Le medicament du mois. Bydureon: premier agoniste des recepteurs du GLP-1 en une injection hebdomadaire (exenatide a liberation prolongee). ; Bydureon: first once weekly GLP-1 receptor agonist (exenatide LAR)
peer reviewed ; Bydureon is a new galenic formulation (long-acting release) of exenatide, the first agonist of Glucagon-Like Peptide-1 (GLP-1) receptors having been commercialized for the management of type 2 diabetes. The microsphere technology permits a prolonged absorption of exenatide from the subcutaneous depot, which allows one injection per week instead of two injections per day with the initial formulation of exenatide (Byetta). The clinical development programme DURATION showed that exenatide 2 mg once weekly more markedly reduces glycated haemoglobin (HbA(1c)), with a similar weight... Mehr ...
peer reviewed ; Bydureon is a new galenic formulation (long-acting release) of exenatide, the first agonist of Glucagon-Like Peptide-1 (GLP-1) receptors having been commercialized for the management of type 2 diabetes. The microsphere technology permits a prolonged absorption of exenatide from the subcutaneous depot, which allows one injection per week instead of two injections per day with the initial formulation of exenatide (Byetta). The clinical development programme DURATION showed that exenatide 2 mg once weekly more markedly reduces glycated haemoglobin (HbA(1c)), with a similar weight loss but a better digestive tolerance profile (less nausea and vomiting after treatment initiation), compared with the twice daily 10 microg exenatide. When compared to other glucose-lowering agents, once weekly exenatide is more efficacious than sitagliptin, pioglitazone or basal insulin (glargine or detemir), with the advantage of producing weight loss and lowering arterial blood pressure. It does not induce hypoglycaemia and does not necessarily require home blood glucose monitoring, two advantages compared with insulin therapy. Bydureon is currently only reimbursed in Belgium after failure of and in addition to metformin-sulfonylurea combination. ; Le Bydureon® est une nouvelle forme galénique, à libération prolongée, de l’exénatide, premier agoniste des récepteurs du Glucagon-Like Peptide-1 (GLP-1) à avoir été commercialisé pour le traitement du diabète de type 2. La technologie des microsphères permet une résorption prolongée de l’exénatide, autorisant une injection sous-cutanée hebdomadaire au lieu de deux injections par jour pour la formulation initiale (Byetta®). Le programme de développement clinique DURATION a montré que la forme hebdomadaire (2 mg/semaine) réduit de façon plus marquée le taux d’hémoglobine glyquée (HbA1c), avec un même effet sur la perte de poids, tout en offrant un meilleur profil de tolérance digestive (moins de nausées et de vomissements à l’instauration du traitement), par rapport à la forme ...