPD. In accordance with GOLD 2020 guidelines, they may have a place as add-on therapy for a subgroup of people with persistent symptoms or exacerbations despite optimal COPD management (e.g. people whose condition is not controlled by fixed-dose long-acting beta₂-agonist (LABA) and inhaled corticosteroid (ICS) combinations). More longer-term trials are..."

Journal • Review • Chronic Obstructive Pulmonary Disease • CNS Disorders • Dyspepsia • Immunology • Insomnia • Respiratory Diseases • Sleep Disorder • Tobacco Cessation

Phosphodiesterase inhibitors in inflammatory bowel disease (Expert Opin Investig Drugs) - Human studies have not been successful in showing significant superiority of PDE4Is in treatment of IBD; PDE7Is have shown synergistic effect with PDE4Is & they may act similar to PDE3Is in experimental settings; Sildenafil as the PDE5I has shown good effects in experimental colitis by balancing oxidant-antioxidant status; Although the present data about PDE superfamily & their specific roles in gastrointestinal tract is limited but inhibitors of PDE4, PDE5 & PDE7 seem good candidates as the next generation of effective drugs

Experimental data • Inflammatory Bowel Disease