Trametinib (BioDeep_00000273069)
代谢物信息卡片
Trametinib (GSK1120212)
化学式: C26H23FIN5O4 (615.0779)
中文名称: 曲美替尼
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CC(=O)Nc1cccc(-n2c(=O)n(C3CC3)c(=O)c3c(Nc4ccc(I)cc4F)n(C)c(=O)c(C)c32)c1
InChI: InChI=1S/C26H23FIN5O4/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34)
描述信息
L - Antineoplastic and immunomodulating agents > L01 - Antineoplastic agents > L01E - Protein kinase inhibitors > L01EE - Mitogen-activated protein kinase (mek) inhibitors
C274 - Antineoplastic Agent > C163758 - Targeted Therapy Agent > C69145 - Mitogen-Activated Protein Kinase Kinase Inhibitor
C274 - Antineoplastic Agent > C2189 - Signal Transduction Inhibitor > C129824 - Antineoplastic Protein Inhibitor
C471 - Enzyme Inhibitor > C129825 - Antineoplastic Enzyme Inhibitor
D004791 - Enzyme Inhibitors > D047428 - Protein Kinase Inhibitors
C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor
D000970 - Antineoplastic Agents
Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
同义名列表
4 个代谢物同义名
数据库引用编号
8 个数据库交叉引用编号
- ChEBI: CHEBI:75998
- KEGGdrug: D10175
- PubChem: 11707110
- DrugBank: DB08911
- ChEMBL: CHEMBL2103875
- CAS: 871700-17-3
- PMhub: MS000004822
- medchemexpress: HY-10999
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 |
|---|
文献列表
- Eric Bouffet, Jordan R Hansford, Maria Luisa Garrè, Junichi Hara, Ashley Plant-Fox, Isabelle Aerts, Franco Locatelli, Jasper van der Lugt, Ludmila Papusha, Felix Sahm, Uri Tabori, Kenneth J Cohen, Roger J Packer, Olaf Witt, Larissa Sandalic, Ana Bento Pereira da Silva, Mark Russo, Darren R Hargrave. Dabrafenib plus Trametinib in Pediatric Glioma with BRAF V600 Mutations.
The New England journal of medicine.
2023 Sep; 389(12):1108-1120. doi:
10.1056/nejmoa2303815. [PMID: 37733309] - 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] - 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] - Pei Jye Voon, Eric X Chen, Helen X Chen, Albert C Lockhart, Solmaz Sahebjam, Karen Kelly, Ulka N Vaishampayan, Vivek Subbiah, Albiruni R Razak, Daniel J Renouf, Sebastien J Hotte, Arti Singh, Philippe L Bedard, Aaron R Hansen, S Percy Ivy, Lisa Wang, Lee-Anne Stayner, Lillian L Siu, Anna Spreafico. Phase I pharmacokinetic study of single agent trametinib in patients with advanced cancer and hepatic dysfunction.
Journal of experimental & clinical cancer research : CR.
2022 Feb; 41(1):51. doi:
10.1186/s13046-021-02236-7. [PMID: 35130943] - 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] - Kanan Alshammari, Kyaw L Aung, Tong Zhang, Albiruni R A Razak, Stefano Serra, Tracy Stockley, Lisa Wang, Jessica Nguyen, Anna Spreafico, Aaron R Hansen, Dave Zwir, Lillian L Siu, Philippe L Bedard. Phase II Trial of Trametinib and Panitumumab in RAS/RAF Wild Type Metastatic Colorectal Cancer.
Clinical colorectal cancer.
2021 12; 20(4):334-341. doi:
10.1016/j.clcc.2021.07.004. [PMID: 34417144] - 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] - Oren Yakovian, Julia Sajman, Rand Arafeh, Yair Neve-Oz, Michal Alon, Yardena Samuels, Eilon Sherman. MEK Inhibition Reverses Aberrant Signaling in Melanoma Cells through Reorganization of NRas and BRAF in Self Nanoclusters.
Cancer research.
2021 03; 81(5):1279-1292. doi:
10.1158/0008-5472.can-20-1205. [PMID: 33355187] - 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] - 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] - 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] - 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] - Samir Chtita, Assia Belhassan, Adnane Aouidate, Salah Belaidi, Mohammed Bouachrine, Tahar Lakhlifi. Discovery of Potent SARS-CoV-2 Inhibitors from Approved Antiviral Drugs via Docking and Virtual Screening.
Combinatorial chemistry & high throughput screening.
2021; 24(3):441-454. doi:
10.2174/1386207323999200730205447. [PMID: 32748740] - Chunyan Dai, Li Shen, Weiyang Jin, Bing Lv, Pei Liu, Xi Wang, Yifei Yin, Yufei Fu, Liguo Liang, Zhongjun Ma, Xiaojian Zhang, Yiping Wang, Daogun Xu, Zhe Chen. Physapubescin B enhances the sensitivity of gastric cancer cells to trametinib by inhibiting the STAT3 signaling pathway.
Toxicology and applied pharmacology.
2020 12; 408(?):115273. doi:
10.1016/j.taap.2020.115273. [PMID: 33035574] - Justin B Collier, Rick G Schnellmann. Extracellular signal-regulated kinase 1/2 regulates NAD metabolism during acute kidney injury through microRNA-34a-mediated NAMPT expression.
Cellular and molecular life sciences : CMLS.
2020 Sep; 77(18):3643-3655. doi:
10.1007/s00018-019-03391-z. [PMID: 31873757] - 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] - Carolyn N Brown, Daniel J Atwood, Deepak Pokhrel, Kameswaran Ravichandran, Sara J Holditch, Sanskriti Saxena, Makoto Miyazaki, Raphael Nemenoff, Mary C M Weiser-Evans, Danica Galesic Ljubanovic, Melanie S Joy, Charles L Edelstein. The effect of MEK1/2 inhibitors on cisplatin-induced acute kidney injury (AKI) and cancer growth in mice.
Cellular signalling.
2020 07; 71(?):109605. doi:
10.1016/j.cellsig.2020.109605. [PMID: 32194168] - Grace Egan, Jill Hamilton, Tara McKeown, Eric Bouffet, Uri Tabori, Peter Dirks, Ute Bartels. Trametinib Toxicities in Patients With Low-grade Gliomas and Diabetes Insipidus: Related Findings?.
Journal of pediatric hematology/oncology.
2020 05; 42(4):e248-e250. doi:
10.1097/mph.0000000000001427. [PMID: 30676433] - Wen-Fu Xu, Zhu-Jun Wang, Kun Li, Ya-Qing Shen, Ke Lu, Xue-Yan Lv, Yu-Xi Wen, Run-Ming Jin. Huai Qi Huang-induced Apoptosis via Down-regulating PRKCH and Inhibiting RAF/MEK/ERK Pathway in Ph+ Leukemia Cells.
Current medical science.
2020 Apr; 40(2):354-362. doi:
10.1007/s11596-020-2181-5. [PMID: 32337697] - 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] - Shannon N Westin, Michael W Sill, Robert L Coleman, Steven Waggoner, Kathleen N Moore, Cara A Mathews, Lainie P Martin, Susan C Modesitt, Sanghoon Lee, Zhenlin Ju, Gordon B Mills, Russell J Schilder, Paula M Fracasso, Michael J Birrer, Carol Aghajanian. Safety lead-in of the MEK inhibitor trametinib in combination with GSK2141795, an AKT inhibitor, in patients with recurrent endometrial cancer: An NRG Oncology/GOG study.
Gynecologic oncology.
2019 12; 155(3):420-428. doi:
10.1016/j.ygyno.2019.09.024. [PMID: 31623857] - 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] - Jorge Iván Castillo-Quan, Luke S Tain, Kerri J Kinghorn, Li Li, Sebastian Grönke, Yvonne Hinze, T Keith Blackwell, Ivana Bjedov, Linda Partridge. A triple drug combination targeting components of the nutrient-sensing network maximizes longevity.
Proceedings of the National Academy of Sciences of the United States of America.
2019 10; 116(42):20817-20819. doi:
10.1073/pnas.1913212116. [PMID: 31570569] - Ranjan Das, Soo-Jin Kim, Nhung Thi Nguyen, Hyeong Ju Kwon, Seung-Kuy Cha, Kyu-Sang Park. Inhibition of the ERK1/2-mTORC1 axis ameliorates proteinuria and the fibrogenic action of transforming growth factor-β in Adriamycin-induced glomerulosclerosis.
Kidney international.
2019 10; 96(4):927-941. doi:
10.1016/j.kint.2019.05.006. [PMID: 31377057] - Ji Young Yoo, Jessica Swanner, Yoshihiro Otani, Mitra Nair, Flora Park, Yeshavanth Banasavadi-Siddegowda, Joseph Liu, Alena Cristina Jaime-Ramirez, Bangxing Hong, Feng Geng, Deliang Guo, Darlene Bystry, Mitch Phelphs, Haroon Quadri, Tae Jin Lee, Balveen Kaur. Oncolytic HSV therapy increases trametinib access to brain tumors and sensitizes them in vivo.
Neuro-oncology.
2019 09; 21(9):1131-1140. doi:
10.1093/neuonc/noz079. [PMID: 31063549] - 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] - Harry P Erba, Pamela S Becker, Paul J Shami, Michael R Grunwald, Donna L Flesher, Min Zhu, Erik Rasmussen, Haby A Henary, Abraham A Anderson, Eunice S Wang. Phase 1b study of the MDM2 inhibitor AMG 232 with or without trametinib in relapsed/refractory acute myeloid leukemia.
Blood advances.
2019 07; 3(13):1939-1949. doi:
10.1182/bloodadvances.2019030916. [PMID: 31253596] - 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] - N Li, X-Y Lu, W-Y Shi, F-J Mao, X-Y Yang, Y-B Luo, W Li. Combined mTOR/MEK inhibition prevents proliferation and induces apoptosis in NF2-mutant tumors.
European review for medical and pharmacological sciences.
2019 Jul; 23(13):5874-5883. doi:
10.26355/eurrev_201907_18331. [PMID: 31298338] - 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] - 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] - Petros Andrikopoulos, Julius Kieswich, Sabrina Pacheco, Luxme Nadarajah, Steven Michael Harwood, Caroline E O'Riordan, Christoph Thiemermann, Muhammad M Yaqoob. The MEK Inhibitor Trametinib Ameliorates Kidney Fibrosis by Suppressing ERK1/2 and mTORC1 Signaling.
Journal of the American Society of Nephrology : JASN.
2019 01; 30(1):33-49. doi:
10.1681/asn.2018020209. [PMID: 30530834] - 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] - David A Barbie, Alexander Spira, Karen Kelly, Rita Humeniuk, Jun Kawashima, Shengchun Kong, Marianna Koczywas. Phase 1B Study of Momelotinib Combined With Trametinib in Metastatic, Kirsten Rat Sarcoma Viral Oncogene Homolog-Mutated Non-Small-Cell Lung Cancer After Platinum-Based Chemotherapy Treatment Failure.
Clinical lung cancer.
2018 11; 19(6):e853-e859. doi:
10.1016/j.cllc.2018.07.004. [PMID: 30087028] - Marilia Takada, Jeremy M L Hix, Sarah Corner, Peter Z Schall, Matti Kiupel, Vilma Yuzbasiyan-Gurkan. Targeting MEK in a Translational Model of Histiocytic Sarcoma.
Molecular cancer therapeutics.
2018 11; 17(11):2439-2450. doi:
10.1158/1535-7163.mct-17-1273. [PMID: 30135215] - Ali Talebi, Jonas Dehairs, Florian Rambow, Aljosja Rogiers, David Nittner, Rita Derua, Frank Vanderhoydonc, Joao A G Duarte, Francesca Bosisio, Kathleen Van den Eynde, Kris Nys, Mónica Vara Pérez, Patrizia Agostinis, Etienne Waelkens, Joost Van den Oord, Sarah-Maria Fendt, Jean-Christophe Marine, Johannes V Swinnen. Sustained SREBP-1-dependent lipogenesis as a key mediator of resistance to BRAF-targeted therapy.
Nature communications.
2018 06; 9(1):2500. doi:
10.1038/s41467-018-04664-0. [PMID: 29950559] - 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:
10.1111/1346-8138.14210. [PMID: 29399853] - S M Boyle, N Ali, A J Olszanski, D J Park, G Xiao, S Guy, A M Doyle. Donor-Derived Metastatic Melanoma and Checkpoint Inhibition.
Transplantation proceedings.
2017 Sep; 49(7):1551-1554. doi:
10.1016/j.transproceed.2017.06.007. [PMID: 28838438] - Luca Perico, Mario Mandalà, Arrigo Schieppati, Camillo Carrara, Paola Rizzo, Sara Conti, Lorena Longaretti, Ariela Benigni, Giuseppe Remuzzi. BRAF Signaling Pathway Inhibition, Podocyte Injury, and Nephrotic Syndrome.
American journal of kidney diseases : the official journal of the National Kidney Foundation.
2017 Jul; 70(1):145-150. doi:
10.1053/j.ajkd.2016.12.013. [PMID: 28242136] - 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] - John J Park, Alan V Boddy, Xiaoman Liu, David Harris, Vincent Lee, Richard F Kefford, Matteo S Carlino. Pharmacokinetics of dabrafenib in a patient with metastatic melanoma undergoing haemodialysis.
Pigment cell & melanoma research.
2017 01; 30(1):68-71. doi:
10.1111/pcmr.12557. [PMID: 27863085] - Amita Patnaik, Anthony Tolcher, Kyriakos P Papadopoulos, Murali Beeram, Drew Rasco, Theresa L Werner, John W Bauman, Anita Scheuber, Donna S Cox, Bela R Patel, YanYan Zhou, Mohammed Hamid, Daniel Schramek, Sunil Sharma. Phase 1 study to evaluate the effect of the MEK inhibitor trametinib on cardiac repolarization in patients with solid tumours.
Cancer chemotherapy and pharmacology.
2016 Sep; 78(3):491-500. doi:
10.1007/s00280-016-3090-y. [PMID: 27392790] - Joshua A Smith, Philip R Mayeux, Rick G Schnellmann. Delayed Mitogen-Activated Protein Kinase/Extracellular Signal-Regulated Kinase Inhibition by Trametinib Attenuates Systemic Inflammatory Responses and Multiple Organ Injury in Murine Sepsis.
Critical care medicine.
2016 08; 44(8):e711-20. doi:
10.1097/ccm.0000000000001672. [PMID: 27031380] - C M Nijenhuis, H Haverkate, H Rosing, J H M Schellens, J H Beijnen. Simultaneous quantification of dabrafenib and trametinib in human plasma using high-performance liquid chromatography-tandem mass spectrometry.
Journal of pharmaceutical and biomedical analysis.
2016 Jun; 125(?):270-9. doi:
10.1016/j.jpba.2016.03.049. [PMID: 27058232] - Max Schreuer, Geert Meersseman, Sari Van Den Herrewegen, Yanina Jansen, Ines Chevolet, Ambre Bott, Sofie Wilgenhof, Teofila Seremet, Bart Jacobs, Ronald Buyl, Geert Maertens, Bart Neyns. Quantitative assessment of BRAF V600 mutant circulating cell-free tumor DNA as a tool for therapeutic monitoring in metastatic melanoma patients treated with BRAF/MEK inhibitors.
Journal of translational medicine.
2016 Apr; 14(?):95. doi:
10.1186/s12967-016-0852-6. [PMID: 27095081] - Daniele Ouellet, Nastya Kassir, Joannellyn Chiu, Mohamad-Samer Mouksassi, Cathrine Leonowens, Donna Cox, Douglas J DeMarini, Olivia Gardner, Wendy Crist, Kiran Patel. Population pharmacokinetics and exposure-response of trametinib, a MEK inhibitor, in patients with BRAF V600 mutation-positive melanoma.
Cancer chemotherapy and pharmacology.
2016 Apr; 77(4):807-17. doi:
10.1007/s00280-016-2993-y. [PMID: 26940938] - Victoria L Bridgeman, Elaine Wan, Shane Foo, Mark R Nathan, Jonathan C Welti, Sophia Frentzas, Peter B Vermeulen, Natasha Preece, Caroline J Springer, Thomas Powles, Paul D Nathan, James Larkin, Martin Gore, Naveen S Vasudev, Andrew R Reynolds. Preclinical Evidence That Trametinib Enhances the Response to Antiangiogenic Tyrosine Kinase Inhibitors in Renal Cell Carcinoma.
Molecular cancer therapeutics.
2016 Jan; 15(1):172-83. doi:
10.1158/1535-7163.mct-15-0170. [PMID: 26487278] - 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:
10.1097/cmr.0000000000000186. [PMID: 26512791] - Alexander M Menzies, James S Wilmott, Martin Drummond, Serigne Lo, Megan Lyle, Matthew M K Chan, John F Thompson, Alex Guminski, Matteo S Carlino, Richard A Scolyer, Richard F Kefford, Georgina V Long. Clinicopathologic features associated with efficacy and long-term survival in metastatic melanoma patients treated with BRAF or combined BRAF and MEK inhibitors.
Cancer.
2015 Nov; 121(21):3826-35. doi:
10.1002/cncr.29586. [PMID: 26218930] - Tessa Gargett, Cara K Fraser, Gianpietro Dotti, Eric S Yvon, Michael P Brown. BRAF and MEK inhibition variably affect GD2-specific chimeric antigen receptor (CAR) T-cell function in vitro.
Journal of immunotherapy (Hagerstown, Md. : 1997).
2015 Jan; 38(1):12-23. doi:
10.1097/cji.0000000000000061. [PMID: 25415284] - Joao A Paulo, Fiona E McAllister, Robert A Everley, Sean A Beausoleil, Alexander S Banks, Steven P Gygi. Effects of MEK inhibitors GSK1120212 and PD0325901 in vivo using 10-plex quantitative proteomics and phosphoproteomics.
Proteomics.
2015 Jan; 15(2-3):462-73. doi:
10.1002/pmic.201400154. [PMID: 25195567] - Le Min Lee, Lynn Feun, Yaohong Tan. A case of intracranial hemorrhage caused by combined dabrafenib and trametinib therapy for metastatic melanoma.
The American journal of case reports.
2014 Oct; 15(?):441-3. doi:
10.12659/ajcr.890875. [PMID: 25305754] - Shruthi Vaidhyanathan, Rajendar K Mittapalli, Jann N Sarkaria, William F Elmquist. Factors influencing the CNS distribution of a novel MEK-1/2 inhibitor: implications for combination therapy for melanoma brain metastases.
Drug metabolism and disposition: the biological fate of chemicals.
2014 Aug; 42(8):1292-300. doi:
10.1124/dmd.114.058339. [PMID: 24875464] - May Y K Ho, Michael J Morris, Jill L Pirhalla, John W Bauman, Carolyn B Pendry, Keith W Orford, Royce A Morrison, Donna S Cox. Trametinib, a first-in-class oral MEK inhibitor mass balance study with limited enrollment of two male subjects with advanced cancers.
Xenobiotica; the fate of foreign compounds in biological systems.
2014 Apr; 44(4):352-68. doi:
10.3109/00498254.2013.831143. [PMID: 23971497] - Jeffrey R Infante, Leslie A Fecher, Gerald S Falchook, Sujatha Nallapareddy, Michael S Gordon, Carlos Becerra, Douglas J DeMarini, Donna S Cox, Yanmei Xu, Shannon R Morris, Vijay G R Peddareddigari, Ngocdiep T Le, Lowell Hart, Johanna C Bendell, Gail Eckhardt, Razelle Kurzrock, Keith Flaherty, Howard A Burris, Wells A Messersmith. Safety, pharmacokinetic, pharmacodynamic, and efficacy data for the oral MEK inhibitor trametinib: a phase 1 dose-escalation trial.
The Lancet. Oncology.
2012 Aug; 13(8):773-81. doi:
10.1016/s1470-2045(12)70270-x. [PMID: 22805291]
