Name: | cinacalcet |
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PubChem Compound ID: | 156418 |
Molecular formula: | C22H23ClF3N |
Molecular weight: | 393.873 g/mol |
Synonyms: |
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 |
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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. |
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Pharmacology: |
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: |
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