Abstract
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▲ Oral cinacalcet hydrochloride (HCl) [Sensipar®, Mimpara®] is the first in a new class of therapeutic agents, the calcimimetics, and has a novel mechanism of action. It directly modulates the principal regulator of parathyroid hormone (PTH) secretion, namely the calcium-sensing receptor (CaR) on the chief cells in the parathyroid gland. Cinacalcet HCl reduces circulating PTH levels by increasing the sensitivity of the CaR to extracellular calcium.
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▲ In three pivotal phase III, 26-week, randomised, double-blind, multicentre trials in chronic kidney disease (CKD) patients (n = 1136) on dialysis with uncontrolled secondary hyperparathyroidism (HPT), a significantly higher proportion of oral cinacalcet HCl 30–180 mg/day than placebo recipients achieved a reduction in intact PTH levels to ≤250 pg/mL. Cinacalcet HCl treatment also simultaneously lowered serum calcium and phosphorus, and calcium-phosphorous product levels.
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▲ Notably, cinacalcet HCl proved effective in a broad range of CKD patients on dialysis with uncontrolled secondary HPT, regardless of disease severity, duration of dialysis treatment, dialysis modality, race, age, gender, or concurrent phosphate binder or vitamin D sterol use.
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▲ Cinacalcet HCl (60–360 mg/day) also reduced elevated serum calcium levels by ≥1 mg/dL in 15 of 21 (71%) patients with parathyroid carcinoma in an open-label, multicentre, dose-titration trial.
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▲ Cinacalcet HCl was generally well tolerated in clinical trials. Most treatment-emergent adverse events were mild to moderate in severity.
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Balfour, J.A.B., Scott, L.J. Cinacalcet Hydrochloride. Drugs 65, 271–281 (2005). https://doi.org/10.2165/00003495-200565020-00007
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DOI: https://doi.org/10.2165/00003495-200565020-00007