Pexidartinib (BioDeep_00000182288)
human metabolite blood metabolite
代谢物信息卡片
5-({5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl}methyl)-N-{[6-(trifluoromethyl)pyridin-3-yl]methyl}pyridin-2-amine
化学式: C20H15ClF3N5 (417.09680160000005)
中文名称: 吡昔替尼
谱图信息:
最多检出来源 Homo sapiens(blood) 50%
分子结构信息
SMILES: C1=CC(=NC=C1CC2=CNC3=C2C=C(C=N3)Cl)NCC4=CN=C(C=C4)C(F)(F)F
InChI: InChI=1S/C20H15ClF3N5/c21-15-6-16-14(10-28-19(16)29-11-15)5-12-2-4-18(26-7-12)27-9-13-1-3-17(25-8-13)20(22,23)24/h1-4,6-8,10-11H,5,9H2,(H,26,27)(H,28,29)
描述信息
C274 - Antineoplastic Agent > C2189 - Signal Transduction Inhibitor > C129824 - Antineoplastic Protein Inhibitor
L - Antineoplastic and immunomodulating agents > L01 - Antineoplastic agents > L01E - Protein kinase inhibitors
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
8 个数据库交叉引用编号
- ChEBI: CHEBI:145373
- PubChem: 25151352
- HMDB: HMDB0256360
- DrugBank: DB12978
- ChEMBL: CHEMBL3813873
- Wikipedia: Pexidartinib
- chemspider: 35308322
- CAS: 1029044-16-3
分类词条
相关代谢途径
Reactome(4)
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
- T J Xiao, J Zhang, J B Kang, L Li, J F Zhan, Y Wei, A Tian. [Regulation of colony-stimulating factor 1 receptor inhibitor pexidartinib on the senescence of mouse bone marrow-derived macrophages stimulated by lipopolysaccharide].
Zhonghua kou qiang yi xue za zhi = Zhonghua kouqiang yixue zazhi = Chinese journal of stomatology.
2023 Jun; 58(6):575-583. doi:
10.3760/cma.j.cn112144-20230326-00116. [PMID: 37272003] - Yang Zhou, Shuang Xiang, Fang Yang, Xiaoyun Lu. Targeting Gatekeeper Mutations for Kinase Drug Discovery.
Journal of medicinal chemistry.
2022 12; 65(23):15540-15558. doi:
10.1021/acs.jmedchem.2c01361. [PMID: 36395392] - Hamim Zahir, Jonathan Greenberg, Ching Hsu, Thomas C Marbury, Kenneth C Lasseter, Li-An Xu, William D Tap, John H Healey, Silvia Stacchiotti, Frank LaCreta. Effect of Mild and Moderate Hepatic Impairment (Defined by Child-Pugh Classification and National Cancer Institute Organ Dysfunction Working Group Criteria) on Pexidartinib Pharmacokinetics.
Journal of clinical pharmacology.
2022 Aug; 62(8):992-1005. doi:
10.1002/jcph.2042. [PMID: 35247274] - Essam Ezzeldin, Muzaffar Iqbal, Yousif A Asiri, Gamal A E Mostafa, Ahmed Y A Sayed. Eco-Friendly, Simple, Fast, and Sensitive UPLC-MS/MS Method for Determination of Pexidartinib in Plasma and Its Application to Metabolic Stability.
Molecules (Basel, Switzerland).
2022 Jan; 27(1):. doi:
10.3390/molecules27010297. [PMID: 35011540] - Jens Martens-Lobenhoffer, Stylianos Tomaras, Eugen Feist, Stefanie M Bode-Böger. Quantification of the janus kinase 1 inhibitor upadacitinib in human plasma by LC-MS/MS.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2022 Jan; 1188(?):123076. doi:
10.1016/j.jchromb.2021.123076. [PMID: 34871917] - Shulan Qiu, Juan Pablo Palavicini, Jianing Wang, Nancy S Gonzalez, Sijia He, Elizabeth Dustin, Cheng Zou, Lin Ding, Anindita Bhattacharjee, Candice E Van Skike, Veronica Galvan, Jeffrey L Dupree, Xianlin Han. Adult-onset CNS myelin sulfatide deficiency is sufficient to cause Alzheimer's disease-like neuroinflammation and cognitive impairment.
Molecular neurodegeneration.
2021 09; 16(1):64. doi:
10.1186/s13024-021-00488-7. [PMID: 34526055] - Ophelia Yin, Andrew J Wagner, Jia Kang, William Knebel, Hamim Zahir, Michiel van de Sande, William D Tap, Hans Gelderblom, John H Healey, Dale Shuster, Silvia Stacchiotti. Population Pharmacokinetic Analysis of Pexidartinib in Healthy Subjects and Patients With Tenosynovial Giant Cell Tumor or Other Solid Tumors.
Journal of clinical pharmacology.
2021 04; 61(4):480-492. doi:
10.1002/jcph.1753. [PMID: 33043474] - Hamim Zahir, Fumiaki Kobayashi, Cynthia Zamora, Roohi Gajee, Michael S Gordon, Hani M Babiker, Qiang Wang, Jonathan Greenberg, Andrew J Wagner. Evaluation of Potential Drug-Drug Interaction Risk of Pexidartinib With Substrates of Cytochrome P450 and P-Glycoprotein.
Journal of clinical pharmacology.
2021 03; 61(3):298-306. doi:
10.1002/jcph.1734. [PMID: 32918831] - Dongdong Zhang, Sheng Li, Liyan Hou, Lu Jing, Zhengzheng Ruan, Bingjie Peng, Xiaomeng Zhang, Jau-Shyong Hong, Jie Zhao, Qingshan Wang. Microglial activation contributes to cognitive impairments in rotenone-induced mouse Parkinson's disease model.
Journal of neuroinflammation.
2021 Jan; 18(1):4. doi:
10.1186/s12974-020-02065-z. [PMID: 33402167] - Lauren H Boal, John Glod, Melissa Spencer, Miki Kasai, Joanne Derdak, Eva Dombi, Mark Ahlman, Daniel W Beury, Melinda S Merchant, Christianne Persenaire, David J Liewehr, Seth M Steinberg, Brigitte C Widemann, Rosandra N Kaplan. Pediatric PK/PD Phase I Trial of Pexidartinib in Relapsed and Refractory Leukemias and Solid Tumors Including Neurofibromatosis Type I-Related Plexiform Neurofibromas.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2020 12; 26(23):6112-6121. doi:
10.1158/1078-0432.ccr-20-1696. [PMID: 32943455] - Lu Shi, Zheli Jiang, Bowen Zhang, Congrong Tang, Ren-Ai Xu. Development of UPLC-MS/MS method for studying the pharmacokinetic interactions of pexidartinib with antifungal drugs in rats.
Journal of pharmaceutical and biomedical analysis.
2020 Sep; 188(?):113386. doi:
10.1016/j.jpba.2020.113386. [PMID: 32502954] - Priya S Shankarappa, Cody J Peer, Arman Odabas, Cynthia L McCully, Rafael C Garcia, William D Figg, Katherine E Warren. Cerebrospinal fluid penetration of the colony-stimulating factor-1 receptor (CSF-1R) inhibitor, pexidartinib.
Cancer chemotherapy and pharmacology.
2020 05; 85(5):1003-1007. doi:
10.1007/s00280-020-04071-7. [PMID: 32306101] - Catherine C Smith, Mark J Levis, Olga Frankfurt, John M Pagel, Gail J Roboz, Richard M Stone, Eunice S Wang, Paul L Severson, Brian L West, Mai H Le, Sabine Kayser, Bao Lam, Henry H Hsu, Chao Zhang, Gideon Bollag, Alexander E Perl. A phase 1/2 study of the oral FLT3 inhibitor pexidartinib in relapsed/refractory FLT3-ITD-mutant acute myeloid leukemia.
Blood advances.
2020 04; 4(8):1711-1721. doi:
10.1182/bloodadvances.2020001449. [PMID: 32330242] - Jih-Hsiang Lee, Tom Wei-Wu Chen, Chih-Hung Hsu, Yu-Hsin Yen, James Chih-Hsin Yang, Ann-Lii Cheng, Shun-Ichi Sasaki, LiYin Lillian Chiu, Masahiro Sugihara, Tomoko Ishizuka, Toshihiro Oguma, Naoyuki Tajima, Chia-Chi Lin. A phase I study of pexidartinib, a colony-stimulating factor 1 receptor inhibitor, in Asian patients with advanced solid tumors.
Investigational new drugs.
2020 02; 38(1):99-110. doi:
10.1007/s10637-019-00745-z. [PMID: 30825104] - Qiuju Xun, Zhang Zhang, Jinfeng Luo, Linjiang Tong, Minhao Huang, Zhen Wang, Jian Zou, Yingqiang Liu, Yong Xu, Hua Xie, Zheng-Chao Tu, Xiaoyun Lu, Ke Ding. Design, Synthesis, and Structure-Activity Relationship Study of 2-Oxo-3,4-dihydropyrimido[4,5- d]pyrimidines as New Colony Stimulating Factor 1 Receptor (CSF1R) Kinase Inhibitors.
Journal of medicinal chemistry.
2018 03; 61(6):2353-2371. doi:
10.1021/acs.jmedchem.7b01612. [PMID: 29499108] - Justyna Sosna, Stephan Philipp, Ricardo Albay, Jorge Mauricio Reyes-Ruiz, David Baglietto-Vargas, Frank M LaFerla, Charles G Glabe. Early long-term administration of the CSF1R inhibitor PLX3397 ablates microglia and reduces accumulation of intraneuronal amyloid, neuritic plaque deposition and pre-fibrillar oligomers in 5XFAD mouse model of Alzheimer's disease.
Molecular neurodegeneration.
2018 03; 13(1):11. doi:
10.1186/s13024-018-0244-x. [PMID: 29490706] - Nicholas Butowski, Howard Colman, John F De Groot, Antonio M Omuro, Lakshmi Nayak, Patrick Y Wen, Timothy F Cloughesy, Adhirai Marimuthu, Sam Haidar, Arie Perry, Jason Huse, Joanna Phillips, Brian L West, Keith B Nolop, Henry H Hsu, Keith L Ligon, Annette M Molinaro, Michael Prados. Orally administered colony stimulating factor 1 receptor inhibitor PLX3397 in recurrent glioblastoma: an Ivy Foundation Early Phase Clinical Trials Consortium phase II study.
Neuro-oncology.
2016 Apr; 18(4):557-64. doi:
10.1093/neuonc/nov245. [PMID: 26449250]