Dabrafenib Mesylate (BioDeep_00000774016)
代谢物信息卡片
Dabrafenib Mesylate
化学式: C24H24F3N5O5S3 (615.0892)
中文名称: 达帕菲尼甲磺酸盐
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F.CS(=O)(=O)O
InChI: 1H3,(H,2,3,4)
描述信息
C274 - Antineoplastic Agent > C2189 - Signal Transduction Inhibitor > C129824 - Antineoplastic Protein Inhibitor
C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor > C61074 - Serine/Threonine Kinase Inhibitor
C274 - Antineoplastic Agent > C163758 - Targeted Therapy Agent > C2336 - Raf Kinase Inhibitor
C471 - Enzyme Inhibitor > C129825 - Antineoplastic Enzyme Inhibitor
Dabrafenib Mesylate is a potent and selective Raf kinase inhibitor with IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively.
同义名列表
数据库引用编号
6 个数据库交叉引用编号
- ChEBI: CHEBI:75048
- KEGGdrug: D10104
- PubChem: 44516822
- ChEMBL: CHEMBL2105729
- CAS: 1195768-06-9
- medchemexpress: HY-14660A
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
- Fatemeh Aghai-Trommeschlaeger, Sebastian Zimmermann, Anja Gesierich, Charis Kalogirou, Maria-Elisabeth Goebeler, Pius Jung, Theo Pelzer, Max Kurlbaum, Hartwig Klinker, Nora Isberner, Oliver Scherf-Clavel. Comparison of a newly developed high performance liquid chromatography method with diode array detection to a liquid chromatography tandem mass spectrometry method for the quantification of cabozantinib, dabrafenib, nilotinib and osimertinib in human serum - Application to therapeutic drug monitoring.
Clinical biochemistry.
2022 Jul; 105-106(?):35-43. doi:
10.1016/j.clinbiochem.2022.04.011. [PMID: 35483452] - Hussein A Tawbi, Caroline Robert, Jan C Brase, Daniel Gusenleitner, Eduard Gasal, James Garrett, Alexander Savchenko, Güllü Görgün, Keith T Flaherty, Antoni Ribas, Reinhard Dummer, Dirk Schadendorf, Georgina V Long, Paul D Nathan, Paolo A Ascierto. Spartalizumab or placebo in combination with dabrafenib and trametinib in patients with BRAF V600-mutant melanoma: exploratory biomarker analyses from a randomized phase 3 trial (COMBI-i).
Journal for immunotherapy of cancer.
2022 06; 10(6):. doi:
10.1136/jitc-2021-004226. [PMID: 35728875] - Maria Russi, Gabriele Cavalieri, Domenico Marson, Erik Laurini, Sabrina Pricl. Binding of the B-Raf Inhibitors Dabrafenib and Vemurafenib to Human Serum Albumin: A Biophysical and Molecular Simulation Study.
Molecular pharmaceutics.
2022 05; 19(5):1619-1634. doi:
10.1021/acs.molpharmaceut.2c00100. [PMID: 35436118] - M Raynal, J-C Alvarez, P Saiag, A Beauchet, C Funck-Brentano, E Funck-Brentano. Monitoring of plasma concentrations of dabrafenib and trametinib in advanced BRAFV600mut melanoma patients.
Annales de dermatologie et de venereologie.
2022 Mar; 149(1):32-38. doi:
10.1016/j.annder.2021.04.005. [PMID: 34183171] - Harish Seethapathy, Meghan D Lee, Ian A Strohbehn, Orhan Efe, Nifasha Rusibamayila, Donald F Chute, Robert B Colvin, Ivy A Rosales, Riley M Fadden, Kerry L Reynolds, Ryan J Sullivan, Howard L Kaufman, Kenar D Jhaveri, Meghan E Sise. Clinical features of acute kidney injury in patients receiving dabrafenib and trametinib.
Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association.
2022 02; 37(3):507-514. doi:
10.1093/ndt/gfaa372. [PMID: 33355659] - Eunmi Jo, Harin Rhee. Dabrafenib- and trametinib-associated glomerular toxicity: A case report.
Medicine.
2022 Jan; 101(1):e28485. doi:
10.1097/md.0000000000028485. [PMID: 35029901] - Le Minh Pham, Kishwor Poudel, Cao Dai Phung, Tien Tiep Nguyen, Mahesh Pandit, Hanh Thuy Nguyen, Jae-Hoon Chang, Sung Giu Jin, Jee-Heon Jeong, Sae Kwang Ku, Han-Gon Choi, Chul Soon Yong, Jong Oh Kim. Preparation and evaluation of dabrafenib-loaded, CD47-conjugated human serum albumin-based nanoconstructs for chemoimmunomodulation.
Colloids and surfaces. B, Biointerfaces.
2021 Dec; 208(?):112093. doi:
10.1016/j.colsurfb.2021.112093. [PMID: 34482192] - Akimasa Sanagawa, Yuji Hotta, Nanaka Mori, Natsumi Tomita, Tomoya Kataoka, Masahiro Tohkin, Kazunori Kimura. BRAF/MEK inhibitor-associated nephrotoxicity in a real-world setting and human kidney cells.
Anti-cancer drugs.
2021 11; 32(10):1076-1083. doi:
10.1097/cad.0000000000001106. [PMID: 34232935] - Fernanda Bueno, Erika Abelleira, Florencia von Stecher, Andrea Paes de Lima, Fabián Pitoia. Dramatic clinical response to dabrafenib plus trametinib in anaplastic thyroid carcinoma and the challenges faced during the COVID-19 pandemic.
Archives of endocrinology and metabolism.
2021 Nov; 65(2):242-247. doi:
10.20945/2359-3997000000325. [PMID: 33587835] - Lauriane Goldwirt, B Louveau, B Baroudjian, C Allayous, F Jouenne, L Da Meda, L-T Vu, H Sauvageon, F Herms, J Delyon, C Lebbé, S Mourah. Dabrafenib and trametinib exposure-efficacy and tolerance in metastatic melanoma patients: a pharmacokinetic-pharmacodynamic real-life study.
Cancer chemotherapy and pharmacology.
2021 09; 88(3):427-437. doi:
10.1007/s00280-021-04299-x. [PMID: 34057572] - Zhennan Fang, Huiqiang Wei, Wenfeng Gou, Leyuan Chen, Changfen Bi, Wenbin Hou, Yiliang Li. Recent progress in small-molecule inhibitors for critical therapeutic targets of necroptosis.
Future medicinal chemistry.
2021 05; 13(9):817-837. doi:
10.4155/fmc-2020-0386. [PMID: 33845591] - Mahrukh M Syeda, Jennifer M Wiggins, Broderick C Corless, Georgina V Long, Keith T Flaherty, Dirk Schadendorf, Paul D Nathan, Caroline Robert, Antoni Ribas, Michael A Davies, Jean Jacques Grob, Eduard Gasal, Matthew Squires, Mahtab Marker, James Garrett, Jan C Brase, David Polsky. Circulating tumour DNA in patients with advanced melanoma treated with dabrafenib or dabrafenib plus trametinib: a clinical validation study.
The Lancet. Oncology.
2021 03; 22(3):370-380. doi:
10.1016/s1470-2045(20)30726-9. [PMID: 33587894] - Hiroki Hashimoto, Takamichi Ito, Taketoshi Ide, Natsuki Sasaki, Shiori Hikichi, Masutaka Furue. Pyrexia by COVID-19 in a patient treated with dabrafenib/trametinib therapy.
The Journal of dermatology.
2021 Feb; 48(2):e122-e123. doi:
10.1111/1346-8138.15696. [PMID: 33200424] - Francesca R Ogliari, Giovanni L Rodolfo Masera, Rossana Gueli, Claudio Chini. Dabrafenib and trametinib induced pancreatitis: a case report and review of the literature.
Anti-cancer drugs.
2021 02; 32(2):215-217. doi:
10.1097/cad.0000000000001009. [PMID: 33038084] - David Balakirouchenane, Nihel Khoudour, Sarah Guégan, Nora Kramkimel, Nathalie Franck, Thomas Rodier, François Goldwasser, Nicolas Dupin, Selim Aractingi, Michel Vidal, Benoit Blanchet. Simultaneous quantification of dabrafenib, hydroxy-dabrafenib and trametinib in human plasma by liquid chromatography-tandem mass spectrometry.
Journal of pharmaceutical and biomedical analysis.
2021 Jan; 193(?):113718. doi:
10.1016/j.jpba.2020.113718. [PMID: 33166838] - Ryo Amagai, Taku Fujimura, Yusuke Muto, Yumi Kambayashi, Sadanori Furudate, Kentaro Ohuchi, Takami Okuma, Akira Hashimoto, Setsuya Aiba. Serum soluble CD163 and proinflammatory chemokines may be biomarkers of the onset of adverse events in dabrafenib plus trametinib combination therapy for advanced melanoma.
Dermatologic therapy.
2021 01; 34(1):e14544. doi:
10.1111/dth.14544. [PMID: 33190370] - L Warburton, T M Meniawy, L Calapre, M Pereira, A McEvoy, M Ziman, E S Gray, M Millward. Stopping targeted therapy for complete responders in advanced BRAF mutant melanoma.
Scientific reports.
2020 11; 10(1):18878. doi:
10.1038/s41598-020-75837-5. [PMID: 33139839] - Yujie Liu, Hao Zeng, Ke Wang, Yalun Li, Panwen Tian, Weimin Li. Acquired BRAF N581S mutation mediated resistance to gefitinib and responded to dabrafenib plus trametinib.
Lung cancer (Amsterdam, Netherlands).
2020 08; 146(?):355-357. doi:
10.1016/j.lungcan.2020.06.004. [PMID: 32553555] - Lu Si, Xiaoshi Zhang, Sang Joon Shin, Yun Fan, Chia-Chi Lin, Tae Min Kim, Arunee Dechaphunkul, Jedzada Maneechavakajorn, Chi Sing Wong, Palanichamy Ilankumaran, Dung-Yang Lee, Eduard Gasal, Haifu Li, Jun Guo. Open-label, phase IIa study of dabrafenib plus trametinib in East Asian patients with advanced BRAF V600-mutant cutaneous melanoma.
European journal of cancer (Oxford, England : 1990).
2020 08; 135(?):31-38. doi:
10.1016/j.ejca.2020.04.044. [PMID: 32534242] - Ying Shi, Chunling Huang, Hao Yi, Qinghua Cao, Yongli Zhao, Jason Chen, Xinming Chen, Carol Pollock. RIPK3 blockade attenuates kidney fibrosis in a folic acid model of renal injury.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology.
2020 08; 34(8):10286-10298. doi:
10.1096/fj.201902544rr. [PMID: 32542792] - Chenyang He, Ulises Hernandez Ledezma, Pratik Gurnani, Thais Albelha, Kristofer J Thurecht, Ricardo Correia, Stephen P Morgan, Poulam Patel, Cameron Alexander, Sergiy Korposh. Surface polymer imprinted optical fibre sensor for dose detection of dabrafenib.
The Analyst.
2020 Jul; 145(13):4504-4511. doi:
10.1039/d0an00434k. [PMID: 32409797] - Ying Shi, Chunling Huang, Yongli Zhao, Qinghua Cao, Hao Yi, Xinming Chen, Carol Pollock. RIPK3 blockade attenuates tubulointerstitial fibrosis in a mouse model of diabetic nephropathy.
Scientific reports.
2020 06; 10(1):10458. doi:
10.1038/s41598-020-67054-x. [PMID: 32591618] - Anastasios Dimou, Gregory Barron, Daniel T Merrick, Jason Kolfenbach, Robert C Doebele. Granulomatosis with polyangiitis in a patient treated with dabrafenib and trametinib for BRAF V600E positive lung adenocarcinoma.
BMC cancer.
2020 Mar; 20(1):177. doi:
10.1186/s12885-020-6661-6. [PMID: 32131760] - M Piroth, C Frenard, G Quereux, A Khammari, S Corvec, B Dréno. Gut dysbiosis: not only with checkpoint inhibitors!.
Clinical and experimental dermatology.
2020 Mar; 45(2):247-249. doi:
10.1111/ced.14018. [PMID: 31222907] - Yuta Adachi, Naohiro Yanagimura, Chiaki Suzuki, Sakiko Ootani, Azusa Tanimoto, Akihiro Nishiyama, Kaname Yamashita, Koushiro Ohtsubo, Shinji Takeuchi, Seiji Yano. Reduced doses of dabrafenib and trametinib combination therapy for BRAF V600E-mutant non-small cell lung cancer prevent rhabdomyolysis and maintain tumor shrinkage: a case report.
BMC cancer.
2020 Feb; 20(1):156. doi:
10.1186/s12885-020-6626-9. [PMID: 32093631] - Shu-Su Liu, Yan-Yi Chen, Shao-Xia Wang, Qing Yu. Protective effect of dabrafenib on renal ischemia-reperfusion injury in vivo and in vitro.
Biochemical and biophysical research communications.
2020 02; 522(2):395-401. doi:
10.1016/j.bbrc.2019.11.105. [PMID: 31771879] - Synnøve Nymark Aasen, Heidi Espedal, Christopher Florian Holte, Olivier Keunen, Tine Veronika Karlsen, Olav Tenstad, Zaynah Maherally, Hrvoje Miletic, Tuyen Hoang, Anne Vaag Eikeland, Habib Baghirov, Dag Erlend Olberg, Geoffrey John Pilkington, Gobinda Sarkar, Robert B Jenkins, Terje Sundstrøm, Rolf Bjerkvig, Frits Thorsen. Improved Drug Delivery to Brain Metastases by Peptide-Mediated Permeabilization of the Blood-Brain Barrier.
Molecular cancer therapeutics.
2019 11; 18(11):2171-2181. doi:
10.1158/1535-7163.mct-19-0160. [PMID: 31467182] - Porntipa Korprasertthaworn, Nuy Chau, Pramod C Nair, Andrew Rowland, John O Miners. Inhibition of human UDP-glucuronosyltransferase (UGT) enzymes by kinase inhibitors: Effects of dabrafenib, ibrutinib, nintedanib, trametinib and BIBF 1202.
Biochemical pharmacology.
2019 11; 169(?):113616. doi:
10.1016/j.bcp.2019.08.018. [PMID: 31445021] - Manon de Vries-Brilland, Baptiste Sionneau, Caroline Dutriaux, Jean-Yves Blay, Alain Ravaud, Marine Gross-Goupil. Successful Treatment of Metastatic Adult Wilms Tumor With Anti-BRAF Treatment: A Case Report and a Brief Review of the Literature.
Clinical genitourinary cancer.
2019 08; 17(4):e721-e723. doi:
10.1016/j.clgc.2019.02.012. [PMID: 31109800] - Cristina C Santini, James Longden, Erwin M Schoof, Craig D Simpson, Grace R Jeschke, Pau Creixell, Jinho Kim, Xuewei Wu, Benjamin E Turk, Neal Rosen, Poulikos I Poulikakos, Rune Linding. Global view of the RAF-MEK-ERK module and its immediate downstream effectors.
Scientific reports.
2019 07; 9(1):10865. doi:
10.1038/s41598-019-47245-x. [PMID: 31350469] - Simona Caporali, Adriana Amaro, Lauretta Levati, Ester Alvino, Pedro Miguel Lacal, Simona Mastroeni, Federica Ruffini, Laura Bonmassar, Gian Carlo Antonini Cappellini, Nadia Felli, Alessandra Carè, Ulrich Pfeffer, Stefania D'Atri. miR-126-3p down-regulation contributes to dabrafenib acquired resistance in melanoma by up-regulating ADAM9 and VEGF-A.
Journal of experimental & clinical cancer research : CR.
2019 Jun; 38(1):272. doi:
10.1186/s13046-019-1238-4. [PMID: 31227006] - Sophie Leboulleux, Corinne Dupuy, Ludovic Lacroix, Marie Attard, Serena Grimaldi, Raphaël Corre, Marcel Ricard, Sarah Nasr, Amandine Berdelou, Julien Hadoux, Dana Hartl, Marie Terroir, Eric Baudin, Martin Schlumberger, Abir Al Ghuzlan. Redifferentiation of a BRAFK601E-Mutated Poorly Differentiated Thyroid Cancer Patient with Dabrafenib and Trametinib Treatment.
Thyroid : official journal of the American Thyroid Association.
2019 05; 29(5):735-742. doi:
10.1089/thy.2018.0457. [PMID: 30880598] - Alicja Puszkiel, Gaëlle Noé, Audrey Bellesoeur, Nora Kramkimel, Marie-Noëlle Paludetto, Audrey Thomas-Schoemann, Michel Vidal, François Goldwasser, Etienne Chatelut, Benoit Blanchet. Clinical Pharmacokinetics and Pharmacodynamics of Dabrafenib.
Clinical pharmacokinetics.
2019 04; 58(4):451-467. doi:
10.1007/s40262-018-0703-0. [PMID: 30094711] - Saki Akino, Hiroyuki Ohashi, Tatsuro Okano, Sora Takeuchi, Tamihiro Kawakami, Yoshinao Soma, Takafumi Kadono. Sudden elevation of plasma D-dimer levels induced by the combination therapy of dabrafenib and trametinib: Report of two cases.
The Journal of dermatology.
2019 Apr; 46(4):358-360. doi:
10.1111/1346-8138.14798. [PMID: 30719722] - Hannah Yejin Kim, Janna K Duong, Maria Gonzalez, Georgina V Long, Alexander M Menzies, Helen Rizos, Su Yin Lim, Jenny Lee, Alan V Boddy. Pharmacokinetic and cytokine profiles of melanoma patients with dabrafenib and trametinib-induced pyrexia.
Cancer chemotherapy and pharmacology.
2019 04; 83(4):693-704. doi:
10.1007/s00280-019-03780-y. [PMID: 30661097] - Zili Suo, Xinnuo Xiong, Qiaomei Sun, Ludan Zhao, Peixiao Tang, Quan Hou, Yongkui Zhang, Di Wu, Hui Li. Investigation on the Interaction of Dabrafenib with Human Serum Albumin Using Combined Experiment and Molecular Dynamics Simulation: Exploring the Binding Mechanism, Esterase-like Activity, and Antioxidant Activity.
Molecular pharmaceutics.
2018 12; 15(12):5637-5645. doi:
10.1021/acs.molpharmaceut.8b00806. [PMID: 30422663] - Evelina Cardoso, Thomas Mercier, Anna Dorothea Wagner, Krisztian Homicsko, Olivier Michielin, Kim Ellefsen-Lavoie, Laurène Cagnon, Manuel Diezi, Thierry Buclin, Nicolas Widmer, Chantal Csajka, Laurent Decosterd. Quantification of the next-generation oral anti-tumor drugs dabrafenib, trametinib, vemurafenib, cobimetinib, pazopanib, regorafenib and two metabolites in human plasma by liquid chromatography-tandem mass spectrometry.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2018 Apr; 1083(?):124-136. doi:
10.1016/j.jchromb.2018.02.008. [PMID: 29544202] - Naoya Yamazaki, Arata Tsutsumida, Akira Takahashi, Kenjiro Namikawa, Shusuke Yoshikawa, Yutaka Fujiwara, Shunsuke Kondo, Akihira Mukaiyama, Fanghong Zhang, Yoshio Kiyohara. Phase 1/2 study assessing the safety and efficacy of dabrafenib and trametinib combination therapy in Japanese patients with BRAF V600 mutation-positive advanced cutaneous melanoma.
The Journal of dermatology.
2018 Apr; 45(4):397-407. doi:
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Scientific reports.
2017 Nov; 7(1):15523. doi:
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Clinica chimica acta; international journal of clinical chemistry.
2017 Sep; 472(?):26-29. doi:
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Transplantation proceedings.
2017 Sep; 49(7):1551-1554. doi:
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American journal of kidney diseases : the official journal of the National Kidney Foundation.
2017 Jul; 70(1):145-150. doi:
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Clinica chimica acta; international journal of clinical chemistry.
2017 Jul; 470(?):8-13. doi:
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Analytical and bioanalytical chemistry.
2017 Jun; 409(15):3749-3756. doi:
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Drug metabolism and disposition: the biological fate of chemicals.
2017 06; 45(6):646-656. doi:
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Clinical journal of the American Society of Nephrology : CJASN.
2017 01; 12(1):176-189. doi:
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Pigment cell & melanoma research.
2017 01; 30(1):68-71. doi:
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Melanoma research.
2016 10; 26(5):532-4. doi:
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Journal of pharmaceutical and biomedical analysis.
2016 Jun; 125(?):270-9. doi:
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Electrophoresis.
2016 05; 37(10):1296-302. doi:
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Journal of translational medicine.
2016 Apr; 14(?):95. doi:
10.1186/s12967-016-0852-6. [PMID: 27095081] - Yanina J Jansen, Peter Janssens, Anne Hoorens, Max S Schreuer, Teofila Seremet, Sofie Wilgenhof, Bart Neyns. Granulomatous nephritis and dermatitis in a patient with BRAF V600E mutant metastatic melanoma treated with dabrafenib and trametinib.
Melanoma research.
2015 Dec; 25(6):550-4. doi:
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JAMA oncology.
2015 Nov; 1(8):1133-4. doi:
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Cancer.
2015 Nov; 121(21):3826-35. doi:
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