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QuickView for Cinacalcet (compound)

Name: cinacalcet
PubChem Compound ID: 156418
Molecular formula: C22H23ClF3N
Molecular weight: 393.873 g/mol
KRN-1493; 364782-34-3; 226256-56-0; N-((1R)-1-(Naphthalen-1-yl)ethyl)-3-(3-(trifluoromethyl)phenyl)propan-1-amine hydrochloride; AMG-073; Cinacalcet hydrochloride; Mimpara; AMG073 HCl; Cinacalcet hydrochloride (JAN/USAN); D03505.
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Name: cinacalcet
Name (isomeric): DB01012
Drug Type: small molecule
Brand: Sensipar
Category: Calcimimetics
CAS number: 226256-56-0
Indication: For the treatment of secondary hyperparathyroidism in patients with Chronic Kidney Disease who are on hemodialysis or peritoneal dialysis. Also for the treatment of hypercalcemia in patients with parathyroid carcinoma.
Cinacalcet is a drug that acts as a calcimimetic (i.e. it mimics the action of calcium on tissues). Secondary hyperparathyroidism (HPT) in patients with chronic kidney disease (CKD) is a progressive disease, associated with increases in parathyroid hormone (PTH) levels and derangements in calcium and phosphorus metabolism. Increased PTH stimulates ...
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Mechanism of Action:
The calcium-sensing receptors on the surface of the chief cell of the parathyroid gland is the principal regulator of parathyroid hormone secretion (PTH). Cinacalcet directly lowers parathyroid hormone levels by increasing the sensitivity of the calcium sensing receptors to activation by extracellular calcium, resulting in the inhibition of PTH sec...
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Absorption: Rapidly absorbed following oral administration.
Protein binding: Approximately 93 to 97% bound to plasma proteins.
Biotransformation: Metabolism is hepatic by multiple enzymes, primarily CYP3A4, CYP2D6, and CYP1A2. After administration of a 75 mg radiolabeled dose to healthy volunteers, cinacalcet was rapidly and extensively metabolized via: 1) oxidative N-dealkylation to hydrocinnamic acid and hydroxy-hydrocinnamic acid, which are further metabolized via ß-oxidation and glycine conjugation; the oxidative N-dealkylation process also generates metabolites that contain the naphthalene ring; and 2) oxidation of the naphthalene ring on the parent drug to form dihydrodiols, which are further conjugated with glucuronic acid.
Route of elimination: Cinacalcet is metabolized by multiple enzymes, primarily CYP3A4, CYP2D6 and CYP1A2. Renal excretion of metabolites was the primary route of elimination of radioactivity.
Half Life: Terminal half-life is 30 to 40 hours. The mean half-life of cinacalcet is prolonged by 33% and 70% in patients with moderate and severe hepatic impairment, respectively.
Toxicity: Doses titrated up to 300 mg once daily have been safely administered to patients on dialysis. Overdosage of cinacalcet may lead to hypocalcemia.
Affected organisms: Humans and other mammals
Food interaction:
Peak levels and area under curve (drug exposure) are increased (82% and 68% respectively) when product is taken with a lipid-rich meal.
Take with food or soon after a meal.
Food markedly increases product bioavailability.
Drug interaction:
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of cinacalcet by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of cinacalcet if voriconazole is initiated, discontinued or dose changed.
ErythromycinThe macrolide, erythromycin, may increase the serum concentration and toxicity of cinacalcet.
TolterodineCinacalcet may decrease the metabolism and clearance of Tolterodine. Monitor for adverse/toxic effects of Tolterodine.
KetoconazoleKetoconazole may increase the effect and toxicity of cinacalcet.
TelithromycinTelithromycin may reduce clearance of Cinacalcet. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Cinacalcet if Telithromycin is initiated, discontinued or dose changed.
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