<p>The Ca²⁺-sensing receptor (CaSR), a G-protein-coupled receptor activated by raised extracellular Ca²⁺ concentration, has been well studied for its role in regulating parathyroid hormone (PTH) secretion. As a calcimimetic and positive allosteric modulator of CaSR, cinacalcet activates parathyroid cell CaSR by increasing the latter’s sensitivity to Ca²⁺, causing a reduction in PTH secretion and thus serum Ca²⁺ level. Cinacalcet is clinically used to treat secondary hyperparathyroidism in chronic kidney disease patients and hypercalcemia in parathyroid cancer patients. Recently, cinacalcet has been explored experimentally to produce diverse effects such as diarrhea treatment, anticancer activities, treatment of kidney problems, antibacterial activities, improvement of hematopoietic stem cell transplantation, cardioprotective and neuroprotective effects. Remarkably, in these repurposing studies, CaSR-dependent actions of cinacalcet were demonstrated in some but not all reports; indeed, a CaSR-independent mechanism has been demonstrated for some cinacalcet effects. This review summarizes cinacalcet’s diverse pharmacological and potential therapeutic effects other than treatment of hypercalcemia and finally discusses the precautions and possible protocols in repurposing this drug.</p>