tecalcet

Tecalcet (NPS R-568) is a **phenylalkylamine small molecule** classified as a **type II calcimimetic**. It is a selective, orally active **positive allosteric modulator (agonist) of the calcium-sensing receptor (CaSR)** on parathyroid cells, where it potentiates the actions of extracellular calcium. By increasing the sensitivity of the CaSR, tecalcet suppresses parathyroid hormone (PTH) secretion and reduces plasma calcium levels. The compound acts with high selectivity, showing minimal off-target effects on other G protein-coupled receptors and is 10- to 100-fold more potent as the R-enantiomer than the S-enantiomer. In addition to lowering PTH and calcium, tecalcet can also stimulate calcitonin secretion at higher doses, contributing to its hypocalcemic effects. Initially developed by NPS Pharmaceuticals, it has mainly been investigated for conditions associated with abnormal calcium and PTH homeostasis, including secondary hyperparathyroidism and chronic kidney disease[1][3][4][8][9].

Brand names

TecalcetNorcalcin

Other names

2-chloro-N-[(1R)-1-(3-methoxyphenyl)ethyl]-benzenepropanamineN-(3-[2-chlorophenyl]propyl)-(R)-alpha-methyl-3-methoxybenzylamine