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Piramal’s NCE research releases preclinical efficacy data for two promising molecules

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Piramal Life Sciences – NCE Research, a division of Piramal Enterprises Ltd (PEL), made poster presentations for drugs in early clinical development for metabolic disorders in two different sessions of the 74th Scientific Session of the American Diabetes Association (ADA) in San Francisco, California, US. The presentations covered Piramal’s clinical stage GRP40 agonist, P11187 and Piramal’s clinical stage DGAT1 inhibitor P7435.

GPR40 is a G-protein coupled receptor highly expressed in pancreatic beta cells of humans and rodents. It stimulates insulin-secretion when activated by a free fatty acid under elevated glucose concentrations in the blood. Diacylglycerol acyltransferase (DGAT) is an enzyme catalyzes the final step of triglyceride formation from diacylglycerol and Acyl-CoA. A surplus accumulation of triglycerides in tissues and blood can lead to a range of medical conditions such as severe obesity, insulin resistance, hepatic steatosis, and cardiovascular disease. Therefore, inhibition of triglyceride synthesis has a strong therapeutic rational for treatment of such disorders. P7435 is a potent, selective oral DGAT1 inhibitor, aimed at fulfilling unmet medical needs in hypertriglyceridemia, and combined dyslipidemia.

Overall, P11187 has demonstrated glucose-stimulated insulin secretion and anti-hyperglycemic potential in rodent models of type 2 diabetes with excellent safety profile. The drug is currently being tested in phase I trial in the US.

Dr Owe Orwar, President, Piramal Life Sciences-NCE Research stated, “P11187 is an intelligent oral anti-diabetic investigational drug that evokes insulin release in a glucose and Free Fatty Acid (FFA) dependent fashion. This means, the higher the glucose and free fatty acid concentration in the plasma, the better it may work. For glucose control, this has been corroborated by the phase III study in type-II diabetes mellitus with the investigational drug, Fasiligam (TAK-875), which was the leading molecule in the class until it failed due to hepatotoxicity in December 2013. We have done extensive work to de-risk our asset for this liability, and will shortly be initiating our Multiple Ascending Dose (MAD) portion of our Phase- I trial in type-II diabetics.”

He further continued, “P7435 appears to be one of the safest DGAT1 inhibitors thus far, showing potent triglyceride-lowering potential. We are well on our way to concluding a Phase I in trial in the US the next few months and are looking forward to evaluating this molecule further in clinic and exploit its potential in hypertriglyceridemia, and combined dyslipidemia as well as in type 2 diabetes.

EP News Bureau- Mumbai

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