Mitiglinide [KAD 1229, S 21403], a derivative of benzylsuccinic acid, is a potassium channel antagonist undergoing development with Kissei for the treatment of type 2 diabetes mellitus. It has potent oral hypoglycaemic activity and is structurally different from the sulphonylureas, although it stimulates calcium influx by binding to the suphonylurea receptor on pancreatic beta-cells and closing K+ATP channels. Mitiglinide belongs to a family of meglitinide analogues that also includes repaglinide and nateglinide. Mitiglinide is licensed to Servier for Europe, where it is undergoing phase III development, and for Russia, the Commonwealth of Independent States, the Baltic Republics, the Middle East, Oceania, China (including Hong Kong) and Taiwan. Kissei exclusively licensed mitiglinide to Choongwae Pharma for South Korea in March 2003. In August 2002, Kissei and Takeda entered into a co-marketing agreement for mitiglinide in Japan. The companies will co-market the agent under a single brand name. Mitiglinide was licensed to Purdue Pharma for the US, Canada, Mexico and Central and South America. However, Kissei and Purdue Pharma terminated their agreement in February 2001 following Purdue Pharma's decision to concentrate on core areas such as oncology and analgesics. Kissei's US subsidiary, Kissei Pharma US, is currently carrying on the ongoing phase II clinical development in the US. However, in its Annual Report 2003, Kissei announced that it is considering outlicensing mitiglinide for development in marketing in North America. Mitiglinide has been recommended for approval in Japan for the management of postprandial hyperglycaemia in patients with type 2 diabetes. Kissei is also conducting phase II/III clinical trials with a combination of mitiglinide and an alpha-glucosidase inhibitor (additional indication) in patients with type 2 diabetes in Japan. In the US, the agent is being evaluated in phase II clinical trials with Kissei Pharma USA. Mitiglinide is also undergoing a phase-III, 12-month, multicentre, randomised, double-blind study in a total of 710 patients in comparison with repaglinide for the treatment of type 2 diabetes. This study will be followed by a 12-month open-label treatment with mitiglinide alone or in combination therapy. Servier (Australia) conducted a randomised, double-blind, multicentre phase III study in Australia comparing mitiglinide with metformin or a combination of the two for the treatment of type 2 diabetes.