Cinacalcet hydrochloride - CAS 364782-34-3
Catalog number: 364782-34-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C22H22F3N.HCl
Molecular Weight:
393.87
COA:
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Targets:
CaSR
Description:
Cinacalcet HCl represents a new class of compounds for the treatment of hyperparathyroidism.
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Purity:
>98%
Synonyms:
AMG-073 HCl
MSDS:
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1.Cinacalcet, dialysate calcium concentration, and cardiovascular events in the EVOLVE trial.
Pun PH1, Abdalla S2, Block GA3, Chertow GM2, Correa-Rotter R4, Dehmel B5, Drüeke TB6, Floege J7, Goodman WG5, Herzog CA8, London GM9,10, Mahaffey KW2, Moe SM9,10, Parfrey PS11, Wheeler DC12, Middleton JP1. Hemodial Int. 2015 Nov 13. doi: 10.1111/hdi.12382. [Epub ahead of print]
Among patients receiving hemodialysis, abnormalities in calcium regulation have been linked to an increased risk of cardiovascular events. Cinacalcet lowers serum calcium concentrations through its effect on parathyroid hormone secretion and has been hypothesized to reduce the risk of cardiovascular events. In observational cohort studies, prescriptions of low dialysate calcium concentration and larger observed serum-dialysate calcium gradients have been associated with higher risks of in-dialysis facility or peri-dialytic sudden cardiac arrest. We performed this study to examine the risks associated with dialysate calcium and serum-dialysate gradients among participants in the Evaluation of Cinacalcet Hydrochloride Therapy to Lower Cardiovascular Events (EVOLVE) trial. In EVOLVE, 3883 hemodialysis patients were randomized 1:1 to cinacalcet or placebo. Dialysate calcium was administered at the discretion of treating physicians. We examined whether baseline dialysate calcium concentration or the serum-dialysate calcium gradient modified the effect of cinacalcet on the following adjudicated endpoints: (1) primary composite endpoint (death or first non-fatal myocardial infarction, hospitalization for unstable angina, heart failure, or peripheral vascular event); (2) cardiovascular death; and (3) sudden death.
2.Development and Validation of a Stability-Indicating RP-UPLC Method for the Estimation of Impurities in Cinacalcet Hydrochloride API and its Formulation.
Sunil Reddy P1, Raju TV1, Raju PS1, Varma NS1, Babu KS2. Sci Pharm. 2015 Apr 16;83(4):583-98. doi: 10.3797/scipharm.1502-06. eCollection 2015.
A sensitive, stability-indicating, gradient reversed-phase ultra-performance liquid chromatography method has been developed for the quantitative estimation of cinacalcet hydrochloride impurities in active pharmaceutical ingredients and pharmaceutical formulations. Efficient chromatographic separation was achieved on an Acquity BEH Shield RP18, 100 × 2.1 mm, 1.7 µm column with the mobile phase containing pH 6.6 phosphate buffer and acetonitrile. The flow rate of the mobile phase was 0.3 mL min(-1) with a column temperature of 35°C and detection wavelength at 223 nm. The relative response factor values of (+)-R-1-(1-Naphthyl)ethylamine, regioisomer, diastereomer isomer-1, and diastereomer isomer-2 were 1.79, 0.99, 0.89, and 0.88, respectively. The cinacalcet hydrochloride formulation sample was subjected to the stress conditions of acid, base, oxidative, hydrolytic, thermal, humidity, and photolytic degradation. Cinacalcet hydrochloride was found to degrade significantly under the peroxide stress conditions.
3.Economic Evaluation of Cinacalcet in the United States: The EVOLVE Trial.
Belozeroff V1, Chertow GM2, Graham CN3, Dehmel B4, Parfrey PS5, Briggs AH6. Value Health. 2015 Dec;18(8):1079-87. doi: 10.1016/j.jval.2015.08.007. Epub 2015 Oct 9.
BACKGROUND: Previous economic evaluations of cinacalcet in patients with secondary hyperparathyroidism (sHPT) relied on the combination of surrogate end points in clinical trials and epidemiologic studies.
4.The effects of cinacalcet treatment on bone mineral metabolism, anemia parameters, left ventricular mass index and parathyroid gland volume in hemodialysis patients with severe secondary hyperparathyroidism.
Torun D1, Yildiz I, Micozkadioglu H, Nursal GN, Yigit F, Ozelsancak R. Saudi J Kidney Dis Transpl. 2016 Jan;27(1):15-22. doi: 10.4103/1319-2442.174053.
The aim of this study was to investigate the effects of cinacalcet therapy on anemia parameters, bone mineral metabolism, left ventricular mass index (LVMI) and parathyroid gland volume in hemodialysis (HD) patients with secondary hyperparathyroidism. Twenty-five HD patients (M/F: 11/14, mean age: 45.2±17.9 years, mean HD duration: 96.4±32.7 months) were included in this prospective pilot study. The indication to start calcimimetic therapy was persistent serum levels of parathyroid hormone (PTH)>1000 pg/mL, refractory to intravenous (i.v.) vitamin D and phosphate-binding therapy. The initial and one-year results of adjusted serum calcium (Ca+2), phosphate (P), Ca×P product, PTH, hemoglobin (Hb) and ferritin levels, transferrin saturation index (TSAT), median weekly erythropoietin (EPO) dose, LVMI, and parathyroid volume by parathyroid ultrasonography were determined. There were no differences between pre- and post-treatment levels of serum Ca+2 (P=0.
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