Cinacalcet

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 (Van Wagenen et al. (2001), U.S. Pat. 6,211,244). 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. Cinacalcet was FDA approved in March 2004, and was the first allosteric G protein-coupled receptor modulator to enter the pharmaceutical market. In 2014, cinacalcet was 76th out of the top 100 drugs in the list of largest selling pharmaceutical products. 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 (Van Wagenen et al. (2001), U.S. Pat. 6,211,244). 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. Cinacalcet was FDA approved in March 2004, and was the first allosteric G protein-coupled receptor modulator to enter the pharmaceutical market. In 2014, cinacalcet was 76th out of the top 100 drugs in the list of largest selling pharmaceutical products. Cinacalcet is indicated for the treatment of tertiary hyperparathyroidism in people with chronic kidney disease on dialysis and hypercalcemia in people with parathyroid carcinoma. Cinacalcet can also be used to treat severe hypercalcemia in patients with primary hyperparathyroidism who are unable to undergo parathyroidectomy. In the treatment of tertiary hyperparathyroidism due to chronic kidney disease on dialysis it does not appear to affect mortality. It does decrease the need for a parathyroidectomy but can cause more issues with low blood calcium levels. Cinacalcet has pregnancy category C in the US, meaning that adequate and well-controlled studies involving cinacalcet in pregnant women have not been done. Studies have not been done in lactating women; therefore it is not known whether cinacalcet is excreted into human milk. Hypocalcemia (decreased calcium levels) is a contraindication of cinacalcet. Patients who have serum calcium levels less than 7.5 mg/dL should not be started on cinacalcet. Hypocalcemia symptoms include parathesias, myalgias, muscle cramping, tetany, and convulsions. Cinacalcet should not be administered until serum calcium levels are above 8.0 mg/dL and/or hypocalcemia symptoms are resolved. Common side effects of cinacalcet include stomach upset, vomiting, diarrhea, dizziness, nausea, weakness, and chest pain. Clinical trials conducted in the United States by Amgen to determine whether the drug is safe in children were halted by the FDA in February 2013 following the death of a 14-year-old patient. Serious side effects, including overdose symptoms, of cinacalcet include: