Yokoyama Keitaro
Division of Nephrology and Hypertension, Department of Internal Medicine, The Jikei University School of Medicine, Japan.
Clin Calcium. 2014 Dec;24(12):1815-23.
In patients with end-stage renal disease (ESRD) , hyperphosphatemia contributes to secondary hyperparathyroidism and can lead to skeletal complications including fracture, and vascular calcification. Currently employed phosphate binders include calcium carbonate, sevelamer hydrochloride, and lanthanum carbonate. While these agents are effective at binding orally ingested phosphates, they vary in safety, potency, and off-target effects, some of which may be salutary (e.g., low-density lipoprotein and uric acid lowering with sevelamer) and others adverse (low turnover bone disease and progressive vascular calcification with calcium) . There remains a large unmet need for safe and effective phosphate binders with favorable off-target effects.
在终末期肾病(ESRD)患者中,高磷血症会导致继发性甲状旁腺功能亢进,并可能引发包括骨折和血管钙化在内的骨骼并发症。目前使用的磷结合剂包括碳酸钙、盐酸司维拉姆和碳酸镧。虽然这些药物在结合口服摄入的磷酸盐方面有效,但它们在安全性、效力和非靶向效应方面存在差异,其中一些可能是有益的(例如,司维拉姆可降低低密度脂蛋白和尿酸),而另一些则是有害的(钙会导致低转换骨病和进行性血管钙化)。对于具有良好非靶向效应的安全有效的磷结合剂,仍有很大的未满足需求。