Chemistry:Esaxerenone
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
References
- ↑ 1.0 1.1 1.2 "Esaxerenone - Daiichi Sankyo - AdisInsight". https://adisinsight.springer.com/drugs/800021527.
- ↑ 2.0 2.1 "Mineralocorticoid receptor antagonists-pharmacodynamics and pharmacokinetic differences". Curr Opin Pharmacol 27: 78–85. 2016. doi:10.1016/j.coph.2016.02.005. PMID 26939027.
- ↑ 3.0 3.1 "Nonsteroidal antagonists of the mineralocorticoid receptor". Curr. Opin. Nephrol. Hypertens. 24 (5): 417–24. 2015. doi:10.1097/MNH.0000000000000147. PMID 26083526.
- ↑ "Daiichi Sankyo Announces Approval of MINNEBRO(TM) Tablets for the Treatment of Hypertension in Japan". January 8, 2019. https://www.daiichisankyo.com/media/press_release/detail/index_3212.html.
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