Hoy Sheridan M
Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.
Drugs. 2021 Sep;81(13):1593-1596. doi: 10.1007/s40265-021-01578-y.
Upacicalcet (UPASITA) is an intravenous calcimimetic agent being developed by Sanwa Kagaku Kenkyusho, under license from EA Pharma, for the treatment of secondary hyperparathyroidism (SHPT), a common and early complication of chronic kidney disease, in patients undergoing haemodialysis. By acting directly on parathyroid cell membrane calcium-sensing receptors, upacicalcet suppresses excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels. Upacicalcet received its first approval on 23 June 2021 for the treatment of SHPT in adults undergoing haemodialysis in Japan. It is administered intravenously three times per week into the venous side of the haemodialysis circuit at the time of blood return at the end of the haemodialysis session. The generally recommended starting dose of upacicalcet is 25 µg, with the dose adjusted within a 25-300 µg range based on PTH and serum calcium levels. This article summarizes the milestones in the development of upacicalcet leading to this first approval for the treatment of SHPT in patients undergoing haemodialysis.
upaicalcet（UPASITA）是三洋化学研究所根据EA制药公司的许可开发的一种静脉注射拟钙剂，用于治疗接受血液透析的患者的继发性甲状旁腺功能亢进（SHPT），这是慢性肾病常见的早期并发症。通过直接作用于甲状旁腺细胞膜钙敏感受体，upaicalcet抑制甲状旁腺激素（PTH）过度分泌，从而降低血液中PTH水平。upaicalcet于2021年6月23日首次获得批准，用于治疗日本接受血液透析的成人SHPT。在血液透析疗程结束回血时，每周通过静脉注射三次，注入血液透析回路的静脉侧。upaicalcet的一般推荐起始剂量为25μg，根据PTH和血清钙水平在25 - 300μg范围内调整剂量。本文总结了upaicalcet开发过程中的里程碑事件，这些事件促成了其首次获批用于治疗接受血液透析患者的SHPT。
