Our Pipeline MLR 1023 (type II diabetes)

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The company's most advanced program is focused on the development of MLR-1023, a previously evaluated, clinical-stage drug candidate. Melior has identified a new therapeutic use for this compound in the treatment of Type II diabetes. MLR-1023 compares favorably to both approved drugs and development stage candidates for diabetes.

MLR-1023 is a potential “next-generation” insulin sensitizer that works independently of a PPAR mechanism. The compound improves glycemic control by directly and selectively activating the enzyme Lyn kinase. Lyn kinase has previously been shown to modulate the insulin-signaling pathway. Indeed, the extrapancratic glycemic control activity of glimepiride (Amaryl^®) is mediated through a non-specific and indirect Lyn kinase activation. Therefore, MLR-1023 is the first described specific and direct activator of Lyn kinase that elicits glycemic control activity through potentiation of insulin activity.  

In animal models, MLR-1023 demonstrates equivalent efficacy to metformin (Glucophage) at a lower dose. In addition, the pre-clinical side-effect profile of MLR-1023 compares favorably to approved drugs. MLR-1023 is orally bioavailable (unlike GLP-1 inhibitors and insulin, which must be administered by injection), does not produce weight gain (in contrast to the glitazones/ thiazolidenediones and sulphonylurea classes of drugs) and does not produce hypoglycemia (in contrast to insulin and the sulphnylureas).  

More than 150 million people worldwide have diabetes, with approximately 90% suffering from Type II diabetes. An estimated 16 million people in the United States suffer from Type II diabetes, which is often part of a metabolic syndrome that includes obesity, elevated blood pressure and high levels of blood lipids. About 80% of people with Type II diabetes mellitus are overweight.

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