生物活性

• 描述Mitiglinide Calcium is a drug for the treatment of type 2 diabetes; it is a highly selective KATP channel antagonist. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) (KATP) channels in pancreatic beta-cells, and its early insulin release and short duration of action would be effective in improving postprandial hyperglycemia. Mitiglinide shows a higher selectivity for the beta-cell type of SUR1/Kir6.2 than the cardiac and smooth muscle types of K(ATP) channels in comparison with glibenclamide and glimepiride. Insulinotropic effect of mitiglinide is more potent than that of nateglinide, and mitiglinide surpassed in controlling postprandial hyperglycemia in normal and diabetic animals. In clinical trials, treatment with mitiglinide provided lasting improvement of postprandial hyperglycemia in Type 2 diabetic patients and decreased the fasting plasma glucose levels and HbA(1C) values^[3]. Mitiglinide induces vasorelaxation via activation of Kv channels and SERCA (sarcoplasmic/endoplasmic reticulum Ca2+-ATPase) pump. However, the vasorelaxant effects of mitiglinide did not involve other K+ channels, Ca2+ channels, PKA/PKG signaling pathways, or the endothelium^[4].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01456130	Diabetes Mellitus	Phase 3	Completed	-	Japan ... more >> Nagoya-shi, Aichi, Japan Fukuoka-shi, Fukuoka, Japan Kurume-shi, Fukuoka, Japan Sapporo-shi, Hokkaido, Japan Kobe-shi, Hyogo, Japan Kagoshima-shi, Kagoshima, Japan Kumamoto-shi, Kumamoto, Japan Osaki-shi, Miyagi, Japan Minou-shi, Osaka, Japan Osaka-shi, Osaka, Japan Kamio-shi, Saitama, Japan Koshigaya-shi, Saitama, Japan Adachi-ku, Tokyo, Japan Chuo-ku, Tokyo, Japan Collapse <<
  NCT01456130	-	-	Completed	-	-
  NCT01403818	Healthy Pharm... more >>acokinetics of ASP1941 Pharmacokinetics of Mitiglinide Collapse <<	Phase 1	Completed	-	Japan ... more >> Kantou, Japan Collapse <<

• 参考文献

• [1] Arao T, Okada Y, et al. Comparison Between Effectiveness of 100 mg/day Sitagliptin and a Switch to Mitiglinide Calcium Hydrate/Voglibose from 50 mg/day Sitagliptin in Patients with Type 2 Diabetes. J UOEH. 2017;39(1):1-9.

  [2] Mogami H, Shibata H, et al. Inhibition of ATP-sensitive K+ channel by a non-sulfonylurea compound KAD-1229 in a pancreatic beta-cell line, MIN 6 cell. Eur J Pharmacol. 1994 Nov 15;269(3):293-8.

  [3] Ojima K, Kiyono Y, Kojima M. Nihon Yakurigaku Zasshi. 2004;124(4):245-255

  [4] Li H, Kim HW, Shin SE, et al. The vasorelaxant effect of mitiglinide via activation of voltage-dependent K+ channels and SERCA pump in aortic smooth muscle. Life Sci. 2017;188:1-9