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Drugs. 2019 Jul;79(10):1135-1146. doi: 10.1007/s40265-019-01148-3.
Dapagliflozin (Forxiga) is a highly potent, reversible and selective sodium-glucose cotransporter-2 inhibitor indicated worldwide for the treatment of type 2 diabetes (T2D). In the EU, oral dapagliflozin once daily is approved for use as monotherapy (in patients who are intolerant of metformin) and as add-on combination therapy (with other glucose-lowering agents, including insulin) for T2D when diet and exercise alone do not provide adequate glycaemic control. In numerous well-designed clinical studies and their extensions, dapagliflozin as monotherapy and combination therapy with other antihyperglycaemic agents provided effective glycaemic control and reduced bodyweight and blood pressure (BP) across a broad spectrum of patients. Dapagliflozin reduced the rate of cardiovascular (CV) death or hospitalization for heart failure (HHF), did not adversely affect major adverse CV events (MACE) and possibly reduced progression of renal disease relative to placebo in patients with established atherosclerotic CV disease (CVD) or multiple risk factors for CVD. Dapagliflozin was generally well tolerated, with a low risk of hypoglycaemia; diabetic ketoacidosis (DKA), although rare, and genital infections were more common with dapagliflozin than placebo. Given its antihyperglycaemic, cardioprotective and possibly renoprotective properties and generally favourable tolerability profile, dapagliflozin provides an important option for the management of a broad patient population, regardless of the history of CVD.
达格列净(Forxiga)是一种高效、可逆且选择性的钠-葡萄糖协同转运蛋白 2(SGLT2)抑制剂,在全球范围内被批准用于治疗 2 型糖尿病(T2D)。在欧盟,达格列净每日口服一次,既可单药治疗(用于不能耐受二甲双胍的患者),也可与其他降糖药物(包括胰岛素)联合治疗,用于饮食和运动不能充分控制血糖的 T2D 患者。在大量精心设计的临床研究及其扩展研究中,达格列净单药治疗和与其他抗高血糖药物联合治疗,在广泛的患者人群中提供了有效的血糖控制,并降低了体重和血压(BP)。达格列净降低了伴有已确诊动脉粥样硬化性心血管疾病(CVD)或 CVD 多种危险因素的患者的心血管(CV)死亡或因心力衰竭(HF)住院的发生率,与安慰剂相比,不增加主要不良心血管事件(MACE)的发生风险,可能还降低了肾脏疾病的进展速度。达格列净总体耐受性良好,低血糖风险低;虽然糖尿病酮症酸中毒(DKA)罕见,但与安慰剂相比,达格列净更常见生殖器感染。鉴于其降糖、心脏保护和可能的肾脏保护作用,以及总体良好的耐受性,达格列净为管理广泛的患者人群提供了一个重要选择,无论其 CVD 病史如何。