Esaxerenone
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| Trade names | Minnebro |
| Other names | CS-3150; XL-550 |
| Routes of administration | By mouth |
| Drug class | Antimineralocorticoid |
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| Formula | C22H21F3N2O4S |
| Molar mass | 466.48 g·mol−1 |
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Esaxerenone (INN) (brand name Minnebro; developmental code names CS-3150, XL-550) is a nonsteroidal antimineralocorticoid which was discovered by Exelixis and developed by Daiichi Sankyo Company and is approved in Japan for the treatment of hypertension.[1][2][3] It acts as a highly selective silent antagonist of the mineralocorticoid receptor (MR), the receptor for aldosterone, with greater than 1,000-fold selectivity for this receptor over other steroid hormone receptors, and 4-fold and 76-fold higher affinity for the MR relative to the existing antimineralocorticoids spironolactone and eplerenone.[1][2][3]
Daiichi Sankyo Company, Limited on January 8, 2019 announced the receipt of marketing approval in Japan for MINNEBROTM Tablets 1.25 mg, 2.5 mg and 5 mg (generic name: esaxerenone) for the treatment of hypertension. As of January 2019, esaxerenone is in phase III clinical trials for diabetic nephropathies.[1][4]
See also
[edit]References
[edit]- ^ a b c "Esaxerenone - Daiichi Sankyo - AdisInsight".
- ^ a b Yang J, Young MJ (2016). "Mineralocorticoid receptor antagonists-pharmacodynamics and pharmacokinetic differences". Curr Opin Pharmacol. 27: 78–85. doi:10.1016/j.coph.2016.02.005. PMID 26939027.
- ^ a b Kolkhof P, Nowack C, Eitner F (2015). "Nonsteroidal antagonists of the mineralocorticoid receptor". Curr. Opin. Nephrol. Hypertens. 24 (5): 417–24. doi:10.1097/MNH.0000000000000147. PMID 26083526. S2CID 22113501.
- ^ https://www.daiichisankyo.com/media/press_release/detail/index_3212.html#:~:text=Tokyo%2C%20Japan%20(January%208%2C,for%20the%20treatment%20of%20hypertension
External links
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