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molecules of the month

Upacicalcet

IV CaSR agonist

Ph. III candidate in secondary hyperparathyroidism

identified from "kokumi-flavor" studies of peptides

Mol. Pharmacol.

Sanwa Kagaku Kenkyusho, Mie, JP

Upacicalcet chemical structure IV CaSR agonist - Sanwa Kagaku Kenkyusho, Mie, JP
3 mins read

Context. Upacicalcet (Sanwa Kagaku Kenkyusho Co) is a calcium-sensing receptor (CaSR) agonist being developed for secondary hyperparathyroidism (SHPT). The IV drug, first identified in "kokumi-flavor" studies of γ-glutamyl peptides, was approved for SHPT in Japan in 2021 and is currently being developed for the US and other markets. Upacicalcet, like other calcimimetics, acts as a positive allosteric modulator of CaSR and activates the expression of parathyroid hormone. However, unlike the other drugs, such as the widely studied cinacalcet and the recently approved etelcalcetide, upacicalcet has a unique binding method resulting in strong positive allosteric activity. Sanwa Kagaku Kenkyusho scientists believe that this novel binding mode will make the drug a new option for patients whose existing therapies are ineffective, such…


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