Dovitinib (BioDeep_00000178529)
Secondary id: BioDeep_00000015449
human metabolite blood metabolite
代谢物信息卡片
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-1,3-benzodiazol-2-yl]-1,2-dihydroquinolin-2-one
化学式: C21H21FN6O (392.17607879999997)
中文名称: 多韦替尼
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CN1CCN(CC1)C1=CC=C2N=C(NC2=C1)C1=C(N)C2=C(NC1=O)C=CC=C2F
InChI: InChI=1S/C21H21FN6O/c1-27-7-9-28(10-8-27)12-5-6-14-16(11-12)25-20(24-14)18-19(23)17-13(22)3-2-4-15(17)26-21(18)29/h2-6,11H,7-10H2,1H3,(H,24,25)(H3,23,26,29)
描述信息
C274 - Antineoplastic Agent > C2189 - Signal Transduction Inhibitor > C129824 - Antineoplastic Protein Inhibitor
C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor > C1967 - Tyrosine Kinase Inhibitor
C471 - Enzyme Inhibitor > C129825 - Antineoplastic Enzyme Inhibitor
同义名列表
数据库引用编号
13 个数据库交叉引用编号
- ChEBI: CHEBI:91395
- KEGG: C75053
- PubChem: 135398510
- HMDB: HMDB0251597
- DrugBank: DB05928
- ChEMBL: CHEMBL4578973
- ChEMBL: CHEMBL522892
- Wikipedia: Fibroblast growth factor receptor 1
- chemspider: 11530944
- CAS: 1447274-99-8
- CAS: 1027263-12-2
- CAS: 804551-71-1
- CAS: 405169-16-6
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
- Suppakan Sripetch, Alexey Ryzhakov, Thorsteinn Loftsson. Preformulation studies of dovitinib free base: Solubility, lipophilicity and stability.
International journal of pharmaceutics.
2022 May; 619(?):121721. doi:
10.1016/j.ijpharm.2022.121721. [PMID: 35398252] - F J Sherida H Woei-A-Jin, Nir I Weijl, Mark C Burgmans, Arantza Fariña Sarasqueta, J Tom van Wezel, Martin N J M Wasser, Minneke J Coenraad, Jacobus Burggraaf, Susanne Osanto. Neoadjuvant Treatment with Angiogenesis-Inhibitor Dovitinib Prior to Local Therapy in Hepatocellular Carcinoma: A Phase II Study.
The oncologist.
2021 10; 26(10):854-864. doi:
10.1002/onco.13901. [PMID: 34251745] - Haitham AlRabiah, Adnan A Kadi, Haya I Aljohar, Mohamed W Attwa, Nasser S Al-Shakliah, Sabry M Attia, Gamal Ae Mostafa. A New Validated HPLC-MS/MS Method for Quantification and Pharmacokinetic Evaluation of Dovitinib, a Multi-Kinase Inhibitor, in Mouse Plasma.
Drug design, development and therapy.
2020; 14(?):407-415. doi:
10.2147/dddt.s223573. [PMID: 32095071] - Wen Wee Ma, Hao Xie, Gerald Fetterly, Laura Pitzonka, Amy Whitworth, Charles LeVea, John Wilton, Krystin Mantione, Sarah Schihl, Grace K Dy, Patrick Boland, Renuka Iyer, Wei Tan, William Brady, Robert M Straubinger, Alex A Adjei. A Phase Ib Study of the FGFR/VEGFR Inhibitor Dovitinib With Gemcitabine and Capecitabine in Advanced Solid Tumor and Pancreatic Cancer Patients.
American journal of clinical oncology.
2019 02; 42(2):184-189. doi:
10.1097/coc.0000000000000492. [PMID: 30418178] - Anne M Filppula, Tiffany M Mustonen, Janne T Backman. In Vitro Screening of Six Protein Kinase Inhibitors for Time-Dependent Inhibition of CYP2C8 and CYP3A4: Possible Implications with regard to Drug-Drug Interactions.
Basic & clinical pharmacology & toxicology.
2018 Dec; 123(6):739-748. doi:
10.1111/bcpt.13088. [PMID: 29956478] - Vincent A de Weger, Sanjay Goel, Roger von Moos, Jan H M Schellens, Nicholas Mach, Eugene Tan, Suraj Anand, Jeffrey W Scott, Ulrik Lassen. A drug-drug interaction study to assess the effect of the CYP1A2 inhibitor fluvoxamine on the pharmacokinetics of dovitinib (TKI258) in patients with advanced solid tumors.
Cancer chemotherapy and pharmacology.
2018 01; 81(1):73-80. doi:
10.1007/s00280-017-3469-4. [PMID: 29101463] - Kelly Gaudelot, Jean-Baptiste Gibier, Nicolas Pottier, Brigitte Hémon, Isabelle Van Seuningen, François Glowacki, Xavier Leroy, Christelle Cauffiez, Viviane Gnemmi, Sébastien Aubert, Michaël Perrais. Targeting miR-21 decreases expression of multi-drug resistant genes and promotes chemosensitivity of renal carcinoma.
Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine.
2017 Jul; 39(7):1010428317707372. doi:
10.1177/1010428317707372. [PMID: 28714373] - Yura Lee, Jung-Il Jung, Kyeong-Yong Park, Soon Ae Kim, Jiyeon Kim. Synergistic inhibition effect of TNIK inhibitor KY-05009 and receptor tyrosine kinase inhibitor dovitinib on IL-6-induced proliferation and Wnt signaling pathway in human multiple myeloma cells.
Oncotarget.
2017 Jun; 8(25):41091-41101. doi:
10.18632/oncotarget.17056. [PMID: 28467797] - Sergio Fernández-Pello, Fabian Hofmann, Rana Tahbaz, Lorenzo Marconi, Thomas B Lam, Laurence Albiges, Karim Bensalah, Steven E Canfield, Saeed Dabestani, Rachel H Giles, Milan Hora, Markus A Kuczyk, Axel S Merseburger, Thomas Powles, Michael Staehler, Alessandro Volpe, Börje Ljungberg, Axel Bex. A Systematic Review and Meta-analysis Comparing the Effectiveness and Adverse Effects of Different Systemic Treatments for Non-clear Cell Renal Cell Carcinoma.
European urology.
2017 03; 71(3):426-436. doi:
10.1016/j.eururo.2016.11.020. [PMID: 27939075] - Ann-Lii Cheng, Sumitra Thongprasert, Ho Yeong Lim, Wattana Sukeepaisarnjaroen, Tsai-Shen Yang, Cheng-Chung Wu, Yee Chao, Stephen L Chan, Masatoshi Kudo, Masafumi Ikeda, Yoon-Koo Kang, Hongming Pan, Kazushi Numata, Guohong Han, Binaifer Balsara, Yong Zhang, Ana-Marie Rodriguez, Yi Zhang, Yongyu Wang, Ronnie T P Poon. Randomized, open-label phase 2 study comparing frontline dovitinib versus sorafenib in patients with advanced hepatocellular carcinoma.
Hepatology (Baltimore, Md.).
2016 09; 64(3):774-84. doi:
10.1002/hep.28600. [PMID: 27082062] - S K Kang, A Volodarskiy, E L Ohmann, A V Balar, S Bangalore. Efficacy and Safety of Selective Vascular Endothelial Growth Factor Receptor Inhibitors Compared with Sorafenib for Metastatic Renal Cell Carcinoma: a Meta-analysis of Randomised Controlled Trials.
Clinical oncology (Royal College of Radiologists (Great Britain)).
2016 May; 28(5):334-41. doi:
10.1016/j.clon.2015.12.004. [PMID: 26723100] - Millie Das, Sukhmani K Padda, Adam Frymoyer, Lisa Zhou, Jonathan W Riess, Joel W Neal, Heather A Wakelee. Dovitinib and erlotinib in patients with metastatic non-small cell lung cancer: A drug-drug interaction.
Lung cancer (Amsterdam, Netherlands).
2015 Sep; 89(3):280-6. doi:
10.1016/j.lungcan.2015.06.011. [PMID: 26149476] - Jeffrey R Infante, Ramesh K Ramanathan, Daniel George, Eugene Tan, Michelle Quinlan, Angela Liu, Jeffrey W Scott, Sunil Sharma. A randomized, crossover phase 1 study to assess the effects of formulation (capsule vs tablet) and meal consumption on the bioavailability of dovitinib (TKI258).
Cancer chemotherapy and pharmacology.
2015 Apr; 75(4):729-37. doi:
10.1007/s00280-015-2681-3. [PMID: 25648347] - C Yoo, M-H Ryu, Y S Na, B-Y Ryoo, S R Park, Y-K Kang. Analysis of serum protein biomarkers, circulating tumor DNA, and dovitinib activity in patients with tyrosine kinase inhibitor-refractory gastrointestinal stromal tumors.
Annals of oncology : official journal of the European Society for Medical Oncology.
2014 Nov; 25(11):2272-2277. doi:
10.1093/annonc/mdu386. [PMID: 25149706] - Sunil Sharma, Carolyn D Britten, Joanne Mortimer, Swarupa Kulkarni, Michelle Quinlan, Angela Liu, Jeffrey W Scott, Daniel George. The effect of formulation and food consumption on the bioavailability of dovitinib (TKI258) in patients with advanced solid tumors.
Cancer chemotherapy and pharmacology.
2014 Oct; 74(4):867-74. doi:
10.1007/s00280-014-2454-4. [PMID: 25193431] - Xinhai Wan, Paul G Corn, Jun Yang, Nallasivam Palanisamy, Michael W Starbuck, Eleni Efstathiou, Elsa M Li Ning Tapia, Elsa M Li-Ning Tapia, Amado J Zurita, Ana Aparicio, Murali K Ravoori, Elba S Vazquez, Dan R Robinson, Yi-Mi Wu, Xuhong Cao, Matthew K Iyer, Wallace McKeehan, Vikas Kundra, Fen Wang, Patricia Troncoso, Arul M Chinnaiyan, Christopher J Logothetis, Nora M Navone. Prostate cancer cell-stromal cell crosstalk via FGFR1 mediates antitumor activity of dovitinib in bone metastases.
Science translational medicine.
2014 Sep; 6(252):252ra122. doi:
10.1126/scitranslmed.3009332. [PMID: 25186177] - Thomas Powles, Shah-Jalal Sarker Foreshew, Jonathan Shamash, Naveed Sarwar, Simon Crabb, Anju Sahdev, Jude Nixon, Louise Lim, Ashish Pungaliya, Abigail Foreshaw, Rachel Davies, Michelle Greenwood, Peter Wilson, Simon Pacey, Myra Galazi, Robert Jones, Simon Chowdhury. A phase Ib study investigating the combination of everolimus and dovitinib in vascular endothelial growth factor refractory clear cell renal cancer.
European journal of cancer (Oxford, England : 1990).
2014 Aug; 50(12):2057-64. doi:
10.1016/j.ejca.2014.04.021. [PMID: 24908540] - Bernard Escudier, Viktor Grünwald, Alain Ravaud, Yen-Chuan Ou, Daniel Castellano, Chia-Chi Lin, Jürgen E Gschwend, Andrea Harzstark, Sarah Beall, Nicoletta Pirotta, Matthew Squires, Michael Shi, Eric Angevin. Phase II results of Dovitinib (TKI258) in patients with metastatic renal cell cancer.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2014 Jun; 20(11):3012-22. doi:
10.1158/1078-0432.ccr-13-3006. [PMID: 24691021] - Manuela Schmidinger. Third-line dovitinib in metastatic renal cell carcinoma.
The Lancet. Oncology.
2014 Mar; 15(3):245-6. doi:
10.1016/s1470-2045(14)70082-8. [PMID: 24556039] - Robert J Motzer, Camillo Porta, Nicholas J Vogelzang, Cora N Sternberg, Cezary Szczylik, Jakub Zolnierek, Christian Kollmannsberger, Sun Young Rha, Georg A Bjarnason, Bohuslav Melichar, Ugo De Giorgi, Viktor Grünwald, Ian D Davis, Jae-Lyun Lee, Emilio Esteban, Gladys Urbanowitz, Can Cai, Matthew Squires, Mahtab Marker, Michael M Shi, Bernard Escudier. Dovitinib versus sorafenib for third-line targeted treatment of patients with metastatic renal cell carcinoma: an open-label, randomised phase 3 trial.
The Lancet. Oncology.
2014 Mar; 15(3):286-96. doi:
10.1016/s1470-2045(14)70030-0. [PMID: 24556040] - Aurore Blesius, Benoit Beuselinck, Christine Chevreau, Alain Ravaud, Frédéric Rolland, Stéphane Oudard, Bernard Escudier. Are tyrosine kinase inhibitors still active in patients with metastatic renal cell carcinoma previously treated with a tyrosine kinase inhibitor and everolimus? Experience of 36 patients treated in France in the RECORD-1 Trial.
Clinical genitourinary cancer.
2013 Jun; 11(2):128-33. doi:
10.1016/j.clgc.2012.12.001. [PMID: 23332872] - Eric Angevin, Jose A Lopez-Martin, Chia-Chi Lin, Jürgen E Gschwend, Andrea Harzstark, Daniel Castellano, Jean-Charles Soria, Paramita Sen, Julie Chang, Michael Shi, Andrea Kay, Bernard Escudier. Phase I study of dovitinib (TKI258), an oral FGFR, VEGFR, and PDGFR inhibitor, in advanced or metastatic renal cell carcinoma.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2013 Mar; 19(5):1257-68. doi:
10.1158/1078-0432.ccr-12-2885. [PMID: 23339124] - Xiaofeng Wang, Andrea Kay, Oezlem Anak, Eric Angevin, Bernard Escudier, Wei Zhou, Yilin Feng, Margaret Dugan, Horst Schran. Population pharmacokinetic/pharmacodynamic modeling to assist dosing schedule selection for dovitinib.
Journal of clinical pharmacology.
2013 Jan; 53(1):14-20. doi:
10.1177/0091270011433330. [PMID: 23400739] - Stéphane Oudard, Reza-Thierry Elaidi. Sequential therapy with targeted agents in patients with advanced renal cell carcinoma: optimizing patient benefit.
Cancer treatment reviews.
2012 Dec; 38(8):981-7. doi:
10.1016/j.ctrv.2011.12.009. [PMID: 22289686] - Anne-Charlotte Dubbelman, Alana Upthagrove, Jos H Beijnen, Serena Marchetti, Eugene Tan, Kimberly Krone, Suraj Anand, Jan H M Schellens. Disposition and metabolism of 14C-dovitinib (TKI258), an inhibitor of FGFR and VEGFR, after oral administration in patients with advanced solid tumors.
Cancer chemotherapy and pharmacology.
2012 Nov; 70(5):653-63. doi:
10.1007/s00280-012-1947-2. [PMID: 23010851] - Z Mihaly, Z Sztupinszki, P Surowiak, B Gyorffy. A comprehensive overview of targeted therapy in metastatic renal cell carcinoma.
Current cancer drug targets.
2012 Sep; 12(7):857-72. doi:
10.2174/156800912802429265. [PMID: 22515521] - Sharanya Sivanand, Samuel Peña-Llopis, Hong Zhao, Blanka Kucejova, Patrick Spence, Andrea Pavia-Jimenez, Toshinari Yamasaki, David J McBride, Jessica Gillen, Nicholas C Wolff, Lorraine Morlock, Yair Lotan, Ganesh V Raj, Arthur Sagalowsky, Vitaly Margulis, Jeffrey A Cadeddu, Mark T Ross, David R Bentley, Wareef Kabbani, Xian-Jin Xie, Payal Kapur, Noelle S Williams, James Brugarolas. A validated tumorgraft model reveals activity of dovitinib against renal cell carcinoma.
Science translational medicine.
2012 Jun; 4(137):137ra75. doi:
10.1126/scitranslmed.3003643. [PMID: 22674553] - Giuseppe Di Lorenzo, Matteo Ferro, Carlo Buonerba. How to carry out retrospective studies in metastatic renal cell cancer: two caveats that should be avoided.
Expert review of anticancer therapy.
2012 Mar; 12(3):331-3. doi:
10.1586/era.11.215. [PMID: 22369324] - Marine Gross-Goupil, Christophe Massard, Alain Ravaud. Targeted therapies in metastatic renal cell carcinoma: overview of the past year.
Current urology reports.
2012 Feb; 13(1):16-23. doi:
10.1007/s11934-011-0232-y. [PMID: 22139625] - Kevin B Kim, Jason Chesney, Douglas Robinson, Humphrey Gardner, Michael M Shi, John M Kirkwood. Phase I/II and pharmacodynamic study of dovitinib (TKI258), an inhibitor of fibroblast growth factor receptors and VEGF receptors, in patients with advanced melanoma.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2011 Dec; 17(23):7451-61. doi:
10.1158/1078-0432.ccr-11-1747. [PMID: 21976540] - V Grünwald, C Seidel, M Fenner, A Ganser, J Busch, S Weikert. Treatment of everolimus-resistant metastatic renal cell carcinoma with VEGF-targeted therapies.
British journal of cancer.
2011 Nov; 105(11):1635-9. doi:
10.1038/bjc.2011.389. [PMID: 22033275] - Sophie Roca, Amandine Quivy, Marine Gross-Goupil, Jean-Christophe Bernhard, Henri De Clermont, Alain Ravaud. Efficacy of re-challenging metastatic renal cell carcinoma with mTOR inhibitors.
Acta oncologica (Stockholm, Sweden).
2011 Oct; 50(7):1135-6. doi:
10.3109/0284186x.2011.592149. [PMID: 21726178] - H Rexer. [Third-line therapy for metastasized renal cell carcinoma: a randomized, multicenter non-blinded phase III study to compare safety and effectiveness of TF1258 versus sorafenib in patients with metastasized renal cell carcinoma following failure of antiangiogenic (VEGF targeted and mTOR inhibition) therapy (GOLD-AN 31/11 of the Working Group Urological Oncology)].
Der Urologe. Ausg. A.
2011 Oct; 50(10):1319-21. doi:
10.1007/s00120-011-2744-y. [PMID: 21976121] - Jonas Busch, Christoph Seidel, Steffen Weikert, Ingmar Wolff, Carsten Kempkensteffen, Lisa Weinkauf, Stefan Hinz, Ahmed Magheli, Kurt Miller, Viktor Grünwald. Intrinsic resistance to tyrosine kinase inhibitors is associated with poor clinical outcome in metastatic renal cell carcinoma.
BMC cancer.
2011 Jul; 11(?):295. doi:
10.1186/1471-2407-11-295. [PMID: 21756335] - Ya-Wen Hsiao, Yung-Chang Lin, Rosaline Chung-Yee Hui, Chih-Hsun Yang. Fulminant acneiform eruptions after administration of dovitinib in a patient with renal cell carcinoma.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
2011 Apr; 29(12):e340-1. doi:
10.1200/jco.2010.32.9458. [PMID: 21263088] - Pankaj Bhargava, Murray O Robinson. Development of second-generation VEGFR tyrosine kinase inhibitors: current status.
Current oncology reports.
2011 Apr; 13(2):103-11. doi:
10.1007/s11912-011-0154-3. [PMID: 21318618] - T Powles, S Chowdhury, R Jones, M Mantle, P Nathan, A Bex, L Lim, T Hutson. Sunitinib and other targeted therapies for renal cell carcinoma.
British journal of cancer.
2011 Mar; 104(5):741-5. doi:
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Annals of oncology : official journal of the European Society for Medical Oncology.
2010 Jul; 21(7):1559-1560. doi:
10.1093/annonc/mdq237. [PMID: 20444848]