Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

Esaxerenone

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Esaxerenone
Clinical data
Trade namesMinnebro
Other namesCS-3150; XL-550
Routes of
administration
By mouth
Drug classAntimineralocorticoid
Identifiers
  • 1-(2-hydroxyethyl)-4-methyl-N-(4-methylsulfonylphenyl)-5-[2-(trifluoromethyl)phenyl]pyrrole-3-carboxamide
CAS Number
PubChemCID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC22H21F3N2O4S
Molar mass466.48 g·mol−1
3D model (JSmol)
  • CC1=C(N(C=C1C(=O)NC2=CC=C(C=C2)S(=O)(=O)C)CCO)C3=CC=CC=C3C(F)(F)F
  • InChI=1S/C22H21F3N2O4S/c1-14-18(21(29)26-15-7-9-16(10-8-15)32(2,30)31)13-27(11-12-28)20(14)17-5-3-4-6-19(17)22(23,24)25/h3-10,13,28H,11-12H2,1-2H3,(H,26,29)
  • Key:NOSNHVJANRODGR-UHFFFAOYSA-N

Esaxerenone (INNTooltip International Nonproprietary Name) (brand nameMinnebro; developmental code namesCS-3150,XL-550) is anonsteroidalantimineralocorticoid which was discovered byExelixis and developed byDaiichi Sankyo Company and is approved inJapan for the treatment ofhypertension.[1][2][3] It acts as a highlyselectivesilent antagonist of themineralocorticoid receptor (MR), thereceptor foraldosterone, with greater than 1,000-fold selectivity for this receptor over othersteroid hormone receptors, and 4-fold and 76-fold higheraffinity for the MR relative to the existing antimineralocorticoidsspironolactone andeplerenone.[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 inphase IIIclinical trials fordiabetic nephropathies.[1][4]

See also

[edit]

References

[edit]
  1. ^abc"Esaxerenone - Daiichi Sankyo - AdisInsight".
  2. ^abYang 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.
  3. ^abKolkhof 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.
  4. ^"Daiichi Sankyo Announces Approval of MINNEBRO(TM) Tablets for the Treatment of Hypertension in Japan".Daiichi Sankyo. January 8, 2019.

External links

[edit]


Mineralocorticoids
Antimineralocorticoids
Synthesis modifiers
MRTooltip Mineralocorticoid receptor
Agonists
Antagonists
Stub icon

Thisdrug article relating to thecardiovascular system is astub. You can help Wikipedia byexpanding it.

Retrieved from "https://en.wikipedia.org/w/index.php?title=Esaxerenone&oldid=1311649262"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2025 Movatter.jp