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Therapeutic use of calcimimetics
1Department of Cellular and Molecular Physiology, Yale University School of Medicine, New Haven, Connecticut 06520-8026, USA. steven.hebert@yale.edu
Annual Review of Medicine
|January 18, 2006
Summary
The calcium-sensing receptor (CaSR) regulates parathyroid hormone (PTH) secretion. Modulating CaSR activity with calcimimetics and calcilytics offers new therapies for calcium disorders like hyperparathyroidism and osteoporosis.
Area of Science:
- Endocrinology
- Molecular Biology
- Pharmacology
Background:
- Parathyroid hormone (PTH) secretion is regulated by extracellular calcium.
- The calcium-sensing receptor (CaSR), cloned in 1993, mediates this calcium sensing.
- CaSR is a G protein-coupled receptor crucial for calcium homeostasis.
Purpose of the Study:
- To review the role of the CaSR in regulating PTH secretion and calcium homeostasis.
- To discuss the therapeutic potential of CaSR modulators (calcimimetics and calcilytics).
Main Methods:
- Cloning of the CaSR gene.
- Genetic studies investigating CaSR function.
- Identification and characterization of CaSR agonists (calcimimetics) and antagonists (calcilytics).
Main Results:
- CaSR activity dictates plasma calcium levels by regulating calcium homeostasis.
- Calcimimetics effectively reduce PTH secretion in hyperparathyroidism.
- Calcilytics show potential for increasing PTH and treating osteoporosis.
Conclusions:
- The CaSR is a key regulator of calcium homeostasis and PTH secretion.
- Calcimimetics represent a significant therapeutic strategy for hyperparathyroidism, especially in renal failure.
- Calcilytics offer a promising future therapeutic avenue for conditions like osteoporosis.
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