Farxiga(dapagliflozin，中文药名：达格列净片)于2014年1月8日获美国FDA批准用于改善2型糖尿病患者的血糖控制新药。
批准日期： 2014年1月 8日；公司：Bristol-Myers Squibb和AstraZeneca公司
FARXIGA(dapagliflozin)片为口服使用
美国初始批准：2014
适应证和用途
FARXIGA是一种钠-葡萄糖协同转运蛋白2(SGLT2)抑制剂适用在有2型糖尿病成人中作为辅助饮食和运动改善血糖控制。
使用限制：不为1型糖尿病或糖尿病酮症酸中毒治疗。
剂量和给药方法
（1）推荐起始剂量是5mg每天1次，早晨服用，有或无食物。
（2）在耐受FARXIGA需要附加血糖控制患者中剂量可增加至10mg每天1次。
（3）开始FARXIGA前评估肾功能。如eGFR低于60mL/min/1.73 m2不要开始FARXIGA。
（4）终止FARXIGA如eGFR下降持续低于60mL/min/1.73 m2。
剂型和规格
片：5mg和10mg。
禁忌证
（1）对FARXIGA严重超敏反应史。
（2）严重肾受损，肾病终末期，或透析。
警告和注意事项
（1）低血压：开始FARXIGA前，评估血容量状态和在老年人，在有肾受损或低收缩压患者，和用利尿药患者中纠正低血容量。治疗期间监视体征和症状。
（2）肾功能受损：治疗期间监视肾功能。
（3）低血糖：在用FARXIGA服用胰岛素或一种胰岛素促分泌素患者，考虑较低剂量胰岛素或胰岛素促分泌素以减低低血糖风险。
（4）生殖器真菌感染：如适用监视和治疗。
（5）LDL-C增高：每标准医护监视和治疗。
（6）膀胱癌：在临床试验中观察到膀胱癌不平衡。有活动性膀胱癌患者中不应使用FARXIGA和有膀胱癌既往史患者中应谨慎使用。
（7）大血管病变结局：没有临床研究确定用FARXIGA或任何其他抗糖尿病药物减低大血管风险结论性证据。
不良反应
伴随FARXIGA最常见不良反应(5%或更高发生率)是女性生殖器真菌感染，鼻咽炎，和泌尿道感染。
在特殊人群中使用
（1）妊娠：在妊娠妇女中没有适当和对照良好研究。妊娠期间只有潜在获益胜过对胎儿潜在风险才使用。
（2）哺乳母亲：终止FARXIGA或终止哺乳.
（3）老年人：与减低血管内容量相关不良反应发生率较高。
（4）肾受损：与减低血管内容量和肾功能相关不良反应发生率较高。
完整资料请下载：http://packageinserts.bms.com/pi/pi_farxiga.pdf

US FDA approves FARXIGA™ (dapagliflozin) tablets for the treatment of adult patients with type 2 diabetes
Monday, 13 January 2014
AstraZeneca and Bristol-Myers Squibb Company announced the US Food and Drug Administration (FDA) approved FARXIGA™ [far-SEE-ga] (dapagliflozin), a once-daily oral treatment indicated as an adjunct to diet and exercise to improve glycaemic control in adults with type 2 diabetes mellitus. FARXIGA should not be used for the treatment of patients with type 1 diabetes or diabetic ketoacidosis.
The recommended starting dose of FARXIGA is 5 mg once daily, taken in the morning, with or without food. In patients tolerating FARXIGA 5 mg once daily who require additional glycaemic control, the dose can be increased to 10 mg once daily. FARXIGA is part of a newer class of medicines called sodium-glucose cotransporter 2 (SGLT2) inhibitors, which remove glucose via the kidneys.
“With the diabetes epidemic escalating and many people with type 2 diabetes struggling to reach their blood sugar goals, FARXIGA offers an important new option for healthcare professionals and adult patients,” said Brian Daniels, Senior Vice President, Global Development and Medical Affairs, Bristol-Myers Squibb. “In clinical trials, FARXIGA helped improve glycaemic control, and offered additional benefits of weight and blood pressure reductions.”
FARXIGA is contraindicated in patients with a history of a serious hypersensitivity reaction to FARXIGA or with severe renal impairment, end stage renal disease, or patients on dialysis.
“The addition of FARXIGA to our US treatment portfolio is a step forward as we work to help reduce the burden of type 2 diabetes by offering a range of treatment options with different modes of action,” said Briggs Morrison, Executive Vice President, Global Medicines Development & Chief Medical Officer, AstraZeneca. “We aim to help adults with type 2 diabetes, and their doctors, create individualised treatment programmes that will help patients lower their glucose levels.”
Dapagliflozin (marketed outside of the United States as FORXIGA®) is approved for the treatment of adults with type 2 diabetes, along with diet and exercise, in 40 countries, including European Union countries and Australia.
NOTES TO EDITORS
FARXIGA Clinical Development Programme
The robust FARXIGA clinical development programme included 24 clinical studies eva luating safety and efficacy. The studies included more than 11,000 adults with type 2 diabetes, including more than 6,000 patients treated with FARXIGA.
FARXIGA causes intravascular volume contraction. Symptomatic hypotension can occur after initiating FARXIGA particularly in patients with impaired renal function (eGFR less than 60 mL/min/1.73 m2), elderly patients, or patients on loop diuretics. Before initiating FARXIGA in patients with one or more of these characteristics, volume status should be assessed and corrected. Monitor for signs and symptoms of hypotension after initiating therapy. FARXIGA increases serum creatinine and decreases eGFR. Elderly patients and patients with impaired renal function may be more susceptible to these changes. Adverse reactions related to renal function can occur after initiating FARXIGA. Renal function should be eva luated prior to initiation of FARXIGA and monitored periodically thereafter.
In a 24-week, add-on to metformin clinical trial, adult patients with type 2 diabetes treated with FARXIGA 5 mg (n=137; baseline HbA1c 8.2%) or 10 mg (n=135; baseline HbA1c 7.9%) had significant reductions in HbA1c of -0.7% and -0.8%, respectively, compared with placebo plus metformin reductions of -0.3% (n=137; baseline HbA1c 8.1%). In the same study, the placebo-adjusted reduction in body weight was -2.2 kg with FARXIGA 5 mg (baseline 84.7 kg) and -2.0 kg with 10 mg (baseline 86.3 kg). Also, mean changes from baseline in systolic blood pressure relative to placebo plus metformin were -4.5 mmHg and -5.3 mmHg with FARXIGA 5 mg or 10 mg plus metformin, respectively. No major episodes of hypoglycaemia were seen in any of the treatment arms. Minor episodes of hypoglycaemia were reported in 1.5%, 0.7%, and 0% with FARXIGA 5 mg, 10 mg, and placebo plus metformin, respectively.
In addition to the clinical development programme, the AstraZeneca/Bristol-Myers Squibb Diabetes Alliance has initiated DECLARE, a large, randomised, placebo-controlled study of more than 17,000 adult patients with type 2 diabetes designed to determine the effect of FARXIGA, when added to the patients’ current anti-diabetes therapy, on the risk of CV events, such as CV death, myocardial infarction or ischaemic stroke, compared with placebo. The study, which will also provide additional data on the long-term safety profile, initiated enrolment in April 2013 and has an anticipated completion date of 2019.
FDA批准Forxiga用于治疗2型糖尿病
2014年1月8日，美国食品药品管理局（FDA）批准Forxiga (dapaglifozin)片结合饮食和锻炼，用于改善2型糖尿病患者的血糖控制。在美国，2型糖尿病影响着大约2400万人，占确诊糖尿病患者的90%以上。随着时间的推移，高血糖水平能够增加严重并发症风险，包括心脏疾病、失明及神经和肾损伤。
“在糖尿病的整体治疗与护理当中，控制血糖水平是非常重要的，Forxiga可以为数以百万计的2型糖尿病美国患者提供一种额外的治疗选择，”FDA药物评价与研究中心药物评价办公室主任、医学博士、公共卫生学硕士Curtis Rosebraugh说。
Forxiga是一种钠-葡萄糖协同转动蛋白2抑制剂，它可以阻断肾脏对葡萄糖的重吸收，增加葡萄糖排泄，从而降低血糖水平。这款药物的安全性及有效性在16项临床试验中进行了评价，有9400多名2型糖尿病患者参与了临床试验。临床试验显示这款药物能改善HbA1c（糖化血红蛋白，一种血糖测定指标）水平。
Forxiga作为单独用药及与其它2型糖尿病治疗药物合并用药，包括二甲双胍、吡格列酮、格列美脲、西他列汀及胰岛素均进行了研究。1型糖尿病患者，血液或尿中酮体升高的患者（糖尿病酮症酸中毒），或中度或重度肾损害、终末期肾脏疾病或透析患者不能使用Forxiga进行治疗。
临床试验中，Forxiga用药患者患膀胱癌的人数增加，所以Forxiga不被建议用于膀胱癌活动期患者。有膀胱癌病史的患者应该在使用Forxiga之前咨询其医师。Forxiga可引起脱水，致使血压下降（低血压），导致头晕和/或昏厥及肾功能下降。肾功能受损的老年患者及以利尿剂治疗其它疾病的患者似乎更易出现这种风险。
FDA要求对Forxiga进行6项上市后研究：
1、一项心血管结局临床试验(CVOT)，用以评价Forxiga对高基值心血管疾病风险患者的心血管风险；
2、一项双盲、随机对照试验，用以CVOT中患者膀胱癌风险的评价；
3、一项动物研究，用以评价Forxiga诱发的尿流量/速率的变化，以及诱发啮齿类动物膀胱肿瘤的情况；
4、两项临床试验，用以评价儿科患者的药代动力学、有效性和安全性；
5、一项增强的药物警戒程序，用以监控肝功能异常和妊娠结局的报告。
在临床试验中，Forxiga用药患者最常见的副作用有生殖器霉菌（真菌）感染和尿路感染。Forxiga由百时美施贵宝和阿斯利康上市销售。