Calcimimetics and hyperparathyroidism.

The calcium-sensing receptor (CaSR) is a key regulator of parathyroid hormone (PTH) secretion and parathyroid proliferation. This review discusses the role of the CaSR in hyperparathyroidism (HPT), and the exploitation of the CaSR as a therapeutic target for the treatment of HPT. Calcimimetics act as CaSR agonists or allosteric activators and thereby potentiate the effects of extracellular Ca2+ on parathyroid cell function. Results from clinical trials using calcimimetics to treat primary and secondary HPT, as well as primary HPT from parathyroid carcinoma, suggest that calcimimetic compounds could provide an effective alternative or additional therapeutic approach for various forms of HPT.