Esaxerenone (BioDeep_00000859151)
代谢物信息卡片
Esaxerenone
化学式: C22H21F3N2O4S (466.11740620000006)
中文名称: 艾沙利酮
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CC1=C(N(C=C1C(=O)NC2=CC=C(C=C2)S(=O)(=O)C)CCO)C3=CC=CC=C3C(F)(F)F
InChI: 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)
描述信息
C78274 - Agent Affecting Cardiovascular System > C270 - Antihypertensive Agent
同义名列表
1 个代谢物同义名
数据库引用编号
6 个数据库交叉引用编号
- KEGGdrug: D10892
- PubChem: 25052023
- DrugBank: DB15207
- ChEMBL: CHEMBL2181932
- CAS: 1632006-28-0
- CAS: 880780-76-7
分类词条
相关代谢途径
Reactome(0)
BioCyc(0)
PlantCyc(0)
代谢反应
0 个相关的代谢反应过程信息。
Reactome(0)
BioCyc(0)
WikiPathways(0)
Plant Reactome(0)
INOH(0)
PlantCyc(0)
COVID-19 Disease Map(0)
PathBank(0)
PharmGKB(0)
0 个相关的物种来源信息
在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：
- PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。
文献列表
- Xiaoming Xu, Jing Feng, Yuying Cui, Pingjiang Li, Jianjun Dong, Lin Liao. Renal effects and safety between Asian and non-Asian chronic kidney disease and type 2 diabetes treated with nonsteroidal mineralocorticoid antagonists.
Journal of diabetes.
2024 Jun; 16(6):e13566. doi:
10.1111/1753-0407.13566. [PMID: 38753662] - Ran Sun, Yali Li, Lei Lv, Weiliang Zhang, Xiaoxia Guo. Efficacy and safety of esaxerenone (CS-3150) in primary hypertension: a meta-analysis.
Journal of human hypertension.
2024 Feb; 38(2):102-109. doi:
10.1038/s41371-023-00889-9. [PMID: 38177694] - Oyunbileg Bavuu, Daiju Fukuda, Byambasuren Ganbaatar, Tomomi Matsuura, Takayuki Ise, Kenya Kusunose, Koji Yamaguchi, Shusuke Yagi, Hirotsugu Yamada, Takeshi Soeki, Tetsuzo Wakatsuki, Masataka Sata. Esaxerenone, a selective mineralocorticoid receptor blocker, improves insulin sensitivity in mice consuming high-fat diet.
European journal of pharmacology.
2022 Sep; 931(?):175190. doi:
10.1016/j.ejphar.2022.175190. [PMID: 35961594] - Kenichi Shikata, Sadayoshi Ito, Naoki Kashihara, Masaomi Nangaku, Takashi Wada, Yasuyuki Okuda, Tomoko Sawanobori, Kotaro Sugimoto. Reduction in the magnitude of serum potassium elevation in combination therapy with esaxerenone (CS-3150) and sodium-glucose cotransporter 2 inhibitor in patients with diabetic kidney disease: Subanalysis of two phase III studies.
Journal of diabetes investigation.
2022 Jul; 13(7):1190-1202. doi:
10.1111/jdi.13778. [PMID: 35199478] - Slobodan M Janković, Snežana V Janković. Clinical Pharmacokinetics and Pharmacodynamics of Esaxerenone, a Novel Mineralocorticoid Receptor Antagonist: A Review.
European journal of drug metabolism and pharmacokinetics.
2022 May; 47(3):291-308. doi:
10.1007/s13318-022-00760-1. [PMID: 35190999] - Akiko Watanabe, Tomoko Ishizuka, Makiko Yamada, Yoshiyuki Igawa, Takako Shimizu, Hitoshi Ishizuka. Physiologically based pharmacokinetic modelling to predict the clinical effect of CYP3A inhibitors/inducers on esaxerenone pharmacokinetics in healthy subjects and subjects with hepatic impairment.
European journal of clinical pharmacology.
2022 Jan; 78(1):65-73. doi:
10.1007/s00228-021-03194-x. [PMID: 34415382] - Sadayoshi Ito, Naoki Kashihara, Kenichi Shikata, Masaomi Nangaku, Takashi Wada, Yasuyuki Okuda, Tomoko Sawanobori. Efficacy and safety of esaxerenone (CS-3150) in Japanese patients with type 2 diabetes and macroalbuminuria: a multicenter, single-arm, open-label phase III study.
Clinical and experimental nephrology.
2021 Oct; 25(10):1070-1078. doi:
10.1007/s10157-021-02075-y. [PMID: 34110524] - Kaoru Toyama, Hidetoshi Furuie, Kana Kuroda, Tomoko Ishizuka, Yasuyuki Okuda, Takako Shimizu, Manabu Kato, Yoshiyuki Igawa, Yasuhiro Nishikawa, Hitoshi Ishizuka. Effects of Repeated Oral Administration of Esaxerenone on the Pharmacokinetics of Midazolam in Healthy Japanese Males.
European journal of drug metabolism and pharmacokinetics.
2021 Sep; 46(5):685-694. doi:
10.1007/s13318-021-00701-4. [PMID: 34383278] - Sadayoshi Ito, Hiroshi Itoh, Hiromi Rakugi, Yasuyuki Okuda, Setsuko Iijima. Antihypertensive effects and safety of esaxerenone in patients with moderate kidney dysfunction.
Hypertension research : official journal of the Japanese Society of Hypertension.
2021 05; 44(5):489-497. doi:
10.1038/s41440-020-00585-y. [PMID: 33323991] - Hiromi Rakugi, Satoru Yamakawa, Kotaro Sugimoto. Management of hyperkalemia during treatment with mineralocorticoid receptor blockers: findings from esaxerenone.
Hypertension research : official journal of the Japanese Society of Hypertension.
2021 04; 44(4):371-385. doi:
10.1038/s41440-020-00569-y. [PMID: 33214722] - Ningning Wan, Asadur Rahman, Akira Nishiyama. Esaxerenone, a novel nonsteroidal mineralocorticoid receptor blocker (MRB) in hypertension and chronic kidney disease.
Journal of human hypertension.
2021 02; 35(2):148-156. doi:
10.1038/s41371-020-0377-6. [PMID: 32661269] - Sadayoshi Ito, Naoki Kashihara, Kenichi Shikata, Masaomi Nangaku, Takashi Wada, Yasuyuki Okuda, Tomoko Sawanobori. Esaxerenone (CS-3150) in Patients with Type 2 Diabetes and Microalbuminuria (ESAX-DN): Phase 3 Randomized Controlled Clinical Trial.
Clinical journal of the American Society of Nephrology : CJASN.
2020 12; 15(12):1715-1727. doi:
10.2215/cjn.06870520. [PMID: 33239409] - Peter Rossing. Mineralocorticoid Receptor Antagonists for Diabetic Kidney Disease.
Clinical journal of the American Society of Nephrology : CJASN.
2020 12; 15(12):1696-1698. doi:
10.2215/cjn.16201020. [PMID: 33239412] - Kiyoshi Arai, Yuka Morikawa, Naoko Ubukata, Kotaro Sugimoto. Synergistic reduction in albuminuria in type 2 diabetic mice by esaxerenone (CS-3150), a novel nonsteroidal selective mineralocorticoid receptor blocker, combined with an angiotensin II receptor blocker.
Hypertension research : official journal of the Japanese Society of Hypertension.
2020 11; 43(11):1204-1213. doi:
10.1038/s41440-020-0495-0. [PMID: 32616846] - Yoshiaki Kirigaya, Masanari Shiramoto, Tomoko Ishizuka, Hinako Uchimaru, Shin Irie, Manabu Kato, Takako Shimizu, Takafumi Nakatsu, Yasuhiro Nishikawa, Hitoshi Ishizuka. Effects of itraconazole and rifampicin on the single-dose pharmacokinetics of the nonsteroidal mineralocorticoid receptor blocker esaxerenone in healthy Japanese subjects.
British journal of clinical pharmacology.
2020 10; 86(10):2070-2079. doi:
10.1111/bcp.14302. [PMID: 32250463] - Yoshiaki Kirigaya, Masanari Shiramoto, Tomoko Ishizuka, Hinako Uchimaru, Shin Irie, Manabu Kato, Takako Shimizu, Takafumi Nakatsu, Yasuhiro Nishikawa, Hitoshi Ishizuka. Pharmacokinetic interactions of esaxerenone with amlodipine and digoxin in healthy Japanese subjects.
BMC pharmacology & toxicology.
2020 07; 21(1):55. doi:
10.1186/s40360-020-00423-4. [PMID: 32727577] - Amanda E Garza, Elijah Trefts, Isis A Katayama Rangel, Danielle Brooks, Rene Baudrand, Burhanuddin Moize, Jose R Romero, Sanjay Ranjit, Thitinan Treesaranuwattana, Tham M Yao, Gail K Adler, Luminita H Pojoga, Gordon H Williams. Striatin heterozygous mice are more sensitive to aldosterone-induced injury.
The Journal of endocrinology.
2020 06; 245(3):439-450. doi:
10.1530/joe-19-0562. [PMID: 32229698] - Keisuke Okamura, Masatoshi Matsushima, Fumi Yamamoto, Yosuke Takamiya, Tetsu Okuda, Kazuyuki Shirai, Katsusuke Okamura, Hidenori Urata. A Patient with Bilateral Primary Aldosteronism Refractory to Oral Eplerenone Who Responded to Esaxerenone with Increased Renin Activity.
The American journal of case reports.
2020 Jan; 21(?):e920615. doi:
10.12659/ajcr.920615. [PMID: 31907345] - Akifumi Kurata, Takafumi Yoshida, Megumi Inoue, Tomoko Ishizuka, Takafumi Nakatsu, Takako Shimizu, Manabu Kato, Yasuhiro Nishikawa, Hitoshi Ishizuka. Pharmacokinetics and Safety of Single-Dose Esaxerenone in Japanese Subjects with Mild to Moderate Hepatic Impairment.
Advances in therapy.
2020 01; 37(1):253-264. doi:
10.1007/s12325-019-01121-2. [PMID: 31705436] - Satoru Yamakawa, Tsuyoshi Homma, Makiko Yamada, Yoshiyuki Igawa, Motonobu Yoshimura. [Pharmacological profile, clinical efficacy, and safety of esaxerenone (Minnebro® tablets 1.25 mg, 2.5 mg, 5 mg)].
Nihon yakurigaku zasshi. Folia pharmacologica Japonica.
2020; 155(5):340-350. doi:
10.1254/fpj.20016. [PMID: 32879177] - Hiroshi Itoh, Sadayoshi Ito, Hiromi Rakugi, Yasuyuki Okuda, Satoshi Nishioka. Efficacy and safety of dosage-escalation of low-dosage esaxerenone added to a RAS inhibitor in hypertensive patients with type 2 diabetes and albuminuria: a single-arm, open-label study.
Hypertension research : official journal of the Japanese Society of Hypertension.
2019 10; 42(10):1572-1581. doi:
10.1038/s41440-019-0270-2. [PMID: 31239535] - Sadayoshi Ito, Kenichi Shikata, Masaomi Nangaku, Yasuyuki Okuda, Tomoko Sawanobori. Efficacy and Safety of Esaxerenone (CS-3150) for the Treatment of Type 2 Diabetes with Microalbuminuria: A Randomized, Double-Blind, Placebo-Controlled, Phase II Trial.
Clinical journal of the American Society of Nephrology : CJASN.
2019 08; 14(8):1161-1172. doi:
10.2215/cjn.14751218. [PMID: 31248950] - Akifumi Kurata, Hidetoshi Furuie, Tomoko Ishizuka, Takafumi Nakatsu, Takako Shimizu, Manabu Kato, Yasuhiro Nishikawa, Hitoshi Ishizuka. Absolute Bioavailability of Esaxerenone and Food Effects on its Pharmacokinetics After a Single Oral Dose in Healthy Japanese Subjects: An Open-Label Crossover Study.
Advances in therapy.
2019 07; 36(7):1618-1627. doi:
10.1007/s12325-019-00956-z. [PMID: 31119692] - Sadayoshi Ito, Hiroshi Itoh, Hiromi Rakugi, Yasuyuki Okuda, Satoru Yamakawa. Efficacy and safety of esaxerenone (CS-3150) for the treatment of essential hypertension: a phase 2 randomized, placebo-controlled, double-blind study.
Journal of human hypertension.
2019 07; 33(7):542-551. doi:
10.1038/s41371-019-0207-x. [PMID: 31113987] - Lei Li, Yu Guan, Hiroyuki Kobori, Asahiro Morishita, Hideki Kobara, Tsutomu Masaki, Daisuke Nakano, Akira Nishiyama. Effects of the novel nonsteroidal mineralocorticoid receptor blocker, esaxerenone (CS-3150), on blood pressure and urinary angiotensinogen in low-renin Dahl salt-sensitive hypertensive rats.
Hypertension research : official journal of the Japanese Society of Hypertension.
2019 06; 42(6):769-778. doi:
10.1038/s41440-018-0187-1. [PMID: 30587856] - Abdus Sattar Bhuiyan, Kazi Rafiq, Hideki Kobara, Tsutomu Masaki, Daisuke Nakano, Akira Nishiyama. Effect of a novel nonsteroidal selective mineralocorticoid receptor antagonist, esaxerenone (CS-3150), on blood pressure and renal injury in high salt-treated type 2 diabetic mice.
Hypertension research : official journal of the Japanese Society of Hypertension.
2019 06; 42(6):892-902. doi:
10.1038/s41440-019-0211-0. [PMID: 30664703] - Makiko Yamada, Jeanne Mendell, Hideo Takakusa, Takako Shimizu, Osamu Ando. Pharmacokinetics, Metabolism, and Excretion of [14C]Esaxerenone, a Novel Mineralocorticoid Receptor Blocker in Humans.
Drug metabolism and disposition: the biological fate of chemicals.
2019 03; 47(3):340-349. doi:
10.1124/dmd.118.084897. [PMID: 30541878] - Manabu Kato, Hidetoshi Furuie, Takako Shimizu, Atsuhiro Miyazaki, Fumiaki Kobayashi, Hitoshi Ishizuka. Single- and multiple-dose escalation study to assess pharmacokinetics, pharmacodynamics and safety of oral esaxerenone in healthy Japanese subjects.
British journal of clinical pharmacology.
2018 08; 84(8):1821-1829. doi:
10.1111/bcp.13616. [PMID: 29688582] - Makiko Yamada, Makoto Takei, Eiko Suzuki, Hideo Takakusa, Masakatsu Kotsuma, Takuo Washio, Nobuyuki Murayama, Shin-Ichi Inoue, Takashi Izumi. Pharmacokinetics, distribution, and disposition of esaxerenone, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist, in rats and monkeys.
Xenobiotica; the fate of foreign compounds in biological systems.
2017 Dec; 47(12):1090-1103. doi:
10.1080/00498254.2016.1263766. [PMID: 27866463] - Kiyoshi Arai, Yuka Morikawa, Naoko Ubukata, Hiroyuki Tsuruoka, Tsuyoshi Homma. CS-3150, a Novel Nonsteroidal Mineralocorticoid Receptor Antagonist, Shows Preventive and Therapeutic Effects On Renal Injury in Deoxycorticosterone Acetate/Salt-Induced Hypertensive Rats.
The Journal of pharmacology and experimental therapeutics.
2016 09; 358(3):548-57. doi:
10.1124/jpet.116.234765. [PMID: 27384074] - Kiyoshi Arai, Hiroyuki Tsuruoka, Tsuyoshi Homma. CS-3150, a novel non-steroidal mineralocorticoid receptor antagonist, prevents hypertension and cardiorenal injury in Dahl salt-sensitive hypertensive rats.
European journal of pharmacology.
2015 Dec; 769(?):266-73. doi:
10.1016/j.ejphar.2015.11.028. [PMID: 26607463] - Kiyoshi Arai, Tsuyoshi Homma, Yuka Morikawa, Naoko Ubukata, Hiyoyuki Tsuruoka, Kazumasa Aoki, Hirokazu Ishikawa, Makoto Mizuno, Toshio Sada. Pharmacological profile of CS-3150, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist.
European journal of pharmacology.
2015 Aug; 761(?):226-34. doi:
10.1016/j.ejphar.2015.06.015. [PMID: 26073023]