Cortecs is developing Macrulin, a Macrosol system for the oral delivery of insulin, for the potential treatment of non-insulin dependent diabetes. The compound is in phase II clinical development [272442], [276928]. Final analysis of results from a phase IIa study of Macrulin in type II diabetic patients showed a dose-related decline in blood glucose after administration of oral insulin, accompanied by increases in the serum insulin levels. No episodes of hypoglycemia occurred even at the highest dose [272442]. The first stage of the phase I study was in six volunteers in a placebo-controlled crossover trial. The fasting healthy volunteers were dosed with Macrulin via a tube into the small intestine. At a dose of 200 IU, plasma insulin levels were higher than those observed after administration of a placebo. The second stage used the same model, but optimized conditions by testing the six healthy volunteers after a glucose load. Final results, presented at the Controlled Release Society XXIV Symposium on Controlled Release of Bioactive Materials, showed that Macrulin significantly increased mean insulin levels and decreased mean glucose levels in the blood [255766]. In June 1996, Cortecs announced that it had entered an agreement with Osteometer Biotech and with the Center for Clinical and Basic Research (CCBR) for the clinical development of the oral formulation [211943]. Nomura analysts predict that the formulation should be launched in 2000, and that the potential market could peak at STG 200 million [198488].
