Balcinrenone Explained

Legal Status:	Investigational
Synonyms:	AZD9977; AZD-9977
Cas Number:	1850385-64-6
Pubchem:	118599727
Unii:	6C9UKZ0CYE
Iupac Name:	2-[(3''S'')-7-Fluoro-4-(3-oxo-4''H''-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]-N-methylacetamide
C:	20
H:	18
F:	1
N:	3
O:	5

Balcinrenone is an experimental selective mineralocorticoid receptor modulator developed by AstraZeneca for heart failure. Compared to mineralocorticoid receptor antagonists, it is hoped to have less effect on electrolytes and therefore a lower risk of hyperkalemia.^{[1] [2] [3] [4] [5]}

Notes and References

1. Bamberg . Krister . Johansson . Ulrika . Edman . Karl . William-Olsson . Lena . Myhre . Susanna . Gunnarsson . Anders . Geschwindner . Stefan . Aagaard . Anna . Björnson Granqvist . Anna . Jaisser . Frédéric . Huang . Yufeng . Granberg . Kenneth L. . Jansson-Löfmark . Rasmus . Hartleib-Geschwindner . Judith . Preclinical pharmacology of AZD9977: A novel mineralocorticoid receptor modulator separating organ protection from effects on electrolyte excretion . PLOS ONE . 23 February 2018 . 13 . 2 . e0193380 . 10.1371/journal.pone.0193380 . 29474466 . 5825103 . 2018PLoSO..1393380B . free .
2. Bamberg . Krister . William-Olsson . Lena . Johansson . Ulrika . Jansson-Löfmark . Rasmus . Hartleib-Geschwindner . Judith . The selective mineralocorticoid receptor modulator AZD9977 reveals differences in mineralocorticoid effects of aldosterone and fludrocortisone . Journal of the Renin-Angiotensin-Aldosterone System . January 2019 . 20 . 1 . 147032031982744 . 10.1177/1470320319827449. 30813831 . 6396052 .
3. Whittaker . Andrew . Kragh . Åsa M. . Hartleib-Geschwindner . Judith . Albayaty . Muna . Backlund . Anna . Greasley . Peter J. . Heijer . Maria . Kjaer . Magnus . Forte . Pablo . Unwin . Robert . Wernevik . Linda . Ericsson . Hans . Safety, Tolerability, and Pharmacokinetics of the Mineralocorticoid Receptor Modulator AZD9977 in Healthy Men: A Phase I Multiple Ascending Dose Study . Clinical and Translational Science . March 2020 . 13 . 2 . 275–283 . 10.1111/cts.12705. 31584739 . 7070793 .
4. Squire . Iain B. . Gabrielsen . Anders . Greasley . Peter J. . Wernevik . Linda . Hartleib-Geschwindner . Judith . Holden . Julie . Johansson . Susanne . Rudvik . Anna . Sánchez . José . Bamberg . Krister . Melin . Johanna . Whittaker . Andrew . Effect of AZD9977 and spironolactone on serum potassium in heart failure with preserved or mildly reduced ejection fraction, and renal impairment: A randomized trial . Clinical and Translational Science . October 2022 . 15 . 10 . 2493–2504 . 10.1111/cts.13377. 35971596 . 9579384 .
5. Mallia . Carl J. . Le Bars . Joël . Hardy . Simon . Lamacraft . Alex . Harding . Simon . Hose . David . Snow . Lindsay . Poulten . Rebecca C. . Dobson . Benjamin C. . Churchill . Trevor . Gillespie . Paul M. . Control of Hydrogen Fluoride Formation and Release during a Large-Scale Nitroarene Reduction in the Manufacture of AZD9977 . Organic Process Research & Development . 20 January 2023 . 27 . 1 . 167–178 . 10.1021/acs.oprd.2c00323. 255262346 .