Molidustat (BioDeep_00000776203)
代谢物信息卡片
Molidustat
化学式: C13H14N8O2 (314.124)
中文名称: 莫立司他
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: C1COCCN1C2=NC=NC(=C2)N3C(=O)C(=CN3)N4C=CN=N4
InChI: InChI=1S/C13H14N8O2/c22-13-10(20-2-1-16-18-20)8-17-21(13)12-7-11(14-9-15-12)19-3-5-23-6-4-19/h1-2,7-9,17H,3-6H2
描述信息
C471 - Enzyme Inhibitor
Molidustat (BAY 85-3934) is a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with mean IC50 values of 480 nM for PHD1, 280 nM for PHD2, and 450 nM for PHD3.
同义名列表
2 个代谢物同义名
数据库引用编号
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相关代谢途径
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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)
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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
- Maria da Luz Sousa Fialho, Ujang Purnama, Kaitlyn M J H Dennis, Claudia N Montes Aparicio, Marcos Castro-Guarda, Emmanuelle Massourides, Damian J Tyler, Carolyn A Carr, Lisa C Heather. Activation of HIF1α Rescues the Hypoxic Response and Reverses Metabolic Dysfunction in the Diabetic Heart.
Diabetes.
2021 11; 70(11):2518-2531. doi:
10.2337/db21-0398. [PMID: 34526367] - Boye L Jensen. Get use to the -dustats: Roxadustat and molidustat, members of the hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor drug class promote kidney function, perfusion and oxygenation in rats through nitric oxide.
Acta physiologica (Oxford, England).
2021 09; 233(1):e13706. doi:
10.1111/apha.13706. [PMID: 34143560] - Anqi Zhang, Daisuke Nakano, Norihiko Morisawa, Kento Kitada, Wararat Kittikulsuth, Asadur Rahman, Takashi Morikawa, Yoshio Konishi, Akira Nishiyama. Effects of molidustat, a hypoxia-inducible factor prolyl hydroxylase inhibitor, on sodium dynamics in hypertensive subtotally nephrectomized rats.
Journal of pharmacological sciences.
2021 Jun; 146(2):98-104. doi:
10.1016/j.jphs.2021.03.007. [PMID: 33941326] - Megan L Noonan, Pu Ni, Rafiou Agoro, Spencer A Sacks, Elizabeth A Swallow, Jonathan A Wheeler, Erica L Clinkenbeard, Maegan L Capitano, Matthew Prideaux, Gerald J Atkins, William R Thompson, Matthew R Allen, Hal E Broxmeyer, Kenneth E White. The HIF-PHI BAY 85-3934 (Molidustat) Improves Anemia and Is Associated With Reduced Levels of Circulating FGF23 in a CKD Mouse Model.
Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research.
2021 06; 36(6):1117-1130. doi:
10.1002/jbmr.4272. [PMID: 33592127] - Dorina van der Mey, Michael Gerisch, Natalia A Jungmann, Andreas Kaiser, Kenichi Yoshikawa, Simone Schulz, Martin Radtke, Silvia Lentini. Drug-drug interaction of atazanavir on UGT1A1-mediated glucuronidation of molidustat in human.
Basic & clinical pharmacology & toxicology.
2021 Mar; 128(3):511-524. doi:
10.1111/bcpt.13538. [PMID: 33232579] - Laurie De Wilde, Kris Roels, Koen Deventer, Peter Van Eenoo. Automated sample preparation for the detection and confirmation of hypoxia-inducible factor stabilizers in urine.
Biomedical chromatography : BMC.
2021 Feb; 35(2):e4970. doi:
10.1002/bmc.4970. [PMID: 32840903] - Hiroyasu Yamamoto, Kiyoshi Nobori, Yoshimi Matsuda, Yasuhiro Hayashi, Takanori Hayasaki, Tadao Akizawa. Molidustat for Renal Anemia in Nondialysis Patients Previously Treated with Erythropoiesis-Stimulating Agents: A Randomized, Open-Label, Phase 3 Study.
American journal of nephrology.
2021; 52(10-11):884-893. doi:
10.1159/000518072. [PMID: 34569482] - Hiroyasu Yamamoto, Kiyoshi Nobori, Yoshimi Matsuda, Yasuhiro Hayashi, Takanori Hayasaki, Tadao Akizawa. Efficacy and Safety of Molidustat for Anemia in ESA-Naive Nondialysis Patients: A Randomized, Phase 3 Trial.
American journal of nephrology.
2021; 52(10-11):871-883. doi:
10.1159/000518071. [PMID: 34569489] - Lei Li, Daisuke Nakano, Anqi Zhang, Wararat Kittikulsuth, Norihiko Morisawa, Hiroyuki Ohsaki, Norio Suzuki, Masayuki Yamamoto, Akira Nishiyama. Effects of post-renal anemia treatment with the HIF-PHD inhibitor molidustat on adenine-induced renal anemia and kidney disease in mice.
Journal of pharmacological sciences.
2020 Dec; 144(4):229-236. doi:
10.1016/j.jphs.2020.09.004. [PMID: 33070842] - Silvia Lentini, Dorina van der Mey, Armin Kern, Uwe Thuss, Andreas Kaiser, Kumi Matsuno, Michael Gerisch. Absorption, distribution, metabolism and excretion of molidustat in healthy participants.
Basic & clinical pharmacology & toxicology.
2020 Sep; 127(3):221-233. doi:
10.1111/bcpt.13409. [PMID: 32248614] - Silvia Lentini, Andreas Kaiser, Stefanie Kapsa, Kumi Matsuno, Dorina van der Mey. Effects of oral iron and calcium supplement on the pharmacokinetics and pharmacodynamics of molidustat: an oral HIF-PH inhibitor for the treatment of renal anaemia.
European journal of clinical pharmacology.
2020 Feb; 76(2):185-197. doi:
10.1007/s00228-019-02813-y. [PMID: 31919558] - Tadao Akizawa, Megumi Taguchi, Yoshimi Matsuda, Kazuma Iekushi, Takashi Yamada, Hiroyasu Yamamoto. Molidustat for the treatment of renal anaemia in patients with dialysis-dependent chronic kidney disease: design and rationale of three phase III studies.
BMJ open.
2019 06; 9(6):e026602. doi:
10.1136/bmjopen-2018-026602. [PMID: 31203241] - Hiroyasu Yamamoto, Megumi Taguchi, Yoshimi Matsuda, Kazuma Iekushi, Takashi Yamada, Tadao Akizawa. Molidustat for the treatment of renal anaemia in patients with non-dialysis-dependent chronic kidney disease: design and rationale of two phase III studies.
BMJ open.
2019 06; 9(6):e026704. doi:
10.1136/bmjopen-2018-026704. [PMID: 31203242] - Alexandre Marchand, Ingrid Roulland, Florian Semence, Kaja Schröder, Valérie Domergue, Michel Audran. Detection of Hypoxia-Regulated MicroRNAs in Blood as Potential Biomarkers of HIF Stabilizer Molidustat.
MicroRNA (Shariqah, United Arab Emirates).
2019; 8(3):189-197. doi:
10.2174/2211536608666190117170317. [PMID: 30657053] - Tadao Akizawa, Iain C Macdougall, Jeffrey S Berns, Thomas Bernhardt, Gerald Staedtler, Megumi Taguchi, Kazuma Iekushi, Thilo Krueger. Long-Term Efficacy and Safety of Molidustat for Anemia in Chronic Kidney Disease: DIALOGUE Extension Studies.
American journal of nephrology.
2019; 49(4):271-280. doi:
10.1159/000499111. [PMID: 30852574] - Tadao Akizawa, Iain C Macdougall, Jeffrey S Berns, Hiroyasu Yamamoto, Megumi Taguchi, Kazuma Iekushi, Thomas Bernhardt. Iron Regulation by Molidustat, a Daily Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor, in Patients with Chronic Kidney Disease.
Nephron.
2019; 143(4):243-254. doi:
10.1159/000502012. [PMID: 31387097] - Amit A Joharapurkar, Vrajesh B Pandya, Vishal J Patel, Ranjit C Desai, Mukul R Jain. Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
Journal of medicinal chemistry.
2018 08; 61(16):6964-6982. doi:
10.1021/acs.jmedchem.7b01686. [PMID: 29712435] - M Böttcher, S Lentini, E R Arens, A Kaiser, D van der Mey, U Thuss, D Kubitza, G Wensing. First-in-man-proof of concept study with molidustat: a novel selective oral HIF-prolyl hydroxylase inhibitor for the treatment of renal anaemia.
British journal of clinical pharmacology.
2018 07; 84(7):1557-1565. doi:
10.1111/bcp.13584. [PMID: 29575006] - Hartmut Beck, Mario Jeske, Kai Thede, Friederike Stoll, Ingo Flamme, Metin Akbaba, Jens-Kerim Ergüden, Gunter Karig, Jörg Keldenich, Felix Oehme, Hans-Christian Militzer, Ingo V Hartung, Uwe Thuss. Discovery of Molidustat (BAY 85-3934): A Small-Molecule Oral HIF-Prolyl Hydroxylase (HIF-PH) Inhibitor for the Treatment of Renal Anemia.
ChemMedChem.
2018 05; 13(10):988-1003. doi:
10.1002/cmdc.201700783. [PMID: 29485740] - Wenpei Dong, Ping Yu, Tielong Zhang, Chenzhuang Zhu, Jun Qi, Junhao Liang. Adrenomedullin serves a role in the humoral pathway of delayed remote ischemic preconditioning via a hypoxia-inducible factor-1α-associated mechanism.
Molecular medicine reports.
2018 03; 17(3):4547-4553. doi:
10.3892/mmr.2018.8450. [PMID: 29344650] - Nupur Gupta, Jay B Wish. Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors: A Potential New Treatment for Anemia in Patients With CKD.
American journal of kidney diseases : the official journal of the National Kidney Foundation.
2017 Jun; 69(6):815-826. doi:
10.1053/j.ajkd.2016.12.011. [PMID: 28242135] - Francesco Locatelli, Steven Fishbane, Geoffrey A Block, Iain C Macdougall. Targeting Hypoxia-Inducible Factors for the Treatment of Anemia in Chronic Kidney Disease Patients.
American journal of nephrology.
2017; 45(3):187-199. doi:
10.1159/000455166. [PMID: 28118622] - Josef Dib, Cynthia Mongongu, Corinne Buisson, Adeline Molina, Wilhelm Schänzer, Uwe Thuss, Mario Thevis. Mass spectrometric characterization of the hypoxia-inducible factor (HIF) stabilizer drug candidate BAY 85-3934 (molidustat) and its glucuronidated metabolite BAY-348, and their implementation into routine doping controls.
Drug testing and analysis.
2017 Jan; 9(1):61-67. doi:
10.1002/dta.2011. [PMID: 27346747] - Ingo Flamme, Felix Oehme, Peter Ellinghaus, Mario Jeske, Jörg Keldenich, Uwe Thuss. Mimicking hypoxia to treat anemia: HIF-stabilizer BAY 85-3934 (Molidustat) stimulates erythropoietin production without hypertensive effects.
PloS one.
2014; 9(11):e111838. doi:
10.1371/journal.pone.0111838. [PMID: 25392999]
