Cobimetinib (BioDeep_00000697915)
代谢物信息卡片
Cobimetinib
化学式: C21H21F3IN3O2 (531.0630552)
中文名称: 考比替尼
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: C1CCNC(C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O
InChI: InChI=1S/C21H21F3IN3O2/c22-14-6-5-13(19(18(14)24)27-16-7-4-12(25)9-15(16)23)20(29)28-10-21(30,11-28)17-3-1-2-8-26-17/h4-7,9,17,26-27,30H,1-3,8,10-11H2/t17-/m0/s1
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
C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor
同义名列表
1 个代谢物同义名
数据库引用编号
6 个数据库交叉引用编号
- ChEBI: CHEBI:90851
- KEGGdrug: D10405
- PubChem: 16222096
- DrugBank: DB05239
- ChEMBL: CHEMBL2146883
- CAS: 934660-93-2
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。
文献列表
- 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] - Gabriela Alejandra Sosa, Patricia Dogliani, Andrés Emilio Guidi, Marco Antonio Marangoni, Marcelo Lavarda, Patricia Fainstein-Day. [Erdheim-Chester disease: a rare histiocytosis with outstanding response to cobimetinib.].
Revista de la Facultad de Ciencias Medicas (Cordoba, Argentina).
2021 12; 78(4):398-401. doi:
10.31053/1853.0605.v78.n4.30852. [PMID: 34962740] - 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] - Lichen Zhang, Deqiong Xie, Yonghua Lei, Aoli Na, Lei Zhu. Preclinical activity of cobimetinib alone or in combination with chemotherapy and targeted therapies in renal cell carcinoma.
Future oncology (London, England).
2021 Aug; 17(23):3051-3060. doi:
10.2217/fon-2021-0256. [PMID: 33906367] - Malcolm P Huestis, Darlene Dela Cruz, Antonio G DiPasquale, Matthew R Durk, Charles Eigenbrot, Paul Gibbons, Alberto Gobbi, Thomas L Hunsaker, Hank La, Dennis H Leung, Wendy Liu, Shiva Malek, Mark Merchant, John G Moffat, Christine S Muli, Christine J Orr, Brendan T Parr, Frances Shanahan, Christopher J Sneeringer, Weiru Wang, Ivana Yen, Jianping Yin, Michael Siu, Joachim Rudolph. Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor.
Journal of medicinal chemistry.
2021 04; 64(7):3940-3955. doi:
10.1021/acs.jmedchem.0c02085. [PMID: 33780623] - Qianqian Fan, Jie Ma, Bo Zhang, Qiuyue Li, Fang Liu, Bin Zhao. Assessment of acute kidney injury related to small-molecule protein kinase inhibitors using the FDA adverse event reporting system.
Cancer chemotherapy and pharmacology.
2020 11; 86(5):655-662. doi:
10.1007/s00280-020-04151-8. [PMID: 33001273] - 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] - 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] - 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] - 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] - Ryan H Takahashi, Shuguang Ma, Qin Yue, Heasook Kim-Kang, Yijun Yi, Justin Ly, Jason W Boggs, Alec Fettes, Andrew McClory, Yuzhong Deng, Cornelis E C A Hop, S Cyrus Khojasteh, Edna F Choo. Absorption, metabolism and excretion of cobimetinib, an oral MEK inhibitor, in rats and dogs.
Xenobiotica; the fate of foreign compounds in biological systems.
2017 Jan; 47(1):50-65. doi:
10.3109/00498254.2016.1157645. [PMID: 27055783] - Nageshwar R Budha, Tao Ji, Luna Musib, Steve Eppler, Mark Dresser, Yuan Chen, Jin Y Jin. Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Clinical pharmacokinetics.
2016 11; 55(11):1435-1445. doi:
10.1007/s40262-016-0412-5. [PMID: 27225997] - Lee S Rosen, Patricia LoRusso, Wen Wee Ma, Jonathan W Goldman, Amy Weise, A Dimitrios Colevas, Alex Adjei, Salim Yazji, Angela Shen, Stuart Johnston, Hsin-Ju Hsieh, Iris T Chan, Branimir I Sikic. A first-in-human phase I study to evaluate the MEK1/2 inhibitor, cobimetinib, administered daily in patients with advanced solid tumors.
Investigational new drugs.
2016 10; 34(5):604-13. doi:
10.1007/s10637-016-0374-3. [PMID: 27424159] - Ryan H Takahashi, Edna F Choo, Shuguang Ma, Susan Wong, Jason Halladay, Yuzhong Deng, Isabelle Rooney, Mary Gates, Cornelis E C A Hop, S Cyrus Khojasteh, Mark J Dresser, Luna Musib. Absorption, Metabolism, Excretion, and the Contribution of Intestinal Metabolism to the Oral Disposition of [14C]Cobimetinib, a MEK Inhibitor, in Humans.
Drug metabolism and disposition: the biological fate of chemicals.
2016 Jan; 44(1):28-39. doi:
10.1124/dmd.115.066282. [PMID: 26451002] - Kelong Han, Jin Y Jin, Mathilde Marchand, Stephen Eppler, Nicholas Choong, Stephen P Hack, Nalin Tikoo, Rene Bruno, Mark Dresser, Luna Musib, Nageshwar R Budha. Population pharmacokinetics and dosing implications for cobimetinib in patients with solid tumors.
Cancer chemotherapy and pharmacology.
2015 Nov; 76(5):917-24. doi:
10.1007/s00280-015-2862-0. [PMID: 26365290] - Yuzhong Deng, Luna Musib, Edna Choo, Matthew Chapple, Sarah Burke, James Johnson, Steve Eppler, Brian Dean. Determination of cobimetinib in human plasma using protein precipitation extraction and high-performance liquid chromatography coupled to mass spectrometry.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2014 Dec; 972(?):117-23. doi:
10.1016/j.jchromb.2014.09.034. [PMID: 25444546] - Edna F Choo, Justin Ly, Jocelyn Chan, Sheerin K Shahidi-Latham, Kirsten Messick, Emile Plise, Cristine M Quiason, Lulu Yang. Role of P-glycoprotein on the brain penetration and brain pharmacodynamic activity of the MEK inhibitor cobimetinib.
Molecular pharmaceutics.
2014 Nov; 11(11):4199-207. doi:
10.1021/mp500435s. [PMID: 25243894] - Omar Abdel-Wahab, Virginia M Klimek, Alisa A Gaskell, Agnes Viale, Donavan Cheng, Eunhee Kim, Raajit Rampal, Mark Bluth, James J Harding, Margaret K Callahan, Taha Merghoub, Michael F Berger, David B Solit, Neal Rosen, Ross L Levine, Paul B Chapman. Efficacy of intermittent combined RAF and MEK inhibition in a patient with concurrent BRAF- and NRAS-mutant malignancies.
Cancer discovery.
2014 May; 4(5):538-45. doi:
10.1158/2159-8290.cd-13-1038. [PMID: 24589925] - Edna F Choo, Chee M Ng, Leanne Berry, Marcia Belvin, Nicholas Lewin-Koh, Mark Merchant, Laurent Salphati. PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts.
Cancer chemotherapy and pharmacology.
2013 Jan; 71(1):133-43. doi:
10.1007/s00280-012-1988-6. [PMID: 23053270] - Harvey Wong, Laurent Vernillet, Amy Peterson, Joseph A Ware, Lillian Lee, Jean-Francois Martini, Peiwen Yu, Congfen Li, Geoffrey Del Rosario, Edna F Choo, Klaus P Hoeflich, Yongchang Shi, Blake T Aftab, Ron Aoyama, Sanh Tan Lam, Marcia Belvin, John Prescott. Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2012 Jun; 18(11):3090-9. doi:
10.1158/1078-0432.ccr-12-0445. [PMID: 22496205] - Edna F Choo, Marcia Belvin, Jason Boggs, Yuzhong Deng, Klaus P Hoeflich, Justin Ly, Mark Merchant, Christine Orr, Emile Plise, Kirk Robarge, Jean F Martini, Robert Kassees, Ron G Aoyama, Atulkumar Ramaiya, Stuart H Johnston. Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions.
Drug metabolism and disposition: the biological fate of chemicals.
2012 May; 40(5):919-27. doi:
10.1124/dmd.111.043778. [PMID: 22315332] - L V Burenkova. [Specific activity of immune agglutinating antibodies of the ABO system in the paper-dried blood serum].
Zdravookhranenie Kirgizii.
1976 Jan; ?(1):38-42. doi:
NULL. [PMID: 7071]