Adis, Auckland, New Zealand.
Drugs. 2010 Mar 5;70(4):489-512. doi: 10.2165/11203790-000000000-00000.
Sitagliptin (Januvia, Glactiv(R), Tesavel(R)) is a dipeptidyl peptidase-4 inhibitor indicated for the treatment of type 2 diabetes mellitus. Oral sitagliptin as monotherapy or combination therapy was generally well tolerated and improved glycaemic control in well designed clinical trials in patients with type 2 diabetes. Glycosylated haemoglobin (HbA(1c)) levels were significantly reduced with sitagliptin monotherapy relative to voglibose monotherapy or placebo, and with sitagliptin as initial combination therapy with metformin or pioglitazone relative to monotherapy with these agents or placebo. Moreover, sitagliptin monotherapy was noninferior to metformin monotherapy in terms of the reduction in HbA(1c) levels. Significant reductions in HbA(1c) levels, relative to background therapy, were also observed with sitagliptin add-on therapy to ongoing treatment with thiazolidinediones, sulfonylureas or insulin with or without metformin, or metformin alone. In terms of the reduction in HbA(1c) levels as add-on treatment to metformin, sitagliptin was noninferior to glipizide and generally did not differ from rosiglitazone, and as add-on treatment to pioglitazone, it did not differ significantly from metformin. Sitagliptin had a low risk of hypoglycaemia (except when used in combination with agents that may be associated with hypoglycaemia, such as sulfonylureas or insulin) and was generally weight-neutral. Although additional comparative data and longer-term studies with glycaemic and clinical outcomes are required to definitively position sitagliptin relative to other antihyperglycaemic agents, current evidence suggests that it is a useful treatment option for patients with type 2 diabetes, with potential advantages including oral administration, a generally weight-neutral effect and a low risk of hypoglycaemia.
西他列汀（捷诺维、加乐特、泰萨维尔）是一种二肽基肽酶-4 抑制剂，用于治疗 2 型糖尿病。在设计良好的临床试验中，口服西他列汀单药治疗或联合治疗通常具有良好的耐受性，并改善了 2 型糖尿病患者的血糖控制。与伏格列波糖单药治疗或安慰剂相比，西他列汀单药治疗可显著降低糖化血红蛋白（HbA1c）水平，与二甲双胍或吡格列酮初始联合治疗相比，也可显著降低这些药物单药治疗或安慰剂的 HbA1c 水平。此外，西他列汀单药治疗在降低 HbA1c 水平方面不劣于二甲双胍单药治疗。与背景治疗相比，西他列汀添加治疗也可显著降低噻唑烷二酮类、磺酰脲类或胰岛素（无论是否与二甲双胍合用）或单独使用二甲双胍的治疗中的 HbA1c 水平。在作为二甲双胍添加治疗降低 HbA1c 水平方面，西他列汀不劣于格列吡嗪，通常与罗格列酮无差异，作为吡格列酮的添加治疗，与二甲双胍无显著差异。西他列汀低血糖风险低（与可能与低血糖相关的药物联合使用时除外，如磺酰脲类或胰岛素），通常对体重无影响。虽然需要更多的比较数据和长期的血糖和临床结局研究来明确西他列汀相对于其他抗高血糖药物的地位，但目前的证据表明，它是 2 型糖尿病患者的一种有用的治疗选择，可能的优点包括口服给药、一般对体重无影响和低血糖风险低。
