A calcimimetic is a

pharmaceutical drug A medication (also called medicament, medicine, pharmaceutical drug, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy ( pharmacotherapy) is an important part of the medical field and ...

that mimics the action of

calcium Calcium is a chemical element with the symbol Ca and atomic number 20. As an alkaline earth metal, calcium is a reactive metal that forms a dark oxide-nitride layer when exposed to air. Its physical and chemical properties are most similar t ...

on tissues, by

allosteric activation In biochemistry, allosteric regulation (or allosteric control) is the regulation of an enzyme by binding an effector molecule at a site other than the enzyme's active site. The site to which the effector binds is termed the ''allosteric sit ...

of the

calcium-sensing receptor The calcium-sensing receptor (CaSR) is a Class C G-protein coupled receptor which senses extracellular levels of calcium ions. It is primarily expressed in the parathyroid gland, the renal tubules of the kidney and the brain. In the parathyroid ...

that is expressed in various human organ tissues. Calcimimetics are used to treat

secondary hyperparathyroidism Secondary hyperparathyroidism is the medical condition of excessive secretion of parathyroid hormone (PTH) by the parathyroid glands in response to hypocalcemia (low blood calcium levels), with resultant hyperplasia of these glands. This disorder ...

(SHPT). William G. Goodman, "Calcimimetic agents and secondary hyperparathyroidism: treatment and prevention" ''Nephrology Dialysis Transplantation'' (2002) 17: 204-207.
/ref> In the treatment of SHPT patients on dialysis calcimimetics does not appear to affect the risk of early death. It does decrease the need for a

parathyroidectomy Parathyroidectomy is the surgical removal of one or more of the (usually) four parathyroid glands. This procedure is used to remove an adenoma or hyperplasia of these glands when they are producing excessive parathyroid hormone (PTH): hyperparathy ...

but caused more issues with low blood calcium levels and

vomiting Vomiting (also known as emesis and throwing up) is the involuntary, forceful expulsion of the contents of one's stomach through the mouth and sometimes the nose. Vomiting can be the result of ailments like food poisoning, gastroenteri ...

. Cinacalcet was the first calcimimetic to be approved. Cinacalcet mimics calcium at the

parathyroid hormone receptor There are two known parathyroid hormone receptors in mammals termed PTH1R and PTH2R. These receptors bind parathyroid hormone and are members of the GPCR family of transmembrane proteins. * parathyroid hormone 1 receptor (PTH1R) is the clas ...

. This binding will increase the sensitivity of

s (CaSR) on the parathyroid gland. As a result of the receptor "thinking" there is sufficient calcium,

parathyroid hormone Parathyroid hormone (PTH), also called parathormone or parathyrin, is a peptide hormone secreted by the parathyroid glands that regulates the serum calcium concentration through its effects on bone, kidney, and intestine. PTH influences bone r ...

(PTH) secretion will be reduced. Lower calcium levels will be seen as well. On August 25, 2015

Amgen Amgen Inc. (formerly Applied Molecular Genetics Inc.) is an American multinational biopharmaceutical company headquartered in Thousand Oaks, California. One of the world's largest independent biotechnology companies, Amgen was established in ...

Inc. announced that it had submitted a new drug application with the

United States Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a federal agency of the Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food s ...

for a new calcimimetic, etelcalcetide (formerly velcalcetide), for the treatment of SHPT in

chronic kidney disease Chronic kidney disease (CKD) is a type of kidney disease in which a gradual loss of kidney function occurs over a period of months to years. Initially generally no symptoms are seen, but later symptoms may include leg swelling, feeling tired, ...

(CKD) patients on hemodialysis. Etelcalcetide is administered intravenously thrice weekly at the end of each dialysis session. Etelcalcetide binds to the CaSR on the parathyroid gland, which results in receptor activation and ultimately reduction in PTH. Calcimimetics can be used concomitantly with

vitamin D Vitamin D is a group of fat-soluble secosteroids responsible for increasing intestinal absorption of calcium, magnesium, and phosphate, and many other biological effects. In humans, the most important compounds in this group are vitamin D3 ...

therapy. Calcimimetic use can have

side effects In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequence ...

. Common side effects include:

nausea Nausea is a diffuse sensation of unease and discomfort, sometimes perceived as an urge to vomit. While not painful, it can be a debilitating symptom if prolonged and has been described as placing discomfort on the chest, abdomen, or back of the ...

and

hypocalcemia Hypocalcemia is a medical condition characterized by low calcium levels in the blood serum. The normal range of blood calcium is typically between 2.1–2.6 mmol/L (8.8–10.7 mg/dL, 4.3–5.2 mEq/L) while levels less than 2.1 mm ...

, and adynamic bone disease if intact parathyroid hormone (iPTH) levels drop below 100pg/mL.

References

Systemic hormonal preparations Receptor agonists {{systemic-hormonal-drug-stub