Related Experiment Videos
Calcimimetic agents and the calcium-sensing receptor
1The Medical and Research Services, Veterans Affairs West Los Angeles Healthcare Center, CA 90073, USA.
Current Opinion in Nephrology and Hypertension
|April 11, 2000
Summary
Calcimimetics, like R-568, enhance calcium-sensing receptor sensitivity to lower parathyroid hormone. Early trials show R-568 effectively reduces parathyroid hormone and is well-tolerated in various hyperparathyroidism models.
Area of Science:
- Endocrinology and Molecular Biology
- Calcium Homeostasis Regulation
- G protein-coupled receptor signaling
Background:
- Blood ionized calcium is tightly regulated by the calcium-sensing receptor (CaSR).
- CaSR mutations cause hereditary disorders and are implicated in primary and secondary hyperparathyroidism.
- Parathyroid hormone (PTH) secretion and urinary calcium excretion are key CaSR-regulated processes.
Purpose of the Study:
- To evaluate the efficacy and tolerability of the first-generation calcimimetic, R-568.
- To investigate R-568's effect on parathyroid hormone levels in hyperparathyroidism models.
Main Methods:
- Administration of R-568 to animal models of secondary hyperparathyroidism.
- Clinical trials involving patients with primary hyperparathyroidism.
- Clinical trials involving patients with uremic secondary hyperparathyroidism.
Main Results:
- R-568 demonstrated effective suppression of parathyroid hormone levels.
- The calcimimetic R-568 was well-tolerated in all tested models and patient groups.
- Enhanced CaSR sensitivity by R-568 leads to reduced PTH secretion.
Conclusions:
- Calcimimetics represent a promising therapeutic strategy for hyperparathyroidism.
- R-568 shows potential for managing conditions associated with dysregulated calcium homeostasis.
- Targeting the calcium-sensing receptor offers a viable approach to control parathyroid hormone.