贾纳斯激酶
特应性皮炎
皮肤病科
化学
临床试验
病因学
药理学
激酶
医学
内科学
生物化学
作者
Satoru Noji,Yoshinori Hara,Tomoya Miura,Hiroshi Yamanaka,Kazuyuki Maeda,Akimi Hori,Hiroshi Yamamoto,Shingo Obika,Masafumi Inoue,Yasunori Hase,Tadashi Orita,Satoki Doi,Tsutomu Adachi,Atsuo Tanimoto,Chika Oki,Yukari Kimoto,Yoshihiro Ogawa,Tamotsu Negoro,Harukichi Hashimoto,Makoto Shiozaki
标识
DOI:10.1021/acs.jmedchem.0c00450
摘要
Dermatologic disorders such as atopic dermatitis arise from genetic and environmental causes and are complex and multifactorial in nature. Among possible risk factors, aberrant immunological reactions are one of the leading etiologies. Immunosuppressive agents including topical steroids are common treatments for these disorders. Despite their reliability in clinical settings, topical steroids display side effects, typified by skin thinning. Accordingly, there is a need for alternate effective and well-tolerated therapies. As part of our efforts to investigate new immunomodulators, we have developed a series of JAK inhibitors, which incorporate novel three-dimensional spiro motifs and unexpectedly possess both excellent physicochemical properties and antidermatitis efficacy in the animal models. One of these compounds, JTE-052 (ent-60), also known as delgocitinib, has been shown to be effective and well-tolerated in human clinical trials and has recently been approved in Japan for the treatment of atopic dermatitis as the first drug among Janus kinase inhibitors.
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