Tolimidone (CP-26154; MLR-1023) is a compound which was discovered by scientists at

Pfizer Pfizer Inc. ( ) is an American multinational pharmaceutical and biotechnology corporation headquartered on 42nd Street in Manhattan, New York City. The company was established in 1849 in New York by two German entrepreneurs, Charles Pfizer ...

, was found to stimulate secretion of

gastric mucosa The gastric mucosa is the mucous membrane layer of the stomach, which contains the glands and the gastric pits. In humans, it is about 1 mm thick, and its surface is smooth, soft, and velvety. It consists of simple columnar epithelium, lamin ...

, and was in development by Pfizer as a drug candidate to treat

gastric ulcers Peptic ulcer disease (PUD) is a break in the inner lining of the stomach, the first part of the small intestine, or sometimes the lower esophagus. An ulcer in the stomach is called a gastric ulcer, while one in the first part of the intestines i ...

but was abandoned. After the patent on the compound expired, scientists at the company

Melior Discovery Melior Discovery, Inc. is a private biopharmaceutical company based in Exton, Pennsylvania, USA. The company specializes in drug repositioning and has established a proprietary phenotypic screening platform that it uses for this purpose. Melior a ...

identified it as a potential drug candidate for diabetes through a

phenotypic screen In genetics, the phenotype () is the set of observable characteristics or traits of an organism. The term covers the organism's morphology or physical form and structure, its developmental processes, its biochemical and physiological proper ...

. The company proceeded to show that MLR-1023 is an allosteric activator of Lyn kinase with an EC50 of 63 nM. As of 2012 Melior was

repurposing Repurposing is the process by which an object with one use value is transformed or redeployed as an object with an alternative use value. Description Repurposing is as old as human civilization, with many contemporary scholars investigating tha ...

it for diabetes. In June 2016, the company reported positive results from their Phase 2a clinical study in diabetic subjects

References

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