Postmenopausal osteoporosis is characterized by an increase in resorption and inadequate bone formation. Alteration in bone remodeling is associated with an accelerated risk of fracture. Pharmacological agents that increase bone mass, reduce bone loss or decrease fracture risk have become available in the last few decades. Current compounds used for the treatment of osteoporosis mostly inhibit osteoclast-mediated bone resorption, while few others have an anabolic effect. Inhibition of bone resorption by currently available agents does not restore bone structure or bone that has already been lost and it is coupled with inhibition of bone formation. The identification of new pathways involved in bone turnover, will accelerate clinical research to develop new formation-stimulating and resorption-inhibiting agents with improved safety profile and efficacy in fracture prevention in osteoporosis. In the light of new data, it is estimated that novel antiosteoporotic compounds will increase considerably in the coming years. Turk J Phys Med Rehab 2011;57:165-71.