Vemurafenib (BioDeep_00000184925)
human metabolite blood metabolite
代谢物信息卡片
N-{3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl}propane-1-sulfonamide
化学式: C23H18ClF2N3O3S (489.07254120000005)
中文名称: 维罗非尼
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=C2C=C(C=N3)C4=CC=C(C=C4)Cl)F
InChI: InChI=1S/C23H18ClF2N3O3S/c1-2-9-33(31,32)29-19-8-7-18(25)20(21(19)26)22(30)17-12-28-23-16(17)10-14(11-27-23)13-3-5-15(24)6-4-13/h3-8,10-12,29H,2,9H2,1H3,(H,27,28)
描述信息
L - Antineoplastic and immunomodulating agents > L01 - Antineoplastic agents > L01E - Protein kinase inhibitors > L01EC - B-raf serine-threonine kinase (braf) inhibitors
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
D004791 - Enzyme Inhibitors > D047428 - Protein Kinase Inhibitors
D000970 - Antineoplastic Agents
Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
同义名列表
数据库引用编号
12 个数据库交叉引用编号
- ChEBI: CHEBI:63637
- PubChem: 42611257
- HMDB: HMDB0259779
- DrugBank: DB08881
- ChEMBL: CHEMBL1229517
- Wikipedia: Vemurafenib
- MeSH: Vemurafenib
- chemspider: 24747352
- CAS: 1029872-54-5
- CAS: 1415041-85-8
- CAS: 918504-65-1
- medchemexpress: HY-12057
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
- Gege Li, Changlong Zhou, Lu Wang, Yalong Zheng, Bo Zhou, Guoyan Li, Zhongyu Ma, Peng Sun, Yuantao Deng, Li Su, Junling Wang, Hongmei Cui. MitoCur-1 induces ferroptosis to reverse vemurafenib resistance in melanoma through inhibition of USP14.
Pigment cell & melanoma research.
2024 Mar; 37(2):316-328. doi:
10.1111/pcmr.13150. [PMID: 37985430] - Xingxian Guo, Shiying Huang, Yonghong Zhang, Hong Wang, Lisha Li, Jianhua Ran, Dilong Chen, Xiaopeng Li, Jing Li. Evodiamine inhibits growth of vemurafenib drug-resistant melanoma via suppressing IRS4/PI3K/AKT signaling pathway.
Journal of natural medicines.
2024 Mar; 78(2):342-354. doi:
10.1007/s11418-023-01769-9. [PMID: 38324123] - Aishwarya Saraswat, Richa Vartak, Rehab Hegazy, Yige Fu, Trishaal Janardhanam Raghavendra Rao, Blase Billack, Ketan Patel. Oral lipid nanocomplex of BRD4 PROteolysis TArgeting Chimera and vemurafenib for drug-resistant malignant melanoma.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie.
2023 Dec; 168(?):115754. doi:
10.1016/j.biopha.2023.115754. [PMID: 37871557] - Miguel Alpalhão, David Botequim, João Ferreira, René Santus, Paulo Filipe. Photosensitization of human skin fibroblasts by vemurafenib promotes pleiotropic effects on membrane-enclosed organelles and apoptosis.
Journal of photochemistry and photobiology. B, Biology.
2023 Jan; 238(?):112600. doi:
10.1016/j.jphotobiol.2022.112600. [PMID: 36434899] - J M van Berge Henegouwen, H van der Wijngaart, L J Zeverijn, L R Hoes, M Meertens, A D R Huitema, L A Devriese, M Labots, H M W Verheul, E E Voest, H Gelderblom. Efficacy and toxicity of vemurafenib and cobimetinib in relation to plasma concentrations, after administration via feeding tube in patients with BRAF-mutated thyroid cancer: a case series and review of literature.
Cancer chemotherapy and pharmacology.
2022 07; 90(1):97-104. doi:
10.1007/s00280-022-04437-z. [PMID: 35598186] - Paul B Googe, Stamatios Theocharis, Alexandros Pergaris, Haocheng Li, Yibing Yan, Edward F McKenna, Stergios J Moschos. Theragnostic significance of tumor-infiltrating lymphocytes and Ki67 in BRAFV600-mutant metastatic melanoma (BRIM-3 trial).
Current problems in cancer.
2022 06; 46(3):100862. doi:
10.1016/j.currproblcancer.2022.100862. [PMID: 35398635] - Hai-Yan Wang, Pian Yu, Xi-Sha Chen, Hui Wei, Shi-Jie Cao, Meng Zhang, Yi Zhang, Yong-Guang Tao, Dong-Sheng Cao, Feng Qiu, Yan Cheng. Identification of HMGCR as the anticancer target of physapubenolide against melanoma cells by in silico target prediction.
Acta pharmacologica Sinica.
2022 Jun; 43(6):1594-1604. doi:
10.1038/s41401-021-00745-x. [PMID: 34588618] - 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] - Heike Niessner, Markus Burkard, Christian Leischner, Olga Renner, Sarah Plöger, Francisco Meraz-Torres, Matti Böcker, Constanze Hirn, Ulrich M Lauer, Sascha Venturelli, Christian Busch, Tobias Sinnberg. Therapeutic Efficacy of Pharmacological Ascorbate on Braf Inhibitor Resistant Melanoma Cells In Vitro and In Vivo.
Cells.
2022 04; 11(7):. doi:
10.3390/cells11071229. [PMID: 35406796] - Meng-Ting Chang, Li-Chu Tsai, Kyoko Nakagawa-Goto, Kuo-Hsiung Lee, Lie-Fen Shyur. Phyto-sesquiterpene lactones DET and DETD-35 induce ferroptosis in vemurafenib sensitive and resistant melanoma via GPX4 inhibition and metabolic reprogramming.
Pharmacological research.
2022 04; 178(?):106148. doi:
10.1016/j.phrs.2022.106148. [PMID: 35231572] - Vatche Tchekmedyian, Lara Dunn, Eric Sherman, Shrujal S Baxi, Ravinder K Grewal, Steven M Larson, Keith S Pentlow, Sofia Haque, R Michael Tuttle, Mona M Sabra, Stephanie Fish, Laura Boucai, Jamie Walters, Ronald A Ghossein, Venkatraman E Seshan, Jeffrey A Knauf, David G Pfister, James A Fagin, Alan L Ho. Enhancing Radioiodine Incorporation in BRAF-Mutant, Radioiodine-Refractory Thyroid Cancers with Vemurafenib and the Anti-ErbB3 Monoclonal Antibody CDX-3379: Results of a Pilot Clinical Trial.
Thyroid : official journal of the American Thyroid Association.
2022 03; 32(3):273-282. doi:
10.1089/thy.2021.0565. [PMID: 35045748] - Yasir Q Almajidi, Nidhal K Maraie, Ayad M R Raauf. Modified solid in oil nanodispersion containing vemurafenib-lipid complex- in vitro/ in vivo study.
F1000Research.
2022; 11(?):841. doi:
10.12688/f1000research.123041.2. [PMID: 36339973] - Yuntao Bai, Ji Young Kim, Bijay Bisunke, Laura A Jayne, Josie A Silvaroli, Michael S Balzer, Megha Gandhi, Kevin M Huang, Veronika Sander, Jason Prosek, Rachel E Cianciolo, Sharyn D Baker, Alex Sparreboom, Kenar D Jhaveri, Katalin Susztak, Amandeep Bajwa, Navjot Singh Pabla. Kidney toxicity of the BRAF-kinase inhibitor vemurafenib is driven by off-target ferrochelatase inhibition.
Kidney international.
2021 12; 100(6):1214-1226. doi:
10.1016/j.kint.2021.08.022. [PMID: 34534550] - Xue Tang, Ju Gao, Zhi-Gui Ma, Xia Guo, Qiang Li, Zhi Wan, Jing-Jing Sun. Clinical and prognostic characteristics of 95 cases of Langerhans cell histiocytosis in children: a single-institute experience from 2013 to 2020.
Annals of medicine.
2021 12; 53(1):1537-1546. doi:
10.1080/07853890.2021.1966085. [PMID: 34459688] - Ryo Yamada, Motoko Yanagita. Unexpected cause of vemurafenib-induced nephrotoxicity: ferrochelatase.
Kidney international.
2021 12; 100(6):1158-1160. doi:
10.1016/j.kint.2021.09.010. [PMID: 34802553] - 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] - Mathilde Tardieu, Amélie Néron, Sophie Duvert-Lehembre, Islam Amine Larabi, Mohamed Barkaoui, Jean-Francois Emile, Arnaud Seigneurin, Franck Boralevi, Jean Donadieu. Cutaneous adverse events in children treated with vemurafenib for refractory BRAFV600E mutated Langerhans cell histiocytosis.
Pediatric blood & cancer.
2021 09; 68(9):e29140. doi:
10.1002/pbc.29140. [PMID: 34109735] - Veronica Valvo, Asumi Iesato, Taylor R Kavanagh, Carmen Priolo, Zsuzsanna Zsengeller, Alfredo Pontecorvi, Isaac E Stillman, Suzanne D Burke, Xiaowen Liu, Carmelo Nucera. Fine-Tuning Lipid Metabolism by Targeting Mitochondria-Associated Acetyl-CoA-Carboxylase 2 in BRAFV600E Papillary Thyroid Carcinoma.
Thyroid : official journal of the American Thyroid Association.
2021 09; 31(9):1335-1358. doi:
10.1089/thy.2020.0311. [PMID: 33107403] - Afshan Shirkavand, Ezeddin Mohajerani, Shirin Farivar, Leila Ataie-Fashtami, Mohammad Hossein Ghazimoradi. Monitoring the Response of Skin Melanoma Cell Line (A375) to Treatment with Vemurafenib: A Pilot In Vitro Optical Spectroscopic Study.
Photobiomodulation, photomedicine, and laser surgery.
2021 Mar; 39(3):164-177. doi:
10.1089/photob.2020.4887. [PMID: 33595357] - Aitor Benedicto, Iera Hernandez-Unzueta, Eduardo Sanz, Joana Márquez. Ocoxin Increases the Antitumor Effect of BRAF Inhibition and Reduces Cancer Associated Fibroblast-Mediated Chemoresistance and Protumoral Activity in Metastatic Melanoma.
Nutrients.
2021 Feb; 13(2):. doi:
10.3390/nu13020686. [PMID: 33669949] - Filip Janku, Divya Sakamuri, Shumei Kato, Helen J Huang, S Greg Call, Aung Naing, Veronica R Holley, Sapna P Patel, Rodabe N Amaria, Gerald S Falchook, Sarina A Piha-Paul, Ralph G Zinner, Apostolia M Tsimberidou, David S Hong, Funda Meric-Bernstam. Dose-escalation study of vemurafenib with sorafenib or crizotinib in patients with BRAF-mutated advanced cancers.
Cancer.
2021 02; 127(3):391-402. doi:
10.1002/cncr.33242. [PMID: 33119140] - Lin Run, Liping Wang, Xiting Nong, Nan Li, Xin Huang, Yang Xiao. Involvement of HMGB1 in vemurafenib resistance in thyroid cancer cells harboring BRAF (V600E) mutation by regulating excessive autophagy.
Endocrine.
2021 02; 71(2):418-426. doi:
10.1007/s12020-020-02417-y. [PMID: 32666385] - Ruhul Kayesh, Taleah Farasyn, Alexandra Crowe, Qiang Liu, Sonia Pahwa, Khondoker Alam, Sibylle Neuhoff, Oliver Hatley, Kai Ding, Wei Yue. Assessing OATP1B1- and OATP1B3-Mediated Drug-Drug Interaction Potential of Vemurafenib Using R-Value and Physiologically-Based Pharmacokinetic Models.
Journal of pharmaceutical sciences.
2021 01; 110(1):314-324. doi:
10.1016/j.xphs.2020.06.016. [PMID: 32590030] - Weijiang Zhang, Michael Mathisen, Grant R Goodman, Harper Forbes, Yuyao Song, Enric Bertran, Lev Demidov, Sang Joon Shin. Effect of Itraconazole, a Potent CYP3A4 Inhibitor, on the Steady-State Pharmacokinetics of Vemurafenib in Patients With BRAFV600 Mutation-Positive Malignancies.
Clinical pharmacology in drug development.
2021 01; 10(1):39-45. doi:
10.1002/cpdd.822. [PMID: 32602215] - Jianping Hu, Jieli Wei, Hyerin Yim, Li Wang, Ling Xie, Margaret S Jin, Md Kabir, Lihuai Qin, Xian Chen, Jing Liu, Jian Jin. Potent and Selective Mitogen-Activated Protein Kinase Kinase 1/2 (MEK1/2) Heterobifunctional Small-molecule Degraders.
Journal of medicinal chemistry.
2020 12; 63(24):15883-15905. doi:
10.1021/acs.jmedchem.0c01609. [PMID: 33284613] - 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] - Hechuan Wang, Janel Long-Boyle, Beth Apsel Winger, Theodore Nicolaides, Sabine Mueller, Michael Prados, Vijay Ivaturi. Population Pharmacokinetics of Vemurafenib in Children With Recurrent/Refractory BRAF Gene V600E-Mutant Astrocytomas.
Journal of clinical pharmacology.
2020 09; 60(9):1209-1219. doi:
10.1002/jcph.1617. [PMID: 32476174] - S Dasdelen, F Büschek. [Erdheim-Chester disease-A histiocytic multisystem disease with unusual renal involvement].
Der Internist.
2020 Sep; 61(9):969-979. doi:
10.1007/s00108-020-00849-2. [PMID: 32785740] - Fernanda S de Sousa, João L Baldim, Ricardo A Azevedo, Carlos R Figueiredo, Pauline Pieper, Claire E Sear, Edward A Anderson, João Henrique G Lago. Structure-activity relationship study of cytotoxic neolignan derivatives using multivariate analysis and computation-aided drug design.
Bioorganic & medicinal chemistry letters.
2020 08; 30(16):127349. doi:
10.1016/j.bmcl.2020.127349. [PMID: 32631547] - Patryk Górniak, Maja Wasylecka-Juszczyńska, Iwona Ługowska, Piotr Rutkowski, Anna Polak, Maciej Szydłowski, Przemysław Juszczyński. BRAF inhibition curtails IFN-gamma-inducible PD-L1 expression and upregulates the immunoregulatory protein galectin-1 in melanoma cells.
Molecular oncology.
2020 08; 14(8):1817-1832. doi:
10.1002/1878-0261.12695. [PMID: 32330348] - Weijiang Zhang, Christine McIntyre, Todd Riehl, Harper Forbes, Enric Bertran, Hye Jin Choi, Dae Ho Lee, Jeeyun Lee. Effect of Vemurafenib on the Pharmacokinetics of a Single Dose of Tizanidine (a CYP1A2 Substrate) in Patients With BRAFV600 Mutation-Positive Malignancies.
Clinical pharmacology in drug development.
2020 07; 9(5):651-658. doi:
10.1002/cpdd.788. [PMID: 32311241] - Sanju Sinha, Kuoyuan Cheng, Alejandro A Schäffer, Kenneth Aldape, Eyal Schiff, Eytan Ruppin. In vitro and in vivo identification of clinically approved drugs that modify ACE2 expression.
Molecular systems biology.
2020 07; 16(7):e9628. doi:
10.15252/msb.20209628. [PMID: 32729248] - Weijiang Zhang, Dawn Colburn, Brian Simmons, Zsuzsanna Papai, Enric Bertran, Simone Schadt, Christophe Husser, Harper Forbes, Dieter Roethlisberger, Thomas Hartung. Absolute Bioavailability of Vemurafenib in Patients With BRAFV600 Mutation-Positive Malignancies.
Clinical pharmacology in drug development.
2020 05; 9(4):496-504. doi:
10.1002/cpdd.773. [PMID: 32083398] - Ganessan Kichenadasse, Jim Henry Hughes, John O Miners, Arduino A Mangoni, Andrew Rowland, Ashley M Hopkins, Michael J Sorich. Relationship between vemurafenib plasma concentrations and survival outcomes in patients with advanced melanoma.
Cancer chemotherapy and pharmacology.
2020 03; 85(3):615-620. doi:
10.1007/s00280-019-04002-1. [PMID: 31786653] - Jessica Perrin, Thilo Werner, Nils Kurzawa, Anna Rutkowska, Dorothee D Childs, Mathias Kalxdorf, Daniel Poeckel, Eugenia Stonehouse, Katrin Strohmer, Bianca Heller, Douglas W Thomson, Jana Krause, Isabelle Becher, H Christian Eberl, Johanna Vappiani, Daniel C Sevin, Christina E Rau, Holger Franken, Wolfgang Huber, Maria Faelth-Savitski, Mikhail M Savitski, Marcus Bantscheff, Giovanna Bergamini. Identifying drug targets in tissues and whole blood with thermal-shift profiling.
Nature biotechnology.
2020 03; 38(3):303-308. doi:
10.1038/s41587-019-0388-4. [PMID: 31959954] - Teresa Delgado-Goñi, Teresa Casals Galobart, Slawomir Wantuch, Deimante Normantaite, Martin O Leach, Steven R Whittaker, Mounia Beloueche-Babari. Increased inflammatory lipid metabolism and anaplerotic mitochondrial activation follow acquired resistance to vemurafenib in BRAF-mutant melanoma cells.
British journal of cancer.
2020 01; 122(1):72-81. doi:
10.1038/s41416-019-0628-x. [PMID: 31819183] - Jean Donadieu, Islam Amine Larabi, Mathilde Tardieu, Johannes Visser, Caroline Hutter, Elena Sieni, Nabil Kabbara, Mohamed Barkaoui, Jean Miron, François Chalard, Paul Milne, Julien Haroche, Fleur Cohen, Zofia Hélias-Rodzewicz, Nicolas Simon, Mathilde Jehanne, Alexandra Kolenova, Anne Pagnier, Nathalie Aladjidi, Pascale Schneider, Geneviève Plat, Anne Lutun, Anne Sonntagbauer, Thomas Lehrnbecher, Alina Ferster, Viktoria Efremova, Martina Ahlmann, Laurence Blanc, James Nicholson, Anne Lambilliote, Houda Boudiaf, Andrej Lissat, Karel Svojgr, Fanette Bernard, Sarah Elitzur, Michal Golan, Dmitriy Evseev, Michael Maschan, Ahmed Idbaih, Olga Slater, Milen Minkov, Valerie Taly, Matthew Collin, Jean-Claude Alvarez, Jean-François Emile, Sébastien Héritier. Vemurafenib for Refractory Multisystem Langerhans Cell Histiocytosis in Children: An International Observational Study.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
2019 11; 37(31):2857-2865. doi:
10.1200/jco.19.00456. [PMID: 31513482] - Weijiang Zhang, Christine McIntyre, Harper Forbes, Rabab Gaafar, Hanaa Kohail, J Thaddeus Beck, Stjepko Plestina, Enric Bertran, Todd Riehl. Effect of Rifampicin on the Pharmacokinetics of a Single Dose of Vemurafenib in Patients With BRAFV600 Mutation-Positive Metastatic Malignancy.
Clinical pharmacology in drug development.
2019 08; 8(6):837-843. doi:
10.1002/cpdd.643. [PMID: 30570831] - 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] - Luigi Fattore, Ciro Francesco Ruggiero, Maria Elena Pisanu, Domenico Liguoro, Andrea Cerri, Susan Costantini, Francesca Capone, Mario Acunzo, Giulia Romano, Giovanni Nigita, Domenico Mallardo, Concetta Ragone, Maria Vincenza Carriero, Alfredo Budillon, Gerardo Botti, Paolo Antonio Ascierto, Rita Mancini, Gennaro Ciliberto. Reprogramming miRNAs global expression orchestrates development of drug resistance in BRAF mutated melanoma.
Cell death and differentiation.
2019 07; 26(7):1267-1282. doi:
10.1038/s41418-018-0205-5. [PMID: 30254376] - Kathryn E Cronise, Belen G Hernandez, Daniel L Gustafson, Dawn L Duval. Identifying the ErbB/MAPK Signaling Cascade as a Therapeutic Target in Canine Bladder Cancer.
Molecular pharmacology.
2019 07; 96(1):36-46. doi:
10.1124/mol.119.115808. [PMID: 31048548] - Darren J Wozniak, Ben Hitchinson, Milica B Gilic, Wenjun Bie, Vadim Gaponenko, Angela L Tyner. Vemurafenib Inhibits Active PTK6 in PTEN-null Prostate Tumor Cells.
Molecular cancer therapeutics.
2019 05; 18(5):937-946. doi:
10.1158/1535-7163.mct-18-0862. [PMID: 30926642] - Lara A Dunn, Eric J Sherman, Shrujal S Baxi, Vatche Tchekmedyian, Ravinder K Grewal, Steven M Larson, Keith S Pentlow, Sofia Haque, R Michael Tuttle, Mona M Sabra, Stephanie Fish, Laura Boucai, Jamie Walters, Ronald A Ghossein, Venkatraman E Seshan, Ai Ni, Duan Li, Jeffrey A Knauf, David G Pfister, James A Fagin, Alan L Ho. Vemurafenib Redifferentiation of BRAF Mutant, RAI-Refractory Thyroid Cancers.
The Journal of clinical endocrinology and metabolism.
2019 05; 104(5):1417-1428. doi:
10.1210/jc.2018-01478. [PMID: 30256977] - Raimundo Gonçalves de Oliveira Júnior, Antoine Bonnet, Estelle Braconnier, Hugo Groult, Grégoire Prunier, Laureen Beaugeard, Raphäel Grougnet, Jackson Roberto Guedes da Silva Almeida, Christiane Adrielly Alves Ferraz, Laurent Picot. Bixin, an apocarotenoid isolated from Bixa orellana L., sensitizes human melanoma cells to dacarbazine-induced apoptosis through ROS-mediated cytotoxicity.
Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association.
2019 Mar; 125(?):549-561. doi:
10.1016/j.fct.2019.02.013. [PMID: 30738990] - David Garandeau, Justine Noujarède, Justine Leclerc, Caroline Imbert, Virginie Garcia, Marie-Lise Bats, Florian Rambow, Julia Gilhodes, Thomas Filleron, Nicolas Meyer, Stéphanie Brayer, Silvia Arcucci, Sophie Tartare-Deckert, Bruno Ségui, Jean-Christophe Marine, Thierry Levade, Corine Bertolotto, Nathalie Andrieu-Abadie. Targeting the Sphingosine 1-Phosphate Axis Exerts Potent Antitumor Activity in BRAFi-Resistant Melanomas.
Molecular cancer therapeutics.
2019 02; 18(2):289-300. doi:
10.1158/1535-7163.mct-17-1141. [PMID: 30482853] - Yuzhen Niu, Yan Zhang, Xiaojun Yao. Resistance mechanism of the oncogenic β3-αC deletion mutation in BRAF kinase to dabrafenib and vemurafenib revealed by molecular dynamics simulations and binding free energy calculations.
Chemical biology & drug design.
2019 02; 93(2):177-187. doi:
10.1111/cbdd.13399. [PMID: 30225883] - Francesca Sciarretta, Chiara Fulci, Camilla Palumbo, Dante Rotili, Lucio Tentori, Grazia Graziani, Anna Maria Caccuri. Effects of Glutathione Transferase-Targeting Nitrobenzoxadiazole Compounds in Relation to PD-L1 Status in Human Melanoma Cells.
Chemotherapy.
2019; 64(3):138-145. doi:
10.1159/000503339. [PMID: 31639786] - Javier Ros, Eva Muñoz-Couselo. DRESS syndrome due to vemurafenib treatment: switching BRAF inhibitor to solve a big problem.
BMJ case reports.
2018 Sep; 2018(?):. doi:
10.1136/bcr-2018-224379. [PMID: 30275021] - Fleur Cohen-Aubart, Maryse Guerin, Lucie Poupel, Philippe Cluzel, Flora Saint-Charles, Frédéric Charlotte, Youssef Arsafi, Jean-François Emile, Eric Frisdal, Carine Le Goff, Jean Donadieu, Zahir Amoura, Philippe Lesnik, Julien Haroche, Wilfried Le Goff. Hypoalphalipoproteinemia and BRAFV600E Mutation Are Major Predictors of Aortic Infiltration in the Erdheim-Chester Disease.
Arteriosclerosis, thrombosis, and vascular biology.
2018 08; 38(8):1913-1925. doi:
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Nature communications.
2018 06; 9(1):2500. doi:
10.1038/s41467-018-04664-0. [PMID: 29950559] - Julia C Chisholm, Jozef Suvada, Ira J Dunkel, Michela Casanova, Weijiang Zhang, Natasha Ritchie, YounJeong Choi, Jane Park, Meghna Das Thakur, Stephen Simko, Nga Wan Rachel Tam, Andrea Ferrari. BRIM-P: A phase I, open-label, multicenter, dose-escalation study of vemurafenib in pediatric patients with surgically incurable, BRAF mutation-positive melanoma.
Pediatric blood & cancer.
2018 05; 65(5):e26947. doi:
10.1002/pbc.26947. [PMID: 29350463] - 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] - Weijiang Zhang, Dominik Heinzmann, Joseph F Grippo. Clinical Pharmacokinetics of Vemurafenib.
Clinical pharmacokinetics.
2017 09; 56(9):1033-1043. doi:
10.1007/s40262-017-0523-7. [PMID: 28255850] - Guanghui Ji, Yanfang Qian. Successful Treatment of Metastatic Upper Tract Urothelial Carcinoma With Vemurafenib: Case Report.
Clinical genitourinary cancer.
2017 08; 15(4):e719-e721. doi:
10.1016/j.clgc.2016.11.003. [PMID: 28024948] - Daniele Oddo, Giulia Siravegna, Annunziata Gloghini, Claudio Vernieri, Benedetta Mussolin, Federica Morano, Giovanni Crisafulli, Rosa Berenato, Giorgio Corti, Chiara Costanza Volpi, Michela Buscarino, Monica Niger, Philip D Dunne, Giuseppe Rospo, Emanuele Valtorta, Alice Bartolini, Giovanni Fucà, Simona Lamba, Antonia Martinetti, Maria Di Bartolomeo, Filippo de Braud, Alberto Bardelli, Filippo Pietrantonio, Federica Di Nicolantonio. Emergence of MET hyper-amplification at progression to MET and BRAF inhibition in colorectal cancer.
British journal of cancer.
2017 Jul; 117(3):347-352. doi:
10.1038/bjc.2017.196. [PMID: 28654634] - Marine Rousset, Karine Titier, Stephane Bouchet, Caroline Dutriaux, Anne Pham-Ledard, Sorilla Prey, Mireille Canal-Raffin, Mathieu Molimard. An UPLC-MS/MS method for the quantification of BRAF inhibitors (vemurafenib, dabrafenib) and MEK inhibitors (cobimetinib, trametinib, binimetinib) in human plasma. Application to treated melanoma patients.
Clinica chimica acta; international journal of clinical chemistry.
2017 Jul; 470(?):8-13. doi:
10.1016/j.cca.2017.04.009. [PMID: 28412197] - Luca Hegedũs, Tamás Garay, Eszter Molnár, Karolina Varga, Ágnes Bilecz, Szilvia Török, Rita Padányi, Katalin Pászty, Matthias Wolf, Michael Grusch, Enikõ Kállay, Balázs Döme, Walter Berger, Balázs Hegedũs, Agnes Enyedi. The plasma membrane Ca2+ pump PMCA4b inhibits the migratory and metastatic activity of BRAF mutant melanoma cells.
International journal of cancer.
2017 06; 140(12):2758-2770. doi:
10.1002/ijc.30503. [PMID: 27813079] - Paul Slobbe, Albert D Windhorst, Kevin Adamzek, Marije Bolijn, Robert C Schuit, Daniëlle A M Heideman, Guus A M S van Dongen, Alex J Poot. Development of [11C]vemurafenib employing a carbon-11 carbonylative Stille coupling and preliminary evaluation in mice bearing melanoma tumor xenografts.
Oncotarget.
2017 Jun; 8(24):38337-38350. doi:
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Targeted oncology.
2017 06; 12(3):365-371. doi:
10.1007/s11523-017-0491-8. [PMID: 28527094] - Cécile Teuma, Solenne Pelletier, Mona Amini-Adl, Marie Perier-Muzet, Delphine Maucort-Boulch, Luc Thomas, Maurice Laville, Denis Fouque, Stéphane Dalle. Adjunction of a MEK inhibitor to Vemurafenib in the treatment of metastatic melanoma results in a 60\% reduction of acute kidney injury.
Cancer chemotherapy and pharmacology.
2017 May; 79(5):1043-1049. doi:
10.1007/s00280-017-3300-2. [PMID: 28396940] - Peter Kubiniok, Hugo Lavoie, Marc Therrien, Pierre Thibault. Time-resolved Phosphoproteome Analysis of Paradoxical RAF Activation Reveals Novel Targets of ERK.
Molecular & cellular proteomics : MCP.
2017 04; 16(4):663-679. doi:
10.1074/mcp.m116.065128. [PMID: 28188228] - Drew C Deniger, Mei Li M Kwong, Anna Pasetto, Mark E Dudley, John R Wunderlich, Michelle M Langhan, Chyi-Chia Richard Lee, Steven A Rosenberg. A Pilot Trial of the Combination of Vemurafenib with Adoptive Cell Therapy in Patients with Metastatic Melanoma.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2017 Jan; 23(2):351-362. doi:
10.1158/1078-0432.ccr-16-0906. [PMID: 28093487] - Rimda Wanchoo, Ala Abudayyeh, Mona Doshi, Amaka Edeani, Ilya G Glezerman, Divya Monga, Mitchell Rosner, Kenar D Jhaveri. Renal Toxicities of Novel Agents Used for Treatment of Multiple Myeloma.
Clinical journal of the American Society of Nephrology : CJASN.
2017 01; 12(1):176-189. doi:
10.2215/cjn.06100616. [PMID: 27654928] - Nguyen Dinh Thang, Nguyen Van Minh, Pham Thu Huong. Translocation of BBAP from the cytoplasm to the nucleus reduces the metastatic ability of vemurafenib-resistant SKMEL28 cells.
Molecular medicine reports.
2017 Jan; 15(1):317-322. doi:
10.3892/mmr.2016.5976. [PMID: 27922665] - Ana Teixeira, Patrice Morlière, João Ferreira, Marie-Alix Conte, Antoine Galmiche, Jean-Claude Mazière, René Santus, Paulo Filipe. Interplay Between Membrane Lipid Peroxidation and Photoproduct Formation in the Ultraviolet A-Induced Phototoxicity of Vemurafenib in Skin Keratinocytes.
Toxicological sciences : an official journal of the Society of Toxicology.
2016 12; 154(2):289-295. doi:
10.1093/toxsci/kfw159. [PMID: 27566444] - Teresa Delgado-Goni, Maria Falck Miniotis, Slawomir Wantuch, Harold G Parkes, Richard Marais, Paul Workman, Martin O Leach, Mounia Beloueche-Babari. The BRAF Inhibitor Vemurafenib Activates Mitochondrial Metabolism and Inhibits Hyperpolarized Pyruvate-Lactate Exchange in BRAF-Mutant Human Melanoma Cells.
Molecular cancer therapeutics.
2016 12; 15(12):2987-2999. doi:
10.1158/1535-7163.mct-16-0068. [PMID: 27765851] - Alicja Puszkiel, Mélanie White-Koning, Nicolas Dupin, Nora Kramkimel, Audrey Thomas-Schoemann, Gaëlle Noé, Nicolas Chapuis, Michel Vidal, François Goldwasser, Etienne Chatelut, Benoit Blanchet. Plasma vemurafenib exposure and pre-treatment hepatocyte growth factor level are two factors contributing to the early peripheral lymphocytes depletion in BRAF-mutated melanoma patients.
Pharmacological research.
2016 11; 113(Pt A):709-718. doi:
10.1016/j.phrs.2016.06.032. [PMID: 27378568] - Vanessa Jean-Michel, Marc Coustans, Bassem Wehbe, Iona Metes, Pascale Siohan. Erdheim Chester disease: A rare obstructive case of acute renal failure.
Presse medicale (Paris, France : 1983).
2016 Nov; 45(11):1066-1069. doi:
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Journal of clinical pharmacology.
2016 10; 56(10):1307-12. doi:
10.1002/jcph.728. [PMID: 26918324] - Dariusz Borys, Lucas Nystrom, Albert Song, Laurie M Lomasney. Erdheim Chester disease with appendicular skeletal, renal and pleural involvement responding to Zelboraf (BRAF inhibitor) treatment: case report.
Skeletal radiology.
2016 Oct; 45(10):1397-402. doi:
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Biomedical chromatography : BMC.
2016 Aug; 30(8):1234-9. doi:
10.1002/bmc.3672. [PMID: 26683023] - Cécile Teuma, Marie Perier-Muzet, Solenne Pelletier, Mathilde Nouvier, Mona Amini-Adl, Frédérique Dijoud, Gérard Duru, Luc Thomas, Denis Fouque, Maurice Laville, Stéphane Dalle. New insights into renal toxicity of the B-RAF inhibitor, vemurafenib, in patients with metastatic melanoma.
Cancer chemotherapy and pharmacology.
2016 Aug; 78(2):419-26. doi:
10.1007/s00280-016-3086-7. [PMID: 27371224] - M van der Graaf, C Seynaeve, W Kruit. A medical cause for fifty shades of grey.
The Netherlands journal of medicine.
2016 Aug; 74(7):320. doi:
NULL. [PMID: 27571952] - Jia-Hua Feng, Kyoko Nakagawa-Goto, Kuo-Hsiung Lee, Lie-Fen Shyur. A Novel Plant Sesquiterpene Lactone Derivative, DETD-35, Suppresses BRAFV600E Mutant Melanoma Growth and Overcomes Acquired Vemurafenib Resistance in Mice.
Molecular cancer therapeutics.
2016 06; 15(6):1163-76. doi:
10.1158/1535-7163.mct-15-0973. [PMID: 27048951] - Heike Seifert, Rosalie Fisher, Juan Martin-Liberal, Kim Edmonds, Peta Hughes, Komel Khabra, Martin Gore, James Larkin. Prognostic markers and tumour growth kinetics in melanoma patients progressing on vemurafenib.
Melanoma research.
2016 Apr; 26(2):138-44. doi:
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Targeted oncology.
2016 Feb; 11(1):59-69. doi:
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Oncotarget.
2016 Jan; 7(4):4428-41. doi:
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PloS one.
2016; 11(3):e0149873. doi:
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Cancer chemotherapy and pharmacology.
2015 Nov; 76(5):917-24. doi:
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Cancer.
2015 Nov; 121(21):3826-35. doi:
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JAMA oncology.
2015 Nov; 1(8):1133-4. doi:
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Oncotarget.
2015 Sep; 6(27):24205-17. doi:
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Melanoma research.
2015 Aug; 25(4):302-5. doi:
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Journal of medical case reports.
2015 Jul; 9(?):158. doi:
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Annals of oncology : official journal of the European Society for Medical Oncology.
2015 Jul; 26(7):1470-5. doi:
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Journal of translational medicine.
2015 Jun; 13(?):191. doi:
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European journal of internal medicine.
2015 May; 26(4):223-9. doi:
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Pharmacology research & perspectives.
2015 Mar; 3(2):e00113. doi:
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Annals of oncology : official journal of the European Society for Medical Oncology.
2015 Mar; 26(3):573-82. doi:
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Therapeutic drug monitoring.
2015 Feb; 37(1):132-6. doi:
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Biochemical pharmacology.
2015 Feb; 93(3):290-304. doi:
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Clinical chemistry.
2015 Jan; 61(1):297-304. doi:
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Journal of immunotherapy (Hagerstown, Md. : 1997).
2015 Jan; 38(1):12-23. doi:
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Expert review of clinical immunology.
2015; 11(9):1033-42. doi:
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Asian Pacific journal of cancer prevention : APJCP.
2015; 16(2):699-705. doi:
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The British journal of dermatology.
2014 Dec; 171(6):1529-32. doi:
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Pharmaceutical research.
2014 Dec; 31(12):3487-502. doi:
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Analytical and bioanalytical chemistry.
2014 Sep; 406(22):5513-20. doi:
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Journal of pharmaceutical and biomedical analysis.
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