[Cinacalcet - an allosteric enhancer at the Ca2+-receptor].
Cinacalcet (trade name: Mimpara) enhances allosterically the action of Ca (2+)-ions at the parathyroid gland Ca (2+)-receptor which belongs to the superfamily of G protein-coupled receptors. As a consequence blood levels of Ca (2+) and parathyroid hormone decline. Cinacalcet is orally administered and approved for a) the treatment of secondary hyperparathyroidism in patients with end stage renal disease receiving hemodialysis and b) to lower hypercalcemia in patients with parathyroid carcinoma. Therapeutic monitoring includes measurement of blood levels of Ca (2+) and parathyroid hormone. The stable suppression of parathyroid hormone levels under chronic treatment was shown in clinical trials. Clinically relevant outcome parameters, such as bone mass and fracture risk, remain to be evaluated.
Kebig
A
A
Pharmakologie und Toxikologie, Pharmazeutisches Institut, Rheinische Friedrich-Wilhelms-Universität Bonn.
Mohr
K
K
D002118:Calcium / Q000097:blood; D000069449:Cinacalcet; D016903:Drug Monitoring / Q000379:methods; D006801:Humans; D006934:Hypercalcemia / Q000188:drug therapy* / Q000209:etiology; D006962:Hyperparathyroidism, Secondary / Q000188:drug therapy* / Q000209:etiology; D007676:Kidney Failure, Chronic / Q000150:complications* / Q000628:therapy; D009281:Naphthalenes / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D010281:Parathyroid Hormone / Q000097:blood; D010282:Parathyroid Neoplasms / Q000150:complications*; D044169:Receptors, Calcium-Sensing / Q000819:agonists / Q000187:drug effects* / Q000378:metabolism; D006435:Renal Dialysis
D009281:Naphthalenes; D010281:Parathyroid Hormone; D044169:Receptors, Calcium-Sensing; D002118:Calcium; D000069449:Cinacalcet