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esaxerenone
Sign in to saveEsaxerenone () (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. 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.
In the Vinony graph
Vinony's link graph records 102 inbound references to esaxerenone, and connects out to mometasone furoate, fludrocortisone and deoxycorticosterone.
It is catalogued under topics including Antimineralocorticoids, Carboxamides and Chemical pages without DrugBank identifier.
Vinony links it to 5 Wikipedia language editions.
Chemical data
- Formula
- C22H21F3N2O4S
- Molecular weight
- 466.5 g/mol
- IUPAC name
- 1-(2-hydroxyethyl)-4-methyl-N-(4-methylsulfonylphenyl)-5-[2-(trifluoromethyl)phenyl]pyrrole-3-carboxamide
- SMILES
- CC1=C(N(C=C1C(=O)NC2=CC=C(C=C2)S(=O)(=O)C)CCO)C3=CC=CC=C3C(F)(F)F
- InChIKey
- NOSNHVJANRODGR-UHFFFAOYSA-N
- XLogP
- 2.9
- Polar surface area
- 96.8 Ų
- H-bond donors
- 2
- H-bond acceptors
- 7
- Formal charge
- 0
via PubChem
Drug data · ChEMBL
- Molecule type
- Small molecule
via ChEMBL · EBI
Wikidata facts
- Subclass of
- chemical compound
- Mass
- 466.117
Show 2 more facts
- canonical SMILES
- CC1=C(N(C=C1C(=O)NC2=CC=C(C=C2)S(=O)(=O)C)CCO)C3=CC=CC=C3C(F)(F)F
- chemical formula
- C₂₂H₂₁F₃N₂O₄S
Sources (1)
via Wikidata · CC0
~1 min read
Encyclopedic overview
3 sectionsContents
- See also
- References
- External links
Esaxerenone () (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. 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.
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.
Excerpted from Wikipedia’s “esaxerenone” article, available under the CC BY-SA 4.0 licence.