Current and emerging therapies for the treatment of osteoporosis.
Current and emerging therapies for the treatment of osteoporosis.
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DOI：
10.2147/jep.s7823
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发表时间：
2010
影响因子：
--
通讯作者：
Waalen J
中科院分区：
文献类型：
--
作者：
Waalen J
骨质疏松症表示由于骨组织内持续进行的骨形成和骨吸收的动态过程的不平衡而导致的骨组织的弱化。大多数目前可用的骨质疏松症治疗是抗吸收剂。在过去的十年中，二膦酸盐，特别是阿仑膦酸盐和利塞膦酸盐，已成为主要药物，较新的二膦酸盐，如伊班膦酸盐和唑来膦酸，给药方案的频率下降的趋势。合成雌激素受体调节剂（SERM）继续被开发为维持雌激素的骨保护作用同时避免其相关不良副作用的药物。目前这类药物包括雷洛昔芬（美国唯一的SERM）和拉索昔芬和巴多昔芬（欧洲）。降钙素，通常作为鼻喷雾剂给药，完成了目前批准的抗吸收剂的列表，而甲状旁腺激素类似物代表了目前在美国和欧洲批准的唯一合成代谢剂。雷奈酸锶是一种在欧洲可用但在美国不可用的额外药物，具有合成代谢和抗吸收活性。预计将进一步扩大治疗选择的新药物包括denosumab，一种再吸收酶组织蛋白酶K的单克隆抗体抑制剂，目前正处于食品和药物管理局批准的最后阶段。临床前开发中的其他药物包括靶向Wnt/β-连环蛋白途径的特定分子的药物，这些分子参与刺激成骨细胞的骨形成。这篇综述讨论了目前可用的药物的使用，以及突出新兴的药物，预计在不久的将来带来显着的变化，骨质疏松症的治疗方法。
Osteoporosis represents a weakening of bone tissue due to an imbalance in the dynamic processes of bone formation and bone resorption that are continually ongoing within bone tissue. Most currently available osteoporosis therapies are antiresorptive agents. Over the past decade, bisphosphonates, notably alendronate and risedronate, have become the dominant agents with newer bisphosphonates such as ibandronate and zoledronic acid following a trend of less frequent dosing regimens. Synthetic estrogen receptor modulators (SERMs) continue to be developed as drugs that maintain the bone-protective effects of estrogen while avoiding its associated adverse side effects. Currently available agents of this class include raloxifene, the only SERM available in the United States (US), and lasofoxifene and bazedoxifene, available in Europe. Calcitonin, usually administered as a nasal spray, completes the list of currently approved antiresorptive agents, while parathyroid hormone analogs represent the only anabolic agents currently approved in both the US and Europe. Strontium ranelate is an additional agent available in Europe but not the US that has both anabolic and antiresorptive activity. New agents expected to further expand therapeutic options include denosumab, a monoclonal antibody inhibitor of the resorptive enzyme cathepsin K, which is in the final stages of Food and Drug Administration approval. Other agents in preclinical development include those targeting specific molecules of the Wnt/β-catenin pathway involved in stimulating bone formation by osteoblast cells. This review discusses the use of currently available agents as well as highlighting emerging agents expected to bring significant changes to the approach to osteoporosis therapy in the near future.