Upacicalcet: First Approval

Upacicalcet (UPASITA^®) is an intravenous calcimimetic agent being developed by Sanwa Kagaku Kenkyusho, under license from EA Pharma, for the treatment of secondary hyperparathyroidism (SHPT), a common and early complication of chronic kidney disease, in patients undergoing haemodialysis. By acting directly on parathyroid cell membrane calcium-sensing receptors, upacicalcet suppresses excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels. Upacicalcet received its first approval on 23 June 2021 for the treatment of SHPT in adults undergoing haemodialysis in Japan. It is administered intravenously three times per week into the venous side of the haemodialysis circuit at the time of blood return at the end of the haemodialysis session. The generally recommended starting dose of upacicalcet is 25 µg, with the dose adjusted within a 25-300 µg range based on PTH and serum calcium levels. This article summarizes the milestones in the development of upacicalcet leading to this first approval for the treatment of SHPT in patients undergoing haemodialysis.