Daprodustat (BioDeep_00000177958)
human metabolite blood metabolite
代谢物信息卡片
2-(1,3-Dicyclohexyl-6-hydroxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamido)acetic acid
化学式: C19H27N3O6 (393.1899762)
中文名称: 达普司他
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: C1CCC(CC1)N2C(=O)C(C(=O)N(C2=O)C3CCCCC3)C(=O)NCC(=O)O
InChI: InChI=1S/C19H27N3O6/c23-14(24)11-20-16(25)15-17(26)21(12-7-3-1-4-8-12)19(28)22(18(15)27)13-9-5-2-6-10-13/h12-13,15H,1-11H2,(H,20,25)(H,23,24)
描述信息
B - Blood and blood forming organs > B03 - Antianemic preparations
C78275 - Agent Affecting Blood or Body Fluid
Daprodustat (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor being developed for the treatment of anemia associated with chronic kidney disease.
同义名列表
6 个代谢物同义名
2-(1,3-Dicyclohexyl-6-hydroxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamido)acetic acid; 2-{[(1,3-dicyclohexyl-2,4,6-trioxo-1,3-diazinan-5-yl)(hydroxy)methylidene]amino}acetate; 2-[(1,3-dicyclohexyl-2,4,6-trioxo-1,3-diazinan-5-yl)formamido]acetic acid; [(1,3-dicyclohexyl-2,4,6-trioxo-1,3-diazinan-5-yl)formamido]acetic acid; Daprodustat; GSK1278863
数据库引用编号
8 个数据库交叉引用编号
- PubChem: 91617630
- HMDB: HMDB0250863
- DrugBank: DB11682
- ChEMBL: CHEMBL3544988
- Wikipedia: Daprodustat
- chemspider: 33427356
- CAS: 960539-70-2
- medchemexpress: HY-17608
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)
1 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
- Ajay K Singh, Borut Cizman, Kevin Carroll, John J V McMurray, Vlado Perkovic, Vivekanand Jha, Kirsten L Johansen, Renato D Lopes, Iain C Macdougall, Gregorio T Obrador, Sushrut S Waikar, Christoph Wanner, David C Wheeler, Andrzej Wiecek, Nicole Stankus, Frank Strutz, Allison Blackorby, Alexander R Cobitz, Amy M Meadowcroft, Gitanjali Paul, Prerna Ranganathan, Sangeeta Sedani, Scott Solomon. Efficacy and Safety of Daprodustat for Treatment of Anemia of Chronic Kidney Disease in Incident Dialysis Patients: A Randomized Clinical Trial.
JAMA internal medicine.
2022 06; 182(6):592-602. doi:
10.1001/jamainternmed.2022.0605. [PMID: 35377393] - Dimitrios Patoulias, Christodoulos Papadopoulos, Michael Doumas. Meta-Analysis Addressing the Cardiovascular Safety of Daprodustat in Patients With Chronic Kidney Disease Undergoing Dialysis or Not.
The American journal of cardiology.
2022 05; 170(?):166-167. doi:
10.1016/j.amjcard.2022.02.003. [PMID: 35260241] - Kelly M Mahar, Bonnie C Shaddinger, Bandi Ramanjineyulu, Susan Andrews, Stephen Caltabiano, Alistair C Lindsay, Alexander R Cobitz. Pharmacokinetics of Daprodustat and Metabolites in Individuals with Normal and Impaired Hepatic Function.
Clinical pharmacology in drug development.
2022 05; 11(5):562-575. doi:
10.1002/cpdd.1090. [PMID: 35355447] - Sheila A Doggrell. Are there advantages of daprodustat over erythropoiesis-stimulating agents (ESAs) in treating anemia associated with chronic kidney disease (CKD)?.
Expert opinion on pharmacotherapy.
2022 May; 23(7):769-773. doi:
10.1080/14656566.2022.2060078. [PMID: 35380500] - Ajay K Singh, Kevin Carroll, Vlado Perkovic, Scott Solomon, Vivekanand Jha, Kirsten L Johansen, Renato D Lopes, Iain C Macdougall, Gregorio T Obrador, Sushrut S Waikar, Christoph Wanner, David C Wheeler, Andrzej Więcek, Allison Blackorby, Borut Cizman, Alexander R Cobitz, Rich Davies, Jo Dole, Lata Kler, Amy M Meadowcroft, Xinyi Zhu, John J V McMurray. Daprodustat for the Treatment of Anemia in Patients Undergoing Dialysis.
The New England journal of medicine.
2021 12; 385(25):2325-2335. doi:
10.1056/nejmoa2113379. [PMID: 34739194] - Ajay K Singh, Kevin Carroll, John J V McMurray, Scott Solomon, Vivekanand Jha, Kirsten L Johansen, Renato D Lopes, Iain C Macdougall, Gregorio T Obrador, Sushrut S Waikar, Christoph Wanner, David C Wheeler, Andrzej Więcek, Allison Blackorby, Borut Cizman, Alexander R Cobitz, Rich Davies, Tara L DiMino, Lata Kler, Amy M Meadowcroft, Lin Taft, Vlado Perkovic. Daprodustat for the Treatment of Anemia in Patients Not Undergoing Dialysis.
The New England journal of medicine.
2021 12; 385(25):2313-2324. doi:
10.1056/nejmoa2113380. [PMID: 34739196] - Kelly M Mahar, Stephen Caltabiano, Susan Andrews, Bandi Ramanjineyulu, Liangfu Chen, Graeme Young, Adrian Pereira, Alistair C Lindsay, Frans van den Berg, Alexander R Cobitz. Clinical Pharmacokinetics of Daprodustat: Results of an Absorption, Distribution, and Excretion Study With Intravenous Microtracer and Concomitant Oral Doses for Bioavailability Determination.
Clinical pharmacology in drug development.
2021 12; 10(12):1419-1431. doi:
10.1002/cpdd.1029. [PMID: 34713596] - Hidetoshi Kanai, Masaomi Nangaku, Reiko Nagai, Nobuhiko Okuda, Kyo Kurata, Takashi Nagakubo, Yukihiro Endo, Alexander Cobitz. Efficacy and safety of daprodustat in Japanese peritoneal dialysis patients.
Therapeutic apheresis and dialysis : official peer-reviewed journal of the International Society for Apheresis, the Japanese Society for Apheresis, the Japanese Society for Dialysis Therapy.
2021 Dec; 25(6):979-987. doi:
10.1111/1744-9987.13686. [PMID: 33964183] - Monica Mazzarino, Ilaria Perretti, Carlotta Stacchini, Fabio Comunità, Xavier de la Torre, Francesco Botrè. UPLC-MS-Based Procedures to Detect Prolyl-Hydroxylase Inhibitors of HIF in Urine.
Journal of analytical toxicology.
2021 Feb; 45(2):184-194. doi:
10.1093/jat/bkaa055. [PMID: 32435795] - Mercedes Kile, Patcharaporn Sudchada. Current treatment practices for anemia in patients with chronic kidney disease and future opportunities with hypoxia-inducible factor prolyl hydroxylase inhibitors: a narrative review.
International urology and nephrology.
2021 Feb; 53(2):283-290. doi:
10.1007/s11255-020-02584-x. [PMID: 32770437] - Masanori Yamada, Minori Osamura, Hirofumi Ogura, Tomohiro Onoue, Akira Wakamatsu, Yotaro Numachi, Stephen Caltabiano, Kelly M Mahar. A Single-Dose, Open-Label, Randomized, Two-Way Crossover Study in Healthy Japanese Participants to Evaluate the Bioequivalence and the Food Effect on the Pharmacokinetics of Daprodustat.
Clinical pharmacology in drug development.
2020 11; 9(8):978-984. doi:
10.1002/cpdd.793. [PMID: 32250021] - Sohita Dhillon. Daprodustat: First Approval.
Drugs.
2020 Sep; 80(14):1491-1497. doi:
10.1007/s40265-020-01384-y. [PMID: 32880805] - Yoshiharu Tsubakihara, Tadao Akizawa, Masaomi Nangaku, Tomohiro Onoue, Taeko Yonekawa, Hideki Matsushita, Yukihiro Endo, Alexander Cobitz. A 24-Week Anemia Correction Study of Daprodustat in Japanese Dialysis Patients.
Therapeutic apheresis and dialysis : official peer-reviewed journal of the International Society for Apheresis, the Japanese Society for Apheresis, the Japanese Society for Dialysis Therapy.
2020 Apr; 24(2):108-114. doi:
10.1111/1744-9987.12962. [PMID: 31306555] - David F Adams, Mark S Watkins, Luc Durette, Josée Laliberté, Félix Goulet, Elaine Debien, Kendall S Frazier, Nacéra Mellal, Liangfu Chen, Wei Shi, Roberta Thomas, Erding Hu. Carcinogenicity Assessment of Daprodustat (GSK1278863), a Hypoxia-Inducible Factor (HIF)-Prolyl Hydroxylase Inhibitor.
Toxicologic pathology.
2020 02; 48(2):362-378. doi:
10.1177/0192623319880445. [PMID: 31640478] - Christine K Bailey, Stephen Caltabiano, Alexander R Cobitz, Chun Huang, Kelly M Mahar, Vickas V Patel. A randomized, 29-day, dose-ranging, efficacy and safety study of daprodustat, administered three times weekly in patients with anemia on hemodialysis.
BMC nephrology.
2019 10; 20(1):372. doi:
10.1186/s12882-019-1547-z. [PMID: 31619187] - Neil S Sanghani, Volker H Haase. Hypoxia-Inducible Factor Activators in Renal Anemia: Current Clinical Experience.
Advances in chronic kidney disease.
2019 07; 26(4):253-266. doi:
10.1053/j.ackd.2019.04.004. [PMID: 31477256] - Dengpiao Xie, Jianting Wang, Xinping Wu, Mingquan Li. Effect of daprodustat on anemia in patients with chronic kidney disease: a meta-analysis.
International urology and nephrology.
2018 Dec; 50(12):2201-2206. doi:
10.1007/s11255-018-1940-8. [PMID: 30073615] - Stephen Caltabiano, Kelly M Mahar, Karyn Lister, David Tenero, Ramiya Ravindranath, Borut Cizman, Alexander R Cobitz. The drug interaction potential of daprodustat when coadministered with pioglitazone, rosuvastatin, or trimethoprim in healthy subjects.
Pharmacology research & perspectives.
2018 04; 6(2):e00327. doi:
10.1002/prp2.327. [PMID: 29545948] - Kimberly A Becker, John J Jones. An Emerging Treatment Alternative for Anemia in Chronic Kidney Disease Patients: A Review of Daprodustat.
Advances in therapy.
2018 01; 35(1):5-11. doi:
10.1007/s12325-017-0655-z. [PMID: 29285707] - Jennifer L Ariazi, Kevin J Duffy, David F Adams, Duke M Fitch, Lusong Luo, Melissa Pappalardi, Mangatt Biju, Erin Hugger DiFilippo, Tony Shaw, Ken Wiggall, Connie Erickson-Miller. Discovery and Preclinical Characterization of GSK1278863 (Daprodustat), a Small Molecule Hypoxia Inducible Factor-Prolyl Hydroxylase Inhibitor for Anemia.
The Journal of pharmacology and experimental therapeutics.
2017 12; 363(3):336-347. doi:
10.1124/jpet.117.242503. [PMID: 28928122] - Stephen Caltabiano, Jon Collins, Gul Serbest, Lisa Morgan, Deborah A Smith, Ramiya Ravindranath, Alexander R Cobitz. A Randomized, Placebo- and Positive-Controlled, Single-Dose, Crossover Thorough QT/QTc Study Assessing the Effect of Daprodustat on Cardiac Repolarization in Healthy Subjects.
Clinical pharmacology in drug development.
2017 Nov; 6(6):627-640. doi:
10.1002/cpdd.342. [PMID: 28419747] - 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] - Tadao Akizawa, Yoshiharu Tsubakihara, Masaomi Nangaku, Yukihiro Endo, Hiromu Nakajima, Tomoko Kohno, Yukiko Imai, Natsumi Kawase, Katsutoshi Hara, John Lepore, Alexander Cobitz. Effects of Daprodustat, a Novel Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor on Anemia Management in Japanese Hemodialysis Subjects.
American journal of nephrology.
2017; 45(2):127-135. doi:
10.1159/000454818. [PMID: 27978511] - 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] - Mario Thevis, Susan Milosovich, Hermes Licea-Perez, Dana Knecht, Tom Cavalier, Wilhelm Schänzer. Mass spectrometric characterization of a prolyl hydroxylase inhibitor GSK1278863, its bishydroxylated metabolite, and its implementation into routine doping controls.
Drug testing and analysis.
2016 Aug; 8(8):858-63. doi:
10.1002/dta.1870. [PMID: 26361079] - Richard A Brigandi, Brendan Johnson, Coreen Oei, Mark Westerman, Gordana Olbina, Janak de Zoysa, Simon D Roger, Manisha Sahay, Nicholas Cross, Lawrence McMahon, Veerabhadra Guptha, Elena A Smolyarchuk, Narinder Singh, Steven F Russ, Sanjay Kumar. A Novel Hypoxia-Inducible Factor-Prolyl Hydroxylase Inhibitor (GSK1278863) for Anemia in CKD: A 28-Day, Phase 2A Randomized Trial.
American journal of kidney diseases : the official journal of the National Kidney Foundation.
2016 Jun; 67(6):861-71. doi:
10.1053/j.ajkd.2015.11.021. [PMID: 26827289] - Louis Holdstock, Amy M Meadowcroft, Rayma Maier, Brendan M Johnson, Delyth Jones, Anjay Rastogi, Steven Zeig, John J Lepore, Alexander R Cobitz. Four-Week Studies of Oral Hypoxia-Inducible Factor-Prolyl Hydroxylase Inhibitor GSK1278863 for Treatment of Anemia.
Journal of the American Society of Nephrology : JASN.
2016 Apr; 27(4):1234-44. doi:
10.1681/asn.2014111139. [PMID: 26494831] - Hermes Licea Perez, Dana Knecht, Christopher A Evans. Overcoming bioanalytical challenges associated with the separation and quantitation of GSK1278863, a HIF-prolyl hydroxylase inhibitor, and its 14 stereoisomeric metabolites.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2016 Jan; 1009-1010(?):7-16. doi:
10.1016/j.jchromb.2015.11.057. [PMID: 26688343] - Kelly K Andringa, Anupam Agarwal. Role of hypoxia-inducible factors in acute kidney injury.
Nephron. Clinical practice.
2014; 127(1-4):70-4. doi:
10.1159/000363669. [PMID: 25343825]