Theme |
Cinacalcet hydrochloride |
Title |
Development and present status of positive allosteric modulators of calcium receptor |
Author |
Nobuo Nagano |
Medical Affairs Department, Kirin Pharma Company, Limited |
Author |
Takayuki Furuta |
Discovery Research Laboratories, Kirin Pharma Company, Limited |
[ Summary ] |
Parathyroid cells can sense small fluctuations in plasma calcium ion levels by virtue of a cell surface calcium receptor (CaR) that belongs to the superfamily of G-protein-coupled receptors. Calcimimetics are positive allosreric modulators that activate parathyroid CaR and thereby immediately suppress parathyroid hormone secretion. Cinacalcet hydrochloride has recently been put on the Japanese market for treatment of secondary hyperparathyroidism in patients with chronic kidney disease on dialysis. Several pharmaceutical companies have been developing calcimimetics and it is intriguing to consider whether these compounds will be able to overcome the unfavorable properties of cinacalcet hydrochloride. |