Bisphosphonates: From Pharmacology to Treatment

Bisphosphonates are among the most widely used drugs in the world for their many clinical indications. Their mechanism of action is based on the increase in the level of bone mineralization through the inhibition of osteoclastic activity and the induction of osteoblastic activity. Recent studies also attribute to bisphosphonates an antineoplastic activity, due to the ability of these drugs to inhibit neo angiogenesis, inhibiting the proliferation of endothelial cells. Bisphosphonates have several common properties, including poorly absorbed orally, high affinity for bone mineral, inhibitory effects on osteoclastic bone resorption, prolonged bone retention, and elimination in the urine. Bisphosphonates are generally well tolerated but their use can be, however, burdened by serious side effects such as hypocalcaemia, renal impairment, and aseptic osteonecrosis of the jaw.