Description
Cinacalcet (226256-56-0) is the first type II calcimimet ic agent approved that improves CaSR sensi Tivity to calcium .
When calcium is bound to the CaSR, phospholipase C is act ivated, and the secretion of PTH is inhibited. In the
presence of cinacalcet , not only is a drop in
PTH levels observed but also a decrease in serum calcium and phosphorous levels.
Chemical Properties
Yellow Oil
Uses
Cinacalcet(226256-56-0) is the first calcimimetic drug approved by the United States Food and Drug Administration for the treatment of secondary hyperparathyroidism in patients with chronic kidney disease
Uses
Labeled Cinacalcet, intended for use as an internal standard for the quantification of Cinacalcet by GC- or LC-mass spectrometry.
Uses
macular degeneration therapy
Definition
ChEBI: A secondary amino compound that is (1R)-1-(naphthalen-1-yl)ethanamine in which one of the hydrogens attached to the nitrogen is substituted by a 3-[3-(trifluoromethyl)phenyl]propyl group.
Brand name
Sensipar (Amgen).
Clinical Use
Cinacalcet hydrochloride(226256-56-0) is a second-generat ion calcimimetic approved for the treatment of secondary
hyperparathyroidism in patients wi th chronic kidney disease on dialysis and for the treatment of hypercalcemia
in patients with parathyroid cancer . It can be used alone, with vitamin D, and/or with a phosphate binder .
Side effects
Common side effects of Cinacalcet(226256-56-0) are nausea, vomiting, dizziness, diarrhoea and loss of appetite.Cinacalcet can cause hypocalcaemia. Patients taking this medication need to be followed closely for common symptoms associated with hypocalcaemia, including tingling, muscle twitching, cramps, mood changes or irritability. On the ECG, there may be a prolonged QT interval. Patients with a history of congenital long QT syndrome, a family history of long QT syndrome, and other conditions predisposing them to prolonged QT intervals may be at increased risk. PTH oversupport can lead to ankylosing bone disease.
Drug interactions
Potentially hazardous interactions with other drugs
Antifungals: metabolism inhibited by ketoconazole.
Hormone antagonists: metabolism of tamoxifen to
active metabolite inhibited - avoid.
Tobacco: metabolism increased by tobacco.
Metabolism
Cinacalcet is rapidly and extensively metabolised by
cytochrome P450 isoenzymes CYP3A4 and CYP1A2, by
oxidation followed by conjugation. The major circulating
metabolites are inactive, and are renally excreted, with
80% of the dose recovered in the urine, and 15% in the
faeces.
