Schultz Thomas C, Valenzano Jonathan P, Verzella Jessica L, Umland Elena M
Jefferson School of Pharmacy, Thomas Jefferson University, 901 Walnut Street, Suite 901, Philadelphia, PA 19107, USA.
Womens Health (Lond). 2015 Nov;11(6):805-14. doi: 10.2217/whe.15.39. Epub 2015 Sep 7.
Odanacatib represents a novel treatment option in the approach of postmenopausal women. Postmenopausal women with osteoporosis experience a disturbance in bone remodeling wherein bone resorption exceeds bone formation. Cathepsin K is a lysosomal cysteine protease found primarily in osteoclasts that plays a major role in the breakdown of bone via its collagenase properties. Targeting a new area of pathophysiology, odanacatib inhibits cathepsin K to reduce bone resorption while preserving bone formation. Phase II and III trials have shown efficacy in increasing bone mineral density in the target treatment group. Overall, safety studies have found odanacatib to be well-tolerated and comparable to placebo; however, some imbalances in adverse events have been observed in the Phase III trials. Current and future studies will analyze the long-term ability of odanacatib in preventing bone fracture.
odanacatib是绝经后女性治疗方法中的一种新型选择。患有骨质疏松症的绝经后女性经历骨重塑紊乱，其中骨吸收超过骨形成。组织蛋白酶K是一种主要存在于破骨细胞中的溶酶体半胱氨酸蛋白酶，通过其胶原酶特性在骨分解中起主要作用。odanacatib针对病理生理学的一个新领域，抑制组织蛋白酶K以减少骨吸收，同时保留骨形成。II期和III期试验已表明在目标治疗组中增加骨矿物质密度具有疗效。总体而言，安全性研究发现odanacatib耐受性良好且与安慰剂相当；然而，在III期试验中观察到不良事件存在一些不平衡。当前和未来的研究将分析odanacatib预防骨折的长期能力。
