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Calcium sensing receptor activators: calcimimetics.

Paul E Harrington1, Christopher Fotsch

  • 1Department of Chemistry Research and Discovery, Amgen, Inc., One Amgen Center Dr., Thousand Oaks, CA 91320-1799, USA. pharring@amgen.com.

Current Medicinal Chemistry
|January 29, 2008
PubMed
Summary
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New calcimimetics, like cinacalcet HCl, enhance calcium sensing receptor (CaR) sensitivity. These drugs lower parathyroid hormone (PTH) levels, offering treatments for hyperparathyroidism.

Area of Science:

  • Endocrinology
  • Pharmacology
  • Molecular Biology

Background:

  • The calcium sensing receptor (CaR), a G protein-coupled receptor (GPCR), is crucial for maintaining serum calcium homeostasis.
  • It is expressed on parathyroid chief cells, regulating parathyroid hormone (PTH) secretion, which impacts bone, kidney, and intestine.
  • Elevated PTH levels characterize disorders like primary and secondary hyperparathyroidism (HPT).

Purpose of the Study:

  • To review the discovery and development of calcimimetics, particularly type II agents.
  • To discuss cinacalcet HCl (Sensipar/Mimpara) as a key therapeutic example.
  • To highlight other recently identified type II calcimimetics.

Main Methods:

  • Review of scientific literature on CaR agonists and allosteric modulators.

Related Experiment Videos

  • Analysis of the mechanism of action for type II calcimimetics.
  • Discussion of clinical relevance and therapeutic potential.

    • Main Results:

    • Type I calcimimetics act as direct agonists of the CaR.
    • Type II calcimimetics act as positive allosteric modulators, amplifying CaR sensitivity to calcium.
    • This amplification leads to reduced PTH secretion, lowering serum calcium levels.

    Conclusions:

    • Calcimimetics, especially type II, are promising therapeutic agents for hyperparathyroidism.
    • Cinacalcet HCl represents a successful example of type II calcimimetic development.
    • Ongoing research into novel type II calcimimetics may offer improved treatments for PTH disorders.