CASR binds CASR agonists

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Reaction [binding]
Homo sapiens
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Patients with chronic kidney disease often develop secondary hyperparathyroidism (SHPT), marked by high levels of circulating parathyroid hormone (PTH) and increased risk of morbidity and mortality. A novel peptide, etelcalcetide (AMG 416), acts as an agonist of the calcium-sensing receptor (CaSR). Etelcalcetide activates the human CaSR in vitro and reduces serum parathyroid hormone and FGF23 levels in healthy male subjects (Walter et al. 2013, Martin et al. 2014). As a long-acting CaSR agonist, etelcalcetide is an innovative new therapy for the treatment of hemodialysis patients with secondary hyperparathyroidism (Patel & Bridgeman 2018) instead of the conventional calcimimetic cinacalcet. Evocalcet is another calcium-sensing receptor (CASR) agonist recently approved in Japan for the treatment of secondary hyperparathyroidism in dialysis patients (Kawata et al. 2018, Akizawa et al. 2019). Cinacalcet, an oral calcimimetic, binds to the transmembrane domain of the CaSR and decreases PTH, calcium, and phosphorus levels. It is used to treat hyperparathyroidism due to parathyroid tumours or renal failure (Block et al. 2010, Chertow et al. 2012, Raggi et al. 2011, Akizawa et al. 2016).
Literature References
PubMed ID Title Journal Year
21148030 The ADVANCE study: a randomized study to evaluate the effects of cinacalcet plus low-dose vitamin D on vascular calcification in patients on hemodialysis

Dehmel, B, Nossuli, K, Downey, G, Moustafa, M, Floege, J, ADVANCE Study Group, -, Naso, A, Torres, PU, Chertow, GM, Csiky, B, Raggi, P, Goodman, WG, Lopez, N

23121374 Effect of cinacalcet on cardiovascular disease in patients undergoing dialysis

Trotman, ML, Mix, TC, Parfrey, PS, Kubo, Y, Floege, J, Moe, SM, Chertow, GM, Mahaffey, KW, Block, GA, Herzog, CA, Correa-Rotter, R, EVOLVE Trial Investigators, -, Dr├╝eke, TB, Goodman, WG, Wheeler, DC, London, GM

29614098 A novel calcimimetic agent, evocalcet (MT-4580/KHK7580), suppresses the parathyroid cell function with little effect on the gastrointestinal tract or CYP isozymes in vivo and in vitro

Fukagawa, M, Akizawa, T, Miyazaki, H, Tokunaga, S, Haruyama, W, Hisada, Y, Masuda, N, Wada, M, Yanagida, T, Shoukei, Y, Murai, M, Kawata, T

23674604 Pharmacology of AMG 416 (Velcalcetide), a novel peptide agonist of the calcium-sensing receptor, for the treatment of secondary hyperparathyroidism in hemodialysis patients

Baruch, A, Janes, J, Johnson, RM, Hunter, T, Bell, G, Karim, F, Dong, J, Walter, S, Tomlinson, JE, Maclean, D, Yin, Q, Alexander, ST, Mendel, DB

20555319 Cinacalcet hydrochloride treatment significantly improves all-cause and cardiovascular survival in a large cohort of hemodialysis patients

Block, GA, St Peter, WL, Nieman, K, Liu, J, Zaun, D, Persky, M, Smits, G, Brillhart, S

27071541 PTH-dependence of the effectiveness of cinacalcet in hemodialysis patients with secondary hyperparathyroidism

Fukagawa, M, Yamaguchi, T, Hasegawa, T, Akizawa, T, Alan Brookhart, M, Kurokawa, K, Fukuma, S, Onishi, Y, Ellis, AR, Fukuhara, S, Mizobuchi, M, Kurita, N

24235081 Velcalcetide (AMG 416), a novel peptide agonist of the calcium-sensing receptor, reduces serum parathyroid hormone and FGF23 levels in healthy male subjects

Peacock, M, Hodsman, P, Bell, G, Vick, A, Huang, S, Martin, KJ, Pickthorn, K

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