tiludronate

Tiludronate is a first-generation, non-nitrogenous bisphosphonate. It is used in human medicine primarily for the treatment of Paget's disease of bone, a chronic disorder characterized by excessive bone degradation and abnormal bone formation. In veterinary medicine, it is used to treat conditions in horses such as navicular disease, bone spavin, and osteoarthritis. Its mechanism of action involves inhibiting osteoclast-mediated bone resorption. It achieves this by binding to hydroxyapatite in bone, being ingested by osteoclasts, and then interfering with essential metabolic pathways within these cells, leading to their apoptosis. Specifically, it disrupts the mevalonate pathway by inhibiting farnesyl pyrophosphate synthase and inhibits protein-tyrosine-phosphatase, which impairs osteoclast function and survival. It also appears to inhibit vacuolar-type proton ATPase (V-ATPase) in osteoclasts. This action reduces bone turnover, stabilizes bone mass, and improves bone density.

Brand names

SkelidTildrenEquidronate

Other names

tiludronate disodium