Cinacalcet

Mechanism of action:
Cinacalcet is a calcimimetic agent that acts as a positive allosteric modulator of the calcium-sensing receptor (CaSR) on parathyroid chief cells and is used to reduce blood levels of parathyroid hormone (PTH). The membranes of parathyroid chief cells contain calcium-sensing receptors that detect blood calcium concentration and regulate parathyroid hormone secretion. When blood calcium is high, parathyroid hormone secretion decreases. When blood calcium is low, parathyroid hormone secretion increases. Cinacalcet positively allosterically modulates the calcium-sensing receptor, increasing its sensitivity to calcium ions. As a result, even when blood calcium concentration is normal or slightly low, the receptor remains activated and suppresses parathyroid hormone secretion.
Reference(s):
1. Torres PU et al. (2006). Cinacalcet HCl: a novel treatment for secondary hyperparathyroidism caused by chronic kidney disease. J Ren Nutr.
2. Padhi D et al. (2009). Clinical pharmacokinetic and pharmacodynamic profile of cinacalcet hydrochloride. Clin Pharmacokinet.
