Taspoglutide: a long acting human glucagon-like polypeptide-1 analogue

Background: Taspoglutide (R1583/BIM51077) is a new anti diabetic drug from Hoffmann-La Roche. The compound is to be administered as a subcutaneous injection once weekly and is also effective given bi-weekly. It is a long acting 10% formulation of (Aib 8-35) human glucagon-like polypeptide-1 (7 - 36 amides) with 93% homology with the native polypeptide. It activates the glucagon-like polypeptide-1 receptor. Phase III trials are currently in process.

Objective: To provide a critical review of taspoglutide based on available published data.

Methods: Information provided from the search on Internet has been reviewed. A clinical interpretation is given on a background of practical experience as an investigator in a clinical trial with taspoglutide.

Results: Search on PubMed, EMBASE and Google gave hits on six clinical studies investigating taspoglutide of which the largest accounted for > 50% of the total study population. In addition, some animal studies were identified. Significant improvement on glucose control as well as several metabolic parameters has been shown with taspoglutide.

Discussion: Data from the clinical trials are interpreted in a medical context. The prospects of taspoglutide in the treatment of diabetes type 2 and metabolic syndrome are discussed.

Conclusion: Taspoglutide is a new activator of the glucagon-like polypeptide-1 receptor. It is effective when injected once weekly and less effective when injected bi-weekly. In addition to its anti diabetic properties, taspoglutide has favorable effects on body weight and significantly reduces three of five diagnostic criteria for metabolic syndrome, namely glucose, waist circumference and fasting triglyceride.