Novartis Institutes for BioMedical Research, Basel, Switzerland.
Expert Opin Ther Pat. 2010 Apr;20(4):563-82. doi: 10.1517/13543771003604729.
Bones play many roles in the body, providing structure, protecting organs, anchoring muscles and storing calcium. Over 100 million people worldwide suffer from bone diseases, mainly osteoporosis, cancer-related bone loss, osteoarthritis and inflammatory arthritis. Osteoporosis itself has no specific symptoms, and the main consequence is the increased risk of bone fractures. Therefore, the prevention of bone diseases is important to maintain the quality of life in the human society. However, treatment options are still insufficient.
This review article gives a summary of the low molecular mass modulators of bone diseases targets disclosed in patent applications and articles, mainly during the last 5 years.
Readers will rapidly gain an overview of these modulators not only for historical targets, but also of emerging and re-visited targets. Readers will also be able to see the current research trend and the main players in this field.
Drug discovery for bone diseases has made progress in the last years. The research area has dynamically shifted from historical targets (bisphosphonate, parathyroid hormone and calcitonin) to newly confirmed targets or targets re-visited which were biologically validated in the past. Cathepsin K inhibitors should be very close to launching in the market.
骨骼在人体中发挥着多种作用，提供结构支撑、保护器官、固定肌肉和储存钙。全球有超过 1 亿人患有骨骼疾病，主要包括骨质疏松症、与癌症相关的骨骼流失、骨关节炎和炎症性关节炎。骨质疏松症本身没有特定的症状，其主要后果是骨折风险增加。因此，预防骨骼疾病对于维持人类社会的生活质量非常重要。然而，治疗选择仍然不足。
本文综述了专利申请和文章中披露的针对骨骼疾病靶点的低分子量调节剂，主要是在过去 5 年。
读者将快速了解这些调节剂，不仅针对历史靶点，还针对新兴和重新研究的靶点。读者还将能够看到该领域当前的研究趋势和主要参与者。
近年来，骨骼疾病的药物发现取得了进展。研究领域已从历史靶点（双膦酸盐、甲状旁腺激素和降钙素）动态转移到过去生物学验证的新确认靶点或重新研究的靶点。组织蛋白酶 K 抑制剂应该很快就会推向市场。
