IJCP：临床试验表明II型糖尿病药物利拉利汀长期使用有效且安全

利拉利汀(linagliptin)通过阻断二肽基肽酶-4(DPP-4)活性而发挥作用，其中DPP-4一种破坏激素GLP-1的酶，而GLP-1则有助于当需要胰岛素时，身体产生更多的胰岛素。

对II型糖尿病患者开展的一项长期的药物临床试验证实一种口服DPP-4抑制剂利拉利汀是安全的和有效的，这就意味着利用利拉利汀或者与其他选定的口服抗糖尿病药物一起能够降低血糖水平长达102周。

由31个国家参与的这项研究追踪了2121名在之前已参与4项为期24周的随机化、双盲和安慰剂受控的临床试验的糖尿病患者，以便再监控他们78周。

那些之前口服利拉利汀的糖尿病患者(1532名)继续服用这种药物，那些在早期试验中接受安慰剂的糖尿病患者(589名)在接下来的为期78周的延长试验(extended rial)中也服用利拉利汀。

初始为期24周的临床试验表明利拉利汀独立地或者其他血糖降低试剂(二甲双胍或二甲双胍与磺脲或二甲双胍与吡格列酮)结合使用能够有效地改善对血糖的控制，同时不会产生体重增加，也不会有提高患上低血糖症的风险。

来自为期78周的延长试验结果表明服用利拉利汀的2121名II型糖尿病患者维持血糖控制长达102周。因此，这项研究表明利拉利汀一种有效的和耐受良好的药物，能够被用来长期控制II型糖尿病患者的血糖水平。

本文编译自32-country study shows that type 2 diabetes drug is clinically effective for long-term use

doi: 10.1111/j.1742-1241.2012.02975.x
PMC:
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Long-term safety and efficacy of linagliptin as monotherapy or in combination with other oral glucose-lowering agents in 2121 subjects with type 2 diabetes: up to 2 years exposure in 24-week phase III trials followed by a 78-week open-label extension

R. Gomis1, D. R. Owens2, M.-R. Taskinen3, S. Del Prato4, S. Patel5, A. Pivovarova6, A. Schlosser7, H.-J. Woerle

Aim:  The aim of this study was to evaluate the long-term safety, tolerability and efficacy of the dipeptidyl peptidase-4 inhibitor linagliptin given either alone or in combination with other oral glucose-lowering agents in persons with type 2 diabetes. Methods:  A 78-week open-label extension study evaluated subjects who participated in one of four preceding 24-week, randomised, double-blind, placebo-controlled parent trials and who received linagliptin, linagliptin + metformin, linagliptin + metformin + a sulphonylurea or linagliptin + pioglitazone (all with linagliptin administered orally once daily). Individuals receiving one of these treatments during a previous trial continued the same treatment (n = 1532) for up to a total of 102 weeks, whereas those previously receiving placebo were switched to linagliptin (n = 589). All 2121 participants received at least one dose of the trial medication and were included in the primary safety analysis. Results:  In subjects previously receiving active treatment, the glycosylated haemoglobin A1c reduction achieved during the 24-week parent trials was sustained through the 78-week extension period (change from baseline to week 102: −0.8%). Drug-related adverse events were experienced by 14.3% of participants. Hypoglycaemia occurred in 13.9% of participants and was similar between those previously receiving treatment (13.6%) and those switching from placebo to linagliptin (14.6%). Hypoglycaemia occurred most frequently with the use of metformin + a sulphonylurea background therapy (11%). Overall, no clinically relevant changes in body weight were observed. Conclusion:  Long-term treatment with linagliptin was well tolerated with no change in the safety profile observed during the extension study. Sustained long-term glycaemic control was maintained for up to 102 weeks with either linagliptin monotherapy or linagliptin in combination with other oral glucose-lowering agents.