Cinacalcet is an oral calcimimetic drug used to treat secondary hyperparathyroidism in dialysis patients, hypercalcemia in parathyroid carcinoma, and primary hyperparathyroidism when surgery is not suitable. Developed by Amgen in the late 1990s and approved by the FDA in 2004, it represented a major advancement in non-surgical management of elevated parathyroid hormone (PTH) and calcium levels. Cinacalcet works by allosterically activating the calcium-sensing receptor (CaSR) on parathyroid cells, increasing their sensitivity to extracellular calcium, which suppresses PTH secretion and helps maintain calcium and phosphate balance. The drug is well absorbed orally, extensively metabolized in the liver, and primarily excreted via the feces, with a relatively long half-life that allows once-daily dosing in many cases. Its introduction offered a safer, targeted alternative to previous treatments like vitamin D analogs, phosphate binders, or surgical intervention, marking a significant milestone in endocrine and renal therapeutics.
