Minodronate is a heterocyclic nitrogen-containing bisphosphonate with high potency in inhibiting bone resorption, and is developed for clinical use in Japan. Minodronate has very high potency in inhibiting farnesyl pyrophosphate synthase, and shows lower affinity for bone matrix hydroxyapatite at both neutral and acidic pH. As a result, small amount of minodronate is deposited in bone but can exert strong anti-resorptive activity in vivo. In this review on minodronate, we summarize the mechanism of action, physico-chemical properties, effects on bone quality in animals, and effects on bone turnover, bone mineral density and fracture prevention, as well as safety in the treatment of patients with osteoporosis.