Tiludronate displays potent inhibitory against proton transport in yeast microsomal preparations with an IC50 of 3.5 μM and inhibits the activity of purified yeast V-ATPase. Tiludronate inhibits proton transport with IC50s of 1.1 mM and 466 nM in kidney-derived vesicles and vesicles derived from osteoclasts[3].

Tiludronate dose-dependently inhibits the resorption of bones. Tiludronate reduces the secrete proton of mature osteoclasts into the resorption space and favors the detachment of mature osteoclasts from the bone matrix. Oral administration of Tiludronate (5-200 mg/kg) prevents the decrease in the skeletal mass in the castrated male rat model[3].