Division of Hepatology and Pancreatology, Department of Internal Medicine, Aichi Medical University, Nagakute, Aichi 480-1195, Japan.
Department of Internal Medicine, Institute of Gastroenterology, Tokyo Women's Medical University, Tokyo 162-8666, Japan.
Int J Mol Sci. 2020 Mar 11;21(6):1907. doi: 10.3390/ijms21061907.
Liver-related diseases are the third-leading causes (9.3%) of mortality in type 2 diabetes (T2D) in Japan. T2D is closely associated with nonalcoholic fatty liver disease (NAFLD), which is the most prevalent chronic liver disease worldwide. Nonalcoholic steatohepatitis (NASH), a severe form of NAFLD, can lead to hepatocellular carcinoma (HCC) and hepatic failure. No pharmacotherapies are established for NASH patients with T2D. Though vitamin E is established as a first-line agent for NASH without T2D, its efficacy for NASH with T2D recently failed to be proven. The effects of pioglitazone on NASH histology with T2D have extensively been established, but several concerns exist, such as body weight gain, fluid retention, cancer incidence, and bone fracture. Glucagon-like peptide 1 (GLP-1) receptor agonists and sodium-glucose cotransporter 2 (SGLT2) inhibitors are expected to ameliorate NASH and NAFLD (LEAN study, LEAD trial, and E-LIFT study). Among a variety of SGLT2 inhibitors, dapagliflozin has already entered the phase 3 trial (DEAN study). A key clinical need is to determine the kinds of antidiabetic drugs that are the most appropriate for the treatment of NASH to prevent the progression of hepatic fibrosis, resulting in HCC or liver-related mortality without increasing the risk of cardiovascular or renal events. Combination therapies, such as glucagon receptor agonist/GLP-1 or gastrointestinal peptide/GLP-1, are under development. This review focused on antidiabetic agents and future perspectives on the view of the treatment of NAFLD with T2D.
在日本,2 型糖尿病(T2D)患者的第三大死因(9.3%)与肝脏相关疾病有关。T2D 与非酒精性脂肪性肝病(NAFLD)密切相关,后者是全球最常见的慢性肝脏疾病。非酒精性脂肪性肝炎(NASH)是一种严重的 NAFLD 形式,可导致肝细胞癌(HCC)和肝功能衰竭。目前尚无针对 T2D 伴 NASH 患者的药物治疗方法。尽管维生素 E 已被确立为无 T2D 的 NASH 的一线药物,但最近其对 T2D 伴 NASH 的疗效未能得到证实。吡格列酮对 T2D 伴 NASH 的组织学影响已得到广泛证实,但仍存在一些问题,如体重增加、体液潴留、癌症发病率和骨折。胰高血糖素样肽 1(GLP-1)受体激动剂和钠-葡萄糖共转运蛋白 2(SGLT2)抑制剂有望改善 NASH 和 NAFLD(LEAN 研究、LEAD 试验和 E-LIFT 研究)。在各种 SGLT2 抑制剂中,达格列净已进入 3 期临床试验(DEAN 研究)。一个关键的临床需求是确定最适合治疗 NASH 的抗糖尿病药物,以防止肝纤维化进展,从而导致 HCC 或与肝脏相关的死亡率,而不会增加心血管或肾脏事件的风险。联合治疗,如胰高血糖素受体激动剂/GLP-1 或胃肠肽/GLP-1,正在开发中。本文重点介绍了抗糖尿病药物,并对 T2D 伴 NAFLD 的治疗观点进行了展望。