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ONO-5334 is a potent, selective, and orally active small molecule inhibitor of cathepsin K, a cysteine protease involved in bone resorption. Developed by Ono Pharmaceutical, it was investigated as a treatment for postmenopausal osteoporosis and osteopenia. Clinical studies demonstrated that ONO-5334 increases bone mineral density (BMD) at the spine and hip in postmenopausal women with osteoporosis or osteopenia. Its mechanism of action involves inhibiting cathepsin K to reduce bone resorption while having minimal suppression on bone formation markers compared to standard treatments like alendronate. Although it showed efficacy in increasing BMD and had an acceptable safety profile during trials, development has been discontinued[1][2][3][5][6].
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