Osteoporosis Therapy: Mechanistic Antiresorptives

J. Dodge, H. Bryant
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Abstract

Osteoporosis is defined as the thinning of bone resulting from the imbalance between bone resorption and bone formation, the two cellular mechanisms that regulate the remodeling of skeletal tissue. This loss of bone ultimately results in an increased risk of fracture. One therapeutic approach to treating patients with osteoporosis is to inhibit the process of bone resorption. This has been clinically manifested by the development of a number of large and small molecules that include calcitonin, integrin inhibitors, cathepsin K inhibitors, OPG/RANKL inhibitors, bisphosponates, and SERMS. This chapter describes recent advances in the anti-resorptive field with a focus on clinically validated targets and the molecules that have been developed to regulate these pathways. Keywords: Osteoporosis; Osteoclast; Osteoblast; Calcitonin; Cathepsin K Inhibitors; Osteoprotegerin; RANKL; Bisphosponates; Selective Estrogen Receptor Modulators; SERMs
骨质疏松症治疗:机械性抗吸收剂
骨质疏松症被定义为由于骨吸收和骨形成(调节骨组织重塑的两种细胞机制)之间的不平衡而导致的骨变薄。这种骨质流失最终会增加骨折的风险。治疗骨质疏松症的一种治疗方法是抑制骨吸收过程。这已经在临床上得到了体现,包括降钙素、整合素抑制剂、组织蛋白酶K抑制剂、OPG/RANKL抑制剂、双磷酸盐和SERMS等许多大分子和小分子药物的开发。本章描述了抗吸收领域的最新进展,重点是临床验证的靶点和已开发的调节这些途径的分子。关键词:骨质疏松症;破骨细胞;成骨细胞;降钙素;组织蛋白酶K抑制剂;Osteoprotegerin;RANKL;Bisphosponates;选择性雌激素受体调节剂;SERMs
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