Nippon rinsho. Japanese journal of clinical medicine 2001-11-01

[KRP-297, MCC-555].

T Yamanouchi

Index: Nihon Rinsho. 59(11) , 2200-6, (2001)

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Abstract

KRP-297 and MCC-555, which are being developed in Japan as thiazolidinediones, uniquely bind and activate peroxisome proliferator-activated receptors(PPAR). KRP-297, unlike other thiazolidinediones, effects on not only PPAR gamma but also PPAR alpha. Furthermore, this compound acts directly on basal glucose uptake in the rat skeletal muscle. KRP-297 decreased plasma glucose and insulin levels, and also blood triglyceride and free fatty acid in diabetic animal models. MCC-555 has significant antidiabetic properties yet its binding affinity for PPAR gamma is less than 1/10 that of BRL 49653. Thus, it is regarded now as a PPAR gamma modulator rather than agonist, depending on cell type. At present, clinical phase II studies of both drugs are under way.