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tecalcet (Kirin Holdings)
- Development stage
- Discontinued
- Lead developer
- Takeda
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Tecalcet (also known as A-568 or NPS R-568) is a first-generation, orally active small molecule calcimimetic that acts as a selective positive allosteric modulator of the calcium-sensing receptor (CaSR). Originally developed by NPS Pharmaceuticals in collaboration with Kirin Brewery and Amgen, tecalcet enhances the sensitivity of CaSR to extracellular calcium, thereby suppressing the secretion of parathyroid hormone (PTH). It was investigated in Phase II clinical trials for the treatment of primary and secondary hyperparathyroidism, postmenopausal osteoporosis, and rheumatic diseases. However, its clinical development was discontinued due to unfavorable pharmacokinetic properties, including low bioavailability and high variability in metabolism mediated by the polymorphic cytochrome P450 enzyme CYP2D6, leading to the development of second-generation calcimimetics like cinacalcet.
- Brand names
- Norcalcin
- Other names
- tecalcet hydrochloride
02
Targets
CaSR (Extracellular calcium-sensing receptor)
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