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Cinacalcet

西那卡塞

Mechanism of action:

Cinacalcet 是一種鈣感受器正向變構調節劑(calcimimetic agent),主要作用於副甲狀腺主細胞(parathyroid chief cell)上的鈣離子感受器(calcium-sensing receptor,CaSR),用於降低血中副甲狀腺素(parathyroid hormone,PTH)濃度。副甲狀腺主細胞膜上具有鈣離子感受器,負責偵測血液中鈣離子濃度,並調節副甲狀腺素分泌。若血鈣濃度高,副甲狀腺素分泌會降低;若血鈣濃度低,副甲狀腺素分泌會提升。Cinacalcet 可正向變構調節(positive allosteric modulator)鈣離子感受器,使其對鈣離子敏感度上升,即使血中鈣濃度正常或略低,鈣離子感受器仍會活化,以抑制副甲狀腺素的分泌。

​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.

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