阿斯利康糖尿病复方新药Xigduo XR获FDA批准

阿斯利康糖尿病复方新药Xigduo XR获FDA批准

                               
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发布日期：2014-10-31  来源：新药汇  

阿斯利康（AstraZeneca）近日宣布，糖尿病复方新药Xigduo XR（dapagliflozin/缓释二甲双胍）获FDA批准，作为一种辅助药物，结合运动和饮食，用于适合dapagliflozin和二甲双胍联合治疗的2型糖尿病成人患者。

                               
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Xigduo XR为每日1次的复方单片，由固定剂量的dapagliflozin（达帕格列净，商品名：Forxiga）和缓释型盐酸二甲双胍组成，这2种成分具有互补性的作用机制，能够帮助改善血糖控制。

此前，Xigduo（dapagliflozin/速释二甲双胍）已于2014年1月获欧盟批准，是欧盟上市的首个SGLT2抑制剂和二甲双胍复方产品。在美国，由于阿斯利康和前合作伙伴百时美的监管推迟，强生Invokamet（canagliflozin/速释二甲双胍）于今年8月率先赢得FDA批准，是美国市场中的首个SGLT2和二甲双胍复方产品。Xigduo由阿斯利康和百时美施贵宝（BMS）达成的全球糖尿病联盟开发。不过，去年12月，阿斯利康耗资41亿美元收购百时美在该联盟中的全部股份后，全面接管了该单元。

目前，SGLT2抑制剂市场已经非常拥挤，除了dapagliflozin和canagliflozin，礼来和勃林格殷格翰empagliflozin也于今年8月获FDA批准，辉瑞和默沙东的ertugliflozin已处于后期临床。

钠-葡萄糖协同转运蛋白（SGLT2）抑制剂是新一类降糖药，具有独特的作用模式，独立于胰岛素发挥作用，能够在肾脏中选择性抑制SGLT2，帮助患者从尿液中排出多余的葡萄糖。SGLT2是一类特异性分布在肾脏近曲小管S1段的葡萄糖转运体，其生理作用是促进葡萄糖在肾小球的重吸收。与非糖尿病人群相比，2型糖尿病患者的肾脏能够重吸收大量的葡萄糖进入血液，这可能会推高血糖水平。

二甲双胍则是2型糖尿病治疗的一线药物，可单独或与其他药物（包括胰岛素）联合用药。在2型糖尿病患者中，肝脏产生过量的葡萄糖（glucose），从而提高血糖水平。二甲双胍可通过降低肝脏产生葡萄糖的量、增加肌肉对葡萄糖的敏感性、延缓肠道的葡萄糖吸收，降低机体的血糖水平。

英文原文：AstraZeneca wins U.S. approval for two-in-one diabetes pill

AstraZeneca ($AZN) won an FDA nod for a one-pill combination of its latest diabetes drug and the long-generic metformin, making it the second to market among a cadre of drugmakers developing similar cocktails.

The drug, to be marketed as Xigduo, pairs AstraZeneca's SGLT2-blocking dapagliflozin with metformin in a once-a-day, extended-release tablet for adults with Type 2 diabetes. Dapagliflozin, approved on its own as Farxiga, works by blocking glucose absorption in the kidneys and leads the body to dispel excess sugars through the urine. Paired with metformin, which decreases glucose production and improves the body's response to insulin, the drug effectively lowered patients' blood sugar levels, the company said.

Thanks to regulatory delays for AstraZeneca and ex-partner Bristol-Myers Squibb ($BMY), rival Johnson & Johnson ($JNJ) was the first mover in SGLT2, winning FDA approval for its canagliflozin last year and securing an August OK for Invokamet, which combines that drug with metformin. The crowded space also includes the tandem of Eli Lilly ($LLY) and Boehringer Ingelheim, which finally won an agency nod for empagliflozin this month. Meanwhile, Pfizer ($PFE) and Merck ($MRK) are working through late-stage trials with the competing ertugliflozin.

However, safety worries have thus far limited uptake for the SGLT2 class, as the treatments have been linked to increased rates of genital and urinary tract infections, plus kidney damage and cardiovascular issues. As a result, peak sales estimates for the class of drugs have been erratic, with some pegging their potential north of $5 billion and others expecting cumulative revenue more in line with $2 billion a year.

The biggest potential for SGLT2 drugs may lie in fixed-dose combinations, and each contender is working up at least one in hopes of boosting its market share. Lilly and Boehringer have submitted a fixed-dose treatment that combines their empagliflozin with linagliptin, a DPP-4 inhibitor marketed as Tradjenta. And Merck and Pfizer have similar goals with their SGLT2 drug, planning to pair it with the former's DPP-4 blockbuster Januvia.

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