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Abstract
Introduction: The identification and cloning of the calcium-sensing receptor (CaSR) in 1993 has enhanced our understanding of calcium metabolism in both health and disease. CaSR, a G protein-coupled receptor, serves as a key signal transduction pathway in a variety of tissues, most notably parathyroid and kidney. The development of agents that activate the CaSR (calcimimetics) has provided for a new approach for the treatment of hyperparathyroidism, especially secondary hyperparathyroidism that is a common complication of chronic kidney disease.
Areas covered: This review provides an overview of the CaSR and calcimimetics as well as a detailed discussion about pharmacokinetics, clinical efficacy, safety profile and the clinical indications for the use of cinacalcet.
Expert opinion: Cinacalcet is presently the only calcimimetic agent approved for the treatment of secondary hyperparathyroidism in dialysis patients. It is also indicated for hypercalcemia due to inoperable parathyroid carcinoma-related parathyroid hormone excess and severe primary hyperparathyroidism in whom surgery is indicated but cannot be performed.