Carotegrast-methyl (brand name: CAROGRA((R)) Tablets) is a new chemical entity created by Ajinomoto Pharmaceuticals Co., Ltd. (currently EA Pharma Co., Ltd.) as an alpha4 integrin inhibitor. In vivo, it exerts an anti-inflammatory effect by inhibiting the functions of both alpha4beta1 integrin and alpha4beta7 integrin expressed on the surface of inflammatory cells such as lymphocytes. Under the joint development of EA Pharma Co., Ltd. and Kissei Pharmaceutical Co., Ltd., the efficacy and safety of carotegrast methyl were confirmed in patients with moderate active ulcerative colitis. Carotegrast-methyl, the Japan-originated, world-first orally available alpha4 integrin antagonist, was approved in March and launched in May 2022 in Japan. Patients who had inadequate response or intolerance to the basic treatment with 5-ASA preparations for ulcerative colitis, have widely desired an orally available treatment with the new mechanism of actions. Carotegrast methyl can be a treatment option that meets that unmet medical need and has the potential to greatly contribute to the treatment of ulcerative colitis based on the thorough practice of proper use. This article mainly introduces the pharmacological properties and clinical trial results of carotegrast methyl.