Osilodrostat (BioDeep_00000837622)
代谢物信息卡片
化学式: C13H10FN3 (227.0859)
中文名称:
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: C1CC2=CN=CN2C1C3=C(C=C(C=C3)C#N)F
InChI: InChI=1S/C13H10FN3/c14-12-5-9(6-15)1-3-11(12)13-4-2-10-7-16-8-17(10)13/h1,3,5,7-8,13H,2,4H2/t13-/m1/s1
描述信息
H - Systemic hormonal preparations, excl. sex hormones and insulins > H02 - Corticosteroids for systemic use > H02C - Antiadrenal preparations > H02CA - Anticorticosteroids
C471 - Enzyme Inhibitor
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: D11061
- PubChem: 44139752
- DrugBank: DB11837
- ChEMBL: CHEMBL3099695
- CAS: 1304733-26-3
- CAS: 928134-65-0
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。
亚细胞结构定位 | 关联基因列表 |
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文献列表
- Juan Valentín-Goyco, Jiayan Liu, Hwei-Ming Peng, Jerry Oommen, Richard J Auchus. Selectivity of osilodrostat as an inhibitor of human steroidogenic cytochromes P450.
The Journal of steroid biochemistry and molecular biology.
2023 07; 231(?):106316. doi:
10.1016/j.jsbmb.2023.106316
. [PMID: 37098354] - Frederic Castinetti, Lynnette K Nieman, Martin Reincke, John Newell-Price. Approach to the Patient Treated with Steroidogenesis Inhibitors.
The Journal of clinical endocrinology and metabolism.
2021 06; 106(7):2114-2123. doi:
10.1210/clinem/dgab122
. [PMID: 33675650] - Cédric Fontaine-Sylvestre, Laurent Létourneau-Guillon, Robert A Moumdjian, France Berthelet, André Lacroix. Corticotroph tumor progression during long-term therapy with osilodrostat in a patient with persistent Cushing's disease.
Pituitary.
2021 Apr; 24(2):207-215. doi:
10.1007/s11102-020-01097-1
. [PMID: 33074401] - Rosario Pivonello, Maria Fleseriu, John Newell-Price, Xavier Bertagna, James Findling, Akira Shimatsu, Feng Gu, Richard Auchus, Rattana Leelawattana, Eun Jig Lee, Jung Hee Kim, André Lacroix, Audrey Laplanche, Paul O'Connell, Libuse Tauchmanova, Alberto M Pedroncelli, Beverly M K Biller. Efficacy and safety of osilodrostat in patients with Cushing's disease (LINC 3): a multicentre phase III study with a double-blind, randomised withdrawal phase.
The lancet. Diabetes & endocrinology.
2020 09; 8(9):748-761. doi:
10.1016/s2213-8587(20)30240-0
. [PMID: 32730798] - Yongfu Liu, Jun Wu, Mingwei Zhou, Wenming Chen, Dongbo Li, Zhanguo Wang, Benoit Hornsperger, Johannes D Aebi, Hans-Peter Märki, Bernd Kuhn, Lisha Wang, Andreas Kuglstatter, Jörg Benz, Stephan Müller, Remo Hochstrasser, Giorgio Ottaviani, Jian Xin, Stephan Kirchner, Susanne Mohr, Philippe Verry, William Riboulet, Hong C Shen, Alexander V Mayweg, Kurt Amrein, Xuefei Tan. Discovery of 3-Pyridyl Isoindolin-1-one Derivatives as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors.
Journal of medicinal chemistry.
2020 07; 63(13):6876-6897. doi:
10.1021/acs.jmedchem.0c00233
. [PMID: 32530624] - Richard A Feelders, John Newell-Price, Rosario Pivonello, Lynnette K Nieman, Leo J Hofland, Andre Lacroix. Advances in the medical treatment of Cushing's syndrome.
The lancet. Diabetes & endocrinology.
2019 04; 7(4):300-312. doi:
10.1016/s2213-8587(18)30155-4
. [PMID: 30033041] - Kenneth Meyers, Derek A Cogan, Jennifer Burke, Raquel Arenas, Michael Balestra, Nicholas F Brown, Zhidong Chen, Matthew A Cerny, Holly E Clifford, Federico Colombo, Lee Fader, Kosea S Frederick, Xin Guo, Daniel Goldberg, Keith R Hornberger, Stanley Kugler, John Lord, Daniel R Marshall, Neil Moss, Jean-Huges Parmentier, Jeremy R Richman, Jennifer Schmenk, Steven M Weldon, Maolin Yu, Michael Zhang. Dihydrobenzisoxazole-4-one compounds are novel selective inhibitors of aldosterone synthase (CYP11B2) with in vivo activity.
Bioorganic & medicinal chemistry letters.
2018 03; 28(5):979-984. doi:
10.1016/j.bmcl.2017.12.015
. [PMID: 29254646] - Juliette Emmerich, Chris J van Koppen, Jens L Burkhart, Qingzhong Hu, Lorenz Siebenbürger, Carsten Boerger, Claudia Scheuer, Matthias W Laschke, Michael D Menger, Rolf W Hartmann. Lead Optimization Generates CYP11B1 Inhibitors of Pyridylmethyl Isoxazole Type with Improved Pharmacological Profile for the Treatment of Cushing's Disease.
Journal of medicinal chemistry.
2017 06; 60(12):5086-5098. doi:
10.1021/acs.jmedchem.7b00437
. [PMID: 28570067] - Sara Armani, Lillian Ting, Nicholas Sauter, Christelle Darstein, Anadya Prakash Tripathi, Lai Wang, Bing Zhu, Helen Gu, Dung Yu Chun, Heidi J Einolf, Swarupa Kulkarni. Drug Interaction Potential of Osilodrostat (LCI699) Based on Its Effect on the Pharmacokinetics of Probe Drugs of Cytochrome P450 Enzymes in Healthy Adults.
Clinical drug investigation.
2017 May; 37(5):465-472. doi:
10.1007/s40261-017-0497-0
. [PMID: 28155129] - Steven M Weldon, Matthew A Cerny, Kristina Gueneva-Boucheva, Derek Cogan, Xin Guo, Neil Moss, Jean-Hugues Parmentier, Jeremy R Richman, Glenn A Reinhart, Nicholas F Brown. Selectivity of BI 689648, a Novel, Highly Selective Aldosterone Synthase Inhibitor: Comparison with FAD286 and LCI699 in Nonhuman Primates.
The Journal of pharmacology and experimental therapeutics.
2016 10; 359(1):142-50. doi:
10.1124/jpet.116.236463
. [PMID: 27481775] - Rita Bernhardt. The potential of targeting CYP11B.
Expert opinion on therapeutic targets.
2016 Aug; 20(8):923-34. doi:
10.1517/14728222.2016.1151873
. [PMID: 26854589] - Maria Fleseriu, Rosario Pivonello, Jacques Young, Amir H Hamrahian, Mark E Molitch, Chikara Shimizu, Tomoaki Tanaka, Akira Shimatsu, Tracy White, Annie Hilliard, Chuan Tian, Nicholas Sauter, Beverly M K Biller, Xavier Bertagna. Osilodrostat, a potent oral 11β-hydroxylase inhibitor: 22-week, prospective, Phase II study in Cushing's disease.
Pituitary.
2016 Apr; 19(2):138-48. doi:
10.1007/s11102-015-0692-z
. [PMID: 26542280] - Rainer E Martin, Johannes D Aebi, Benoit Hornsperger, Hans-Jakob Krebs, Bernd Kuhn, Andreas Kuglstatter, André M Alker, Hans Peter Märki, Stephan Müller, Dominique Burger, Giorgio Ottaviani, William Riboulet, Philippe Verry, Xuefei Tan, Kurt Amrein, Alexander V Mayweg. Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.
Journal of medicinal chemistry.
2015 Oct; 58(20):8054-65. doi:
10.1021/acs.jmedchem.5b00851
. [PMID: 26403853] - Julien P N Papillon, Christopher M Adams, Qi-Ying Hu, Changgang Lou, Alok K Singh, Chun Zhang, Jose Carvalho, Srinivan Rajan, Adam Amaral, Michael E Beil, Fumin Fu, Eric Gangl, Chii-Whei Hu, Arco Y Jeng, Daniel LaSala, Guiqing Liang, Michael Logman, Wieslawa M Maniara, Dean F Rigel, Sherri A Smith, Gary M Ksander. Structure-Activity Relationships, Pharmacokinetics, and in Vivo Activity of CYP11B2 and CYP11B1 Inhibitors.
Journal of medicinal chemistry.
2015 Jun; 58(11):4749-70. doi:
10.1021/acs.jmedchem.5b00407
. [PMID: 25953419] - H-Z Wang, J-B Tian, K H Yang. Efficacy and safety of LCI699 for hypertension: a meta-analysis of randomized controlled trials and systematic review.
European review for medical and pharmacological sciences.
2015; 19(2):296-304. doi:
NULL
. [PMID: 25683946] - Joël Ménard, Dean F Rigel, Catherine Watson, Arco Y Jeng, Fumin Fu, Michael Beil, Jing Liu, Wei Chen, Chii-Whei Hu, Jennifer Leung-Chu, Daniel LaSala, Guiqing Liang, Sam Rebello, Yiming Zhang, William P Dole. Aldosterone synthase inhibition: cardiorenal protection in animal disease models and translation of hormonal effects to human subjects.
Journal of translational medicine.
2014 Dec; 12(?):340. doi:
10.1186/s12967-014-0340-9
. [PMID: 25491597] - Qingzhong Hu, Lina Yin, Rolf W Hartmann. Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.
Journal of medicinal chemistry.
2014 Jun; 57(12):5011-22. doi:
10.1021/jm401430e
. [PMID: 24422519] - Wenkui Li, Suyi Luo, Sam Rebello, Jimmy Flarakos, Francis L S Tse. A semi-automated LC-MS/MS method for the determination of LCI699, a steroid 11β-hydroxylase inhibitor, in human plasma.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2014 Jun; 960(?):182-93. doi:
10.1016/j.jchromb.2014.04.012
. [PMID: 24814004] - Xavier Bertagna, Rosario Pivonello, Maria Fleseriu, Yiming Zhang, Paul Robinson, Ann Taylor, Catherine E Watson, Mario Maldonado, Amir H Hamrahian, Marco Boscaro, Beverly M K Biller. LCI699, a potent 11β-hydroxylase inhibitor, normalizes urinary cortisol in patients with Cushing's disease: results from a multicenter, proof-of-concept study.
The Journal of clinical endocrinology and metabolism.
2014 Apr; 99(4):1375-83. doi:
10.1210/jc.2013-2117
. [PMID: 24423285] - Peter J Trainer. Next generation medical therapy for Cushing's syndrome--can we measure a benefit?.
The Journal of clinical endocrinology and metabolism.
2014 Apr; 99(4):1157-60. doi:
10.1210/jc.2014-1054
. [PMID: 24702012] - Nancy J Brown. Contribution of aldosterone to cardiovascular and renal inflammation and fibrosis.
Nature reviews. Nephrology.
2013 Aug; 9(8):459-69. doi:
10.1038/nrneph.2013.110
. [PMID: 23774812] - Adam D Karns, Jacqueline M Bral, Daniel Hartman, Thomas Peppard, Christoph Schumacher. Study of aldosterone synthase inhibition as an add-on therapy in resistant hypertension.
Journal of clinical hypertension (Greenwich, Conn.).
2013 Mar; 15(3):186-92. doi:
10.1111/jch.12051
. [PMID: 23458591] - Michel Azizi, Laurence Amar, Joël Menard. Aldosterone synthase inhibition in humans.
Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association.
2013 Jan; 28(1):36-43. doi:
10.1093/ndt/gfs388
. [PMID: 23045428] - Karl Andersen, Daniel Hartman, Thomas Peppard, David Hermann, Peter Van Ess, Martin Lefkowitz, Angelo Trapani. The effects of aldosterone synthase inhibition on aldosterone and cortisol in patients with hypertension: a phase II, randomized, double-blind, placebo-controlled, multicenter study.
Journal of clinical hypertension (Greenwich, Conn.).
2012 Sep; 14(9):580-7. doi:
10.1111/j.1751-7176.2012.00667.x
. [PMID: 22947355] - Laurence Amar, Michel Azizi, Joël Menard, Séverine Peyrard, Catherine Watson, Pierre-François Plouin. Aldosterone synthase inhibition with LCI699: a proof-of-concept study in patients with primary aldosteronism.
Hypertension (Dallas, Tex. : 1979).
2010 Nov; 56(5):831-8. doi:
10.1161/hypertensionaha.110.157271
. [PMID: 20837883]