Azilsartan medoxomil (BioDeep_00000662155)
代谢物信息卡片
化学式: C30H24N4O8 (568.1594)
中文名称: 阿齐沙坦奥美沙坦酯
谱图信息:
最多检出来源 () %
分子结构信息
SMILES: CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NOC(=O)N5)C(=O)OCC6=C(OC(=O)O6)C
InChI: InChI=1S/C30H24N4O8/c1-3-38-28-31-23-10-6-9-22(27(35)39-16-24-17(2)40-30(37)41-24)25(23)34(28)15-18-11-13-19(14-12-18)20-7-4-5-8-21(20)26-32-29(36)42-33-26/h4-14H,3,15-16H2,1-2H3,(H,32,33,36)
描述信息
C - Cardiovascular system > C09 - Agents acting on the renin-angiotensin system > C09C - Angiotensin ii receptor blockers (arbs), plain > C09CA - Angiotensin ii receptor blockers (arbs), plain
C78274 - Agent Affecting Cardiovascular System > C270 - Antihypertensive Agent > C66930 - Angiotensin II Receptor Antagonist
D057911 - Angiotensin Receptor Antagonists > D047228 - Angiotensin II Type 1 Receptor Blockers
Azilsartan medoxomil (TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension[1][2][3][4].
同义名列表
2 个代谢物同义名
数据库引用编号
7 个数据库交叉引用编号
- ChEBI: CHEBI:68845
- KEGGdrug: D08067
- PubChem: 135409642
- DrugBank: DB08822
- ChEMBL: CHEMBL2028661
- CAS: 863031-21-4
- medchemexpress: HY-14736
分类词条
相关代谢途径
Reactome()
BioCyc()
PlantCyc()
代谢反应
个相关的代谢反应过程信息。
Reactome()
BioCyc()
WikiPathways()
Plant Reactome()
INOH()
PlantCyc()
COVID-19 Disease Map()
PathBank()
PharmGKB()
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。
| 亚细胞结构定位 | 关联基因列表 |
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文献列表
- Ami Kwon, Gee-Hee Kim. Single-pill Combination Therapy of Azilsartan Medoxomil/Chlorthalidone for Treatment of Hypertension: A Systematic Review.
Clinical therapeutics.
2020 07; 42(7):1390-1403. doi:
10.1016/j.clinthera.2020.05.015. [PMID: 32595000] - Kazuaki Enya, Ben T Saji, Takuya Kato, Hiroyuki Okamoto, Emiko Koumura. Pharmacokinetics of a Single Dose of Azilsartan in Pediatric Patients: A Phase 3, Open-Label, Multicenter Study.
Advances in therapy.
2018 Aug; 35(8):1181-1190. doi:
10.1007/s12325-018-0754-5. [PMID: 30027478] - Michael A Weber, Peter Sever, Attila Juhasz, Andrew Roberts, Charlie Cao. A randomized trial of the efficacy and safety of azilsartan medoxomil combined with chlorthalidone.
Journal of the renin-angiotensin-aldosterone system : JRAAS.
2018 Jul; 19(3):1470320318795000. doi:
10.1177/1470320318795000. [PMID: 30175930] - George L Bakris, Lin Zhao, Stuart Kupfer, Attila Juhasz, Michie Hisada, Eric Lloyd, Suzanne Oparil. Long-term efficacy and tolerability of azilsartan medoxomil/chlorthalidone vs olmesartan medoxomil/hydrochlorothiazide in chronic kidney disease.
Journal of clinical hypertension (Greenwich, Conn.).
2018 04; 20(4):694-702. doi:
10.1111/jch.13230. [PMID: 29504252] - William C Cushman, George L Bakris, William B White, Michael A Weber, Domenic Sica, Andrew Roberts, Eric Lloyd, Stuart Kupfer. A randomized titrate-to-target study comparing fixed-dose combinations of azilsartan medoxomil and chlorthalidone with olmesartan and hydrochlorothiazide in stage-2 systolic hypertension.
Journal of hypertension.
2018 04; 36(4):947-956. doi:
10.1097/hjh.0000000000001647. [PMID: 29334491] - Caroline Dudkowski, Aziz Karim, Zhen Zhao, Alberto B Alonso, Dyal Garg, Richard A Preston. Single-Center Evaluation of the Pharmacokinetics and Safety of the Angiotensin II Receptor Antagonist Azilsartan Medoxomil in Mild to Moderate Hepatic Impairment.
Journal of clinical pharmacology.
2018 Jan; 58(1):48-56. doi:
10.1002/jcph.970. [PMID: 28750149] - Manami Kaneko, Tomoko Satomi, Shuji Fujiwara, Hidefumi Uchiyama, Keiji Kusumoto, Tomoyuki Nishimoto. AT1 receptor blocker azilsartan medoxomil normalizes plasma miR-146a and miR-342-3p in a murine heart failure model.
Biomarkers : biochemical indicators of exposure, response, and susceptibility to chemicals.
2017 May; 22(3-4):253-260. doi:
10.1080/1354750x.2016.1204001. [PMID: 27321284] - Santosh Kumar Puttrevu, Rachumallu Ramakrishna, Manisha Bhateria, Moon Jain, Kashif Hanif, Rabi Sankar Bhatta. Pharmacokinetic-pharmacodynamic modeling of the antihypertensive interaction between azilsartan medoxomil and chlorthalidone in spontaneously hypertensive rats.
Naunyn-Schmiedeberg's archives of pharmacology.
2017 May; 390(5):457-470. doi:
10.1007/s00210-017-1339-6. [PMID: 28190245] - Luke J Laffin, Colleen Majewski, Chuanhong Liao, George L Bakris. Relationship Between Obesity, Hypertension, and Aldosterone Production in Postmenopausal African American Women: A Pilot Study.
Journal of clinical hypertension (Greenwich, Conn.).
2016 12; 18(12):1216-1221. doi:
10.1111/jch.12857. [PMID: 27259699] - Caroline Dudkowski, Aziz Karim, Melvin Munsaka. Effects of Food Intake on the Pharmacokinetics of Azilsartan Medoxomil and Chlorthalidone Alone and in Fixed-Dose Combination in Healthy Adults.
Clinical pharmacology in drug development.
2016 Sep; 5(5):393-8. doi:
10.1002/cpdd.249. [PMID: 27514506] - Keizo Matsushita, Hai-Chun Yang, Manu M Mysore, Jianyong Zhong, Yu Shyr, Li-Jun Ma, Agnes B Fogo. Effects of combination PPARγ agonist and angiotensin receptor blocker on glomerulosclerosis.
Laboratory investigation; a journal of technical methods and pathology.
2016 06; 96(6):602-9. doi:
10.1038/labinvest.2016.42. [PMID: 26999660] - Alison Handley, Eric Lloyd, Andrew Roberts, Bruce Barger. Safety and tolerability of azilsartan medoxomil in subjects with essential hypertension: a one-year, phase 3, open-label study.
Clinical and experimental hypertension (New York, N.Y. : 1993).
2016; 38(2):180-8. doi:
10.3109/10641963.2015.1081213. [PMID: 26817604] - Yoji Kuze, Akifumi Kogame, Fumihiro Jinno, Takahiro Kondo, Satoru Asahi. Development, validation and application of the liquid chromatography tandem mass spectrometry method for simultaneous quantification of azilsartan medoxomil (TAK-491), azilsartan (TAK-536), and its 2 metabolites in human plasma.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2015 Sep; 1001(?):174-81. doi:
10.1016/j.jchromb.2015.07.047. [PMID: 26279009] - Mark S Kipnes, Alison Handley, Eric Lloyd, Bruce Barger, Andrew Roberts. Safety, tolerability, and efficacy of azilsartan medoxomil with or without chlorthalidone during and after 8 months of treatment for hypertension.
Journal of clinical hypertension (Greenwich, Conn.).
2015 Mar; 17(3):183-92. doi:
10.1111/jch.12474. [PMID: 25619410] - Md Abdul Hye Khan, Jan Neckář, Breana Cummens, Geneva M Wahl, John D Imig. Azilsartan decreases renal and cardiovascular injury in the spontaneously hypertensive obese rat.
Cardiovascular drugs and therapy.
2014 Aug; 28(4):313-22. doi:
10.1007/s10557-014-6530-0. [PMID: 24842561] - Tomoko Ishizuka, Yasushi Yoshigae, Nobuyuki Murayama, Takashi Izumi. Different hydrolases involved in bioactivation of prodrug-type angiotensin receptor blockers: carboxymethylenebutenolidase and carboxylesterase 1.
Drug metabolism and disposition: the biological fate of chemicals.
2013 Nov; 41(11):1888-95. doi:
10.1124/dmd.113.053595. [PMID: 23946449] - Richard A Preston, Aziz Karim, Caroline Dudkowski, Zhen Zhao, Dyal Garg, Oliver Lenz, Domenic A Sica. Single-center evaluation of the single-dose pharmacokinetics of the angiotensin II receptor antagonist azilsartan medoxomil in renal impairment.
Clinical pharmacokinetics.
2013 May; 52(5):347-58. doi:
10.1007/s40262-013-0044-y. [PMID: 23575872] - Naohiro Kawaguchi, Takuya Ebihara, Toshiyuki Takeuchi, Akio Morohashi, Hitomi Yamasaki, Yoshihiko Tagawa, Junzo Takahashi, Takahiro Kondo, Satoru Asahi. Absorption of TAK-491, a new angiotensin II receptor antagonist, in animals.
Xenobiotica; the fate of foreign compounds in biological systems.
2013 Feb; 43(2):182-92. doi:
10.3109/00498254.2012.708797. [PMID: 22867273] - George L Bakris, Domenic Sica, William B White, William C Cushman, Michael A Weber, Alison Handley, Eric Song, Stuart Kupfer. Antihypertensive efficacy of hydrochlorothiazide vs chlorthalidone combined with azilsartan medoxomil.
The American journal of medicine.
2012 Dec; 125(12):1229.e1-1229.e10. doi:
10.1016/j.amjmed.2012.05.023. [PMID: 22939358] - Keiji Kusumoto. [In vitro and in vivo pharmacological profiles of a novel angiotensin type 1-receptor blocker, azilsartan].
Nihon yakurigaku zasshi. Folia pharmacologica Japonica.
2012 Jun; 139(6):236-40. doi:
10.1254/fpj.139.236. [PMID: 22728984] - R Weltman, C M J Brands, E Corral, M J E Desmares-Koopmans, M H J Migchielsen, K A Oudhoff, D F de Roode. Assessment of the environmental fate and effects of azilsartan, a selective antagonist of angiotensin II type 1.
Chemosphere.
2012 Jun; 87(11):1323-9. doi:
10.1016/j.chemosphere.2012.01.053. [PMID: 22365278] - Massimo Volpe, Carmine Savoia. New treatment options in the management of hypertension: appraising the potential role of azilsartan medoxomil.
Integrated blood pressure control.
2012; 5(?):19-25. doi:
10.2147/ibpc.s13784. [PMID: 22457601] - M Zhao, Y Li, J Wang, K Ebihara, X Rong, K Hosoda, T Tomita, K Nakao. Azilsartan treatment improves insulin sensitivity in obese spontaneously hypertensive Koletsky rats.
Diabetes, obesity & metabolism.
2011 Dec; 13(12):1123-9. doi:
10.1111/j.1463-1326.2011.01471.x. [PMID: 21749604] - Sum Lam. Azilsartan: a newly approved angiotensin II receptor blocker.
Cardiology in review.
2011 Nov; 19(6):300-4. doi:
10.1097/crd.0b013e31822e9ba3. [PMID: 21983318] - Keiji Kusumoto, Hideki Igata, Mami Ojima, Ayako Tsuboi, Mitsuaki Imanishi, Fuminari Yamaguchi, Hiroki Sakamoto, Takanobu Kuroita, Naohiro Kawaguchi, Nobuhiro Nishigaki, Hideaki Nagaya. Antihypertensive, insulin-sensitising and renoprotective effects of a novel, potent and long-acting angiotensin II type 1 receptor blocker, azilsartan medoxomil, in rat and dog models.
European journal of pharmacology.
2011 Nov; 669(1-3):84-93. doi:
10.1016/j.ejphar.2011.07.014. [PMID: 21816148]
