|Trade names||Sensipar, Mimpara|
|Main uses||Secondary hyperparathyroidism, parathyroid carcinoma, primary hyperparathyroidism|
|Side effects||Nausea, upper GI bleeding, low calcium, low blood pressure, adynamic bone disease|
|Bioavailability||20 to 25%|
increases if taken with food
|Protein binding||93 to 97%|
|Metabolism||Liver (CYP3A4-, CYP2D6- and CYP1A2-mediated)|
|Elimination half-life||30 to 40 hours|
|Excretion||Kidney (80%) and fecal (15%)|
|Chemical and physical data|
|Molar mass||357.420 g·mol−1|
|3D model (JSmol)|
Cinacalcet, sold under the brand name Sensipar among others, is a medication used to treat secondary hyperparathyroidism, parathyroid carcinoma, and primary hyperparathyroidism. In secondary hyperparathyroidism, it is used in those who require dialysis; while in parathyroid carcinoma, it is used to treat high blood calcium. It is taken by mouth with food.
Common side effects include nausea and vomiting. Other side effects may include upper GI bleeding, low calcium, low blood pressure, and adynamic bone disease. It should not be used in people with low blood calcium. Safety in pregnancy is unclear. It is a calcimimetic, meaning that it mimics the action of calcium in the body.
Cinacalcet was approved in the United States and Europe in 2004. It is available as a generic medication. In the United States 30 pills of 30 mg costs about 17 USD as of 2022. This amount in the United Kingdom costs the NHS about £114.
In the United States, cinacalcet is indicated for the treatment of secondary 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 European Union cinacalcet is indicated for:
- the treatment of secondary hyperparathyroidism (HPT) in adults with end stage renal disease (ESRD) on maintenance dialysis therapy.
- the treatment of secondary hyperparathyroidism (HPT) in children aged three years and older with end stage renal disease (ESRD) on maintenance dialysis therapy in whom secondary HPT is not adequately controlled with standard of care therapy.
- part of a therapeutic regimen including phosphate binders and/or vitamin D sterols, as appropriate.
- the treatment of parathyroid carcinoma and primary hyperparathyroidism in adults.
- the reduction of hypercalcaemia in adults with:
It is used at a dose of 30 mg once per day up to 90 mg four times per day based on blood calcium levels.
Hypocalcemia (decreased calcium levels) is a contraindication of cinacalcet. Those 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. Cinacalcet is not approved for pediatric use in the United States.
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 U.S. Food and Drug Administration (FDA) in February 2013, following the death of a 14-year-old participant.
Pregnancy and breastfeeding
Serious side effects, including overdose symptoms, of cinacalcet include:
- unusual feelings of the lips, tongue, fingers, or feet
- muscle aches or cramps
- sudden tightening of muscles in hands, feet, face, or throat
Cinacalcet is a strong inhibitor of the liver enzyme CYP2D6 and is partially metabolized by CYP3A4 and CYP1A2. Dose adjustments may be necessary if people are treated with CYP3A4 and CYP1A2 inhibitors and medications that are metabolized by CYP2D6.
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 negative regulator of parathyroid hormone secretion. Cinacalcet increases the sensitivity of calcium receptors on parathyroid cells to reduce parathyroid hormone (PTH) levels and thus decrease serum calcium levels.
It was the first allosteric G protein-coupled receptor modulator to enter the pharmaceutical market.
Society and culture
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