Lixisenatide (Lyxumia®)



Lixisenatide (Lyxumia®)

Lixisenatide (ZP10, AVE0010) is a glucagon-like peptide 1 (GLP-1) receptor agonist that incorporates Zealand Pharma’s SIP®-technology and is targeted to treat Type 2 diabetes. Lyxumia® is the intended trademark for lixisenatide. Lixisenatide is not currently approved or licensed anywhere in the world.

Endogenous GLP-1 is released from the small intestine in response to food intake and stimulates insulin liberation from the pancreas when blood sugar levels are elevated. In addition, GLP-1 suppresses the production of glucagon (a hormone that stimulates release of stored sugar from the liver into the bloodstream) which also contributes to the normalization of blood glucose.  Furthermore, GLP-1 delays gastric emptying and reduces appetite which are considered important effects for the lowering of body weight that has been observed consistently with this new class of drugs.  Importantly, GLP-1 only stimulates the liberation of insulin when blood glucose levels are elevated, while it is devoid of activity when blood glucose is normal or low.  This mechanism explains the low risk of hypoglycemia (low blood glucose levels) during treatment with GLP-1 agonists. 

GLP-1 receptor agonists like Lixisenatide normalize elevated blood sugar by enhancing insulin secretion until blood sugar levels approach normal concentration.  This mode of action combines high anti-diabetic efficacy with low risk of hypoglycemia (insulin shock).

In June 2003, ZP10 was out-licensed to sanofi on a global basis. Sanofi is responsible for all further clinical development.

There are two programs being developed through the partnership with sanofi. The most advanced program, which involves the use of lixisenatide as a monotherapy, is in late Phase III testing and has reported encouraging initial Phase III results. The second most advanced program involves a combination of lixisenatide and sanofi's Lantus® (insulin glargine), a once-daily, long-acting insulin analog; a complete Phase III development program is being finalized, and initial Phase III clinical trial results for lixisenatide administered in "free combination" with Lantus® were announced in September 2010

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