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.


CONCLUSIONS
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.


CONCLUSIONS
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.
Retterstøl
Kjetil
K
Rikshospitalet-Oslo University Hospital, Lipid Clinic, Medical Department, 0027 Oslo, Norway. kjetil.retterstol@rikshospitalet.no
D000818:Animals; D001786:Blood Glucose / Q000032:analysis; D001835:Body Weight / Q000187:drug effects; D017326:Clinical Trials, Phase III as Topic; D003924:Diabetes Mellitus, Type 2 / Q000097:blood / Q000188:drug therapy* / Q000378:metabolism; D052216:Glucagon-Like Peptide 1 / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D000067757:Glucagon-Like Peptide-1 Receptor; D006442:Glycated Hemoglobin / Q000032:analysis; D006801:Humans; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D050417:Insulin-Secreting Cells / Q000187:drug effects; D010446:Peptide Fragments / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D010455:Peptides / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D016032:Randomized Controlled Trials as Topic; D018027:Receptors, Glucagon / Q000819:agonists*; D016896:Treatment Outcome; D014280:Triglycerides / Q000097:blood
D001786:Blood Glucose; D052216:Glucagon-Like Peptide 1; D000067757:Glucagon-Like Peptide-1 Receptor; D006442:Glycated Hemoglobin; D007004:Hypoglycemic Agents; D010446:Peptide Fragments; D010455:Peptides; D018027:Receptors, Glucagon; D014280:Triglycerides; C000593833:GLP1R protein, human; C517652:hemoglobin A1c protein, human; C055453:glucagon-like peptide 1 (7-36)amide; C541736:taspoglutide