Currently available drugs for the treatment of osteoporosis can still be improved in terms of pharmacokinetics, pharmacodynamics and management. New approaches for the development of innovative drugs are possible thanks to our increasing understanding of the bone tissue biology and the cellular and molecular processes that regulate it. One of the new anti-bone resorption agents, odanacatib, a selective cathepsin-K inhibitor, is in late phase III clinical research. Among new bone anabolic drugs, those that have an action on the Wnt signaling pathway appear to be particularly promising. The development of new compounds for the treatment of osteoporosis represents an excellent example of translational medicine efforts aimed to extend the range of treatment options for osteoporosis, a very common disease with a high social and economic impact, particularly when causing fractures.