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Tiludronate is a bisphosphonate that inhibits bone resorption.1,2 It inhibits pit formation induced by primary mouse osteoclast-like multinucleated cells (OCLs) and decreases primary mouse OCL-induced increases in dentine resorption levels in dentine slices when used at a concentration of 100 µM.1 Tiludronate (300 µM) inhibits secretion of casein-degrading proteinase, proteoglycan-degrading proteinase, and collagenase induced by colony-stimulating factor (CSF) in primary rabbit synovial cells and chondrocytes.3 It decreases the erythrocyte sedimentation rate (ESR), a marker of inflammation, and hindlimb paw levels of prostaglandin E2 (PGE2) in a rat model of M. tuberculosis-induced arthritis. Tiludronate also reduces paw redness, swelling, and volume, and increases the latency to fall in the rotarod test in the same model.4 Formulations containing tiludronate have been used in the treatment of Paget's disease of bone.
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1. A possible mechanism of the specific action of bisphosphonates on osteoclasts: Tiludronate preferentially affects polarized osteoclasts having ruffled borders. Bone 17(2), 137-144 (1995).
2. Bisphosphonates in the treatment of osteoporosis. Endocrine 6(2), 203-206 (1997).
3. Effects of 1-
4. Studies on the chronic phase of adjuvant arthritis: Effect of SR 41319, a new diphosphonate. Ann. Rheum. Dis. 45(1), 67-74 (1986).