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Balcinrenone

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Pharmaceutical
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Pharmaceutical compound
Balcinrenone
Clinical data
Other namesAZD9977; AZD-9977
Legal status
Legal status
  • Investigational
Identifiers
IUPAC name
  • 2--N-methylacetamide
CAS Number
PubChem CID
UNII
Chemical and physical data
FormulaC20H18FN3O5
Molar mass399.378 g·mol

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.

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 (23 February 2018). "Preclinical pharmacology of AZD9977: A novel mineralocorticoid receptor modulator separating organ protection from effects on electrolyte excretion". PLOS ONE. 13 (2): e0193380. Bibcode:2018PLoSO..1393380B. doi:10.1371/journal.pone.0193380. PMC 5825103. PMID 29474466.
  2. Bamberg, Krister; William-Olsson, Lena; Johansson, Ulrika; Jansson-Löfmark, Rasmus; Hartleib-Geschwindner, Judith (January 2019). "The selective mineralocorticoid receptor modulator AZD9977 reveals differences in mineralocorticoid effects of aldosterone and fludrocortisone". Journal of the Renin-Angiotensin-Aldosterone System. 20 (1): 147032031982744. doi:10.1177/1470320319827449. PMC 6396052. PMID 30813831.
  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 (March 2020). "Safety, Tolerability, and Pharmacokinetics of the Mineralocorticoid Receptor Modulator AZD9977 in Healthy Men: A Phase I Multiple Ascending Dose Study". Clinical and Translational Science. 13 (2): 275–283. doi:10.1111/cts.12705. PMC 7070793. PMID 31584739.
  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 (October 2022). "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. 15 (10): 2493–2504. doi:10.1111/cts.13377. PMC 9579384. PMID 35971596.
  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. (20 January 2023). "Control of Hydrogen Fluoride Formation and Release during a Large-Scale Nitroarene Reduction in the Manufacture of AZD9977". Organic Process Research & Development. 27 (1): 167–178. doi:10.1021/acs.oprd.2c00323. S2CID 255262346.
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