Division of Nephrology, Dialysis, and Renal Transplant, Fondazione Ca' Granda-IRCCS, OspedaleMaggiore-Policlinico, v. Commenda 15, 20122 Milano, Italy.
Expert Opin Drug Metab Toxicol. 2011 Apr;7(4):517-28. doi: 10.1517/17425255.2011.562196. Epub 2011 Mar 1.
Cinacalcet has recently been introduced as a treatment for secondary hyperparathyroidism in dialysis patients and for parathyroid carcinoma. However, there has been an increasing interest in finding out whether cinacalcet can be used as a treatment for other parathyroid hormone (PTH)-dependent hypercalcemic conditions also.
The article reports the most relevant recent contributions dealing with calcium sensing receptor (CaSR) physiology as well as cinacalcet pharmacokinetics and pharmacodynamics. It also looks at the different hypercalcemic conditions where the use of cinacalcet has been proposed. This article was researched using clinical trials, case reports and outstanding basic research published in the last 3 years (MEDLINE database up to 31 November 2010). It provides the reader with an insight into the many unaddressed issues regarding cinacalcet that need to be resolved before it can be used in newly proposed fields.
Since cinacalcet may not only have an effect on parathyroid CaSR but also on CaSR expressed at bone and renal levels, it can currently only be considered a good alternative to parathyroidectomy in PTH-dependent hypercalcemic conditions when surgical intervention is burdened by a high failure rate or when it can be considered a risky procedure. At present, cinacalcet cannot be considered the first choice treatment in asymptomatic primary hyperparathyroidism or in mild-to-moderate forms of familial hypocalciuric hypocalcemia.
西那卡塞最近被引入用于治疗透析患者的继发性甲状旁腺功能亢进症和甲状旁腺癌。然而，人们越来越关注西那卡塞是否可用于治疗其他甲状旁腺激素（PTH）依赖性高钙血症。
本文报告了有关钙敏感受体（CaSR）生理学以及西那卡塞药代动力学和药效学的最新相关贡献。它还研究了提出使用西那卡塞的不同高钙血症情况。本文通过临床试验、病例报告和过去 3 年（截至 2010 年 11 月 31 日的 MEDLINE 数据库）发表的杰出基础研究进行了研究。它使读者深入了解在新提出的领域使用西那卡塞之前需要解决的许多尚未解决的问题。
由于西那卡塞不仅可能对甲状旁腺 CaSR 有作用，而且对骨骼和肾脏水平表达的 CaSR 有作用，因此目前仅当手术干预因高失败率而受到限制时，或者当手术被认为是有风险的时，它才能被认为是 PTH 依赖性高钙血症情况下甲状旁腺切除术的一种很好的替代方法。目前，西那卡塞不能被认为是无症状原发性甲状旁腺功能亢进症或轻度至中度家族性低钙血症的首选治疗方法。
