|Systematic (IUPAC) name|
|Licence data||EMA: , US FDA:|
|Pregnancy cat.||B3 (AU) C (US)|
|Legal status||℞ Prescription only|
|Bioavailability||20 to 25%
Increases if taken with food
|Protein binding||93 to 97%|
|Metabolism||Hepatic (CYP3A4-, CYP2D6- and CYP1A2-mediated)|
|Half-life||30 to 40 hours|
|Excretion||Renal (80%) and fecal (15%)|
|Mol. mass||357.412 g/mol|
|(what is this?)|
Cinacalcet (INN) is a drug that acts as a calcimimetic (i.e. it mimics the action of calcium on tissues) by allosteric activation of the calcium-sensing receptor that is expressed in various human organ tissues. It is sold by Amgen under the trade name Sensipar in North America and Australia and as Mimpara in Europe. Cinacalcet is used to treat secondary hyperparathyroidism (elevated parathyroid hormone levels), a consequence of end-stage renal disease. Cinacalcet is also indicated for the treatment of hypercalcemia in patients with parathyroid carcinoma.
Clinical trials conducted in the United States by Amgen to determine whether the drug is safe for children were halted by the FDA in February 2013 following the death of a 14-year-old patient.
Mechanism of action
Cinacalcet is a drug that acts as a calcimimetic (i.e. it mimics the action of calcium on tissues) by allosteric activation of the calcium-sensing receptor that is expressed in various human organ tissues. 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 increases the sensitivity of calcium receptors on parathyroid cells to reduce parathyroid hormone (PTH) levels and thus decrease serum calcium levels.  As receptors are already active from the calcimimetic (Cinacalcet) the native rise and fall of Ca levels now interact with the remaining receptors, effectively lowering the threshold for activation of feedback on the parathyroid chief cells.
B.C. Van Wagenen, S.T. Moe, M.F. Balandrin, E.G. DelMar, E.F. Nemeth, U.S. Patent 6,211,244 (2001).
- Torres PU (2006). "Cinacalcet HCl: a novel treatment for secondary hyperparathyroidism caused by chronic kidney disease". Journal of renal nutrition : the official journal of the Council on Renal Nutrition of the National Kidney Foundation 16 (3): 253–8. doi:10.1053/j.jrn.2006.04.010. PMID 16825031.
- "Sensipar for Parathyroid Carcinoma". Amgen. 2009. Retrieved 25 September 2009.
- Edney, Anna (February 26, 2013). "Amgen Pediatric Trials of Sensipar Halted by FDA After Death". Businessweek.
- 2014 Nurses Drug Handbook (13th ed.). Burlington, MA: Jones & Bartlett Learning. 2014. pp. 245–6. ISBN 978-1-284-03115-7.
- Sensipar website run by Amgen
- Prescribing information (package insert)
- Cinacalcet - Medlineplus.org
- Cinacalcet - Drug Digest.