Patent Evaluation: Tri-arginine insulins and their potential in the treatment of diabetes

Summary

Novelty: Novel forms of tri-arginine insulins are disclosed. It is proposed that they can be formulated as a solution (to pH 6.1) and have prolonged hypoglycaemic activity. They are stated to have potential utility for treatment of diabetes.

Biology: An in vivo rabbit study evaluating activity of the tri-arginine insulins is described. Animals were given a subcutaneous dose of 0.2U/kg. Blood samples were then taken periodically and analysed for glucose content. Test agents were found to give 45-85% of original blood glucose levels (at time zero) one hour post-injection.

Chemistry: Insulins of the disclosure have the formula specified. The most preferred compounds are those where X is Asn, Y is His and Z is Asn. Full preparative details, using enzymatic methods, are presented.