afatinib (BioDeep_00000683535)
代谢物信息卡片
afatinib
化学式: C24H25ClFN5O3 (485.163)
中文名称: 阿法蒂尼(BIBW2992), 阿法替尼
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CN(C)CC=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OC4CCOC4
InChI: InChI=1S/C24H25ClFN5O3/c1-31(2)8-3-4-23(32)30-21-11-17-20(12-22(21)34-16-7-9-33-13-16)27-14-28-24(17)29-15-5-6-19(26)18(25)10-15/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29)/b4-3+/t16-/m0/s1
描述信息
L - Antineoplastic and immunomodulating agents > L01 - Antineoplastic agents > L01E - Protein kinase inhibitors > L01EB - Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors
C274 - Antineoplastic Agent > C2189 - Signal Transduction Inhibitor > C129824 - Antineoplastic Protein Inhibitor
C274 - Antineoplastic Agent > C163758 - Targeted Therapy Agent > C163952 - EGFR-targeting Agent
C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor > C1967 - Tyrosine Kinase Inhibitor
C471 - Enzyme Inhibitor > C129825 - Antineoplastic Enzyme Inhibitor
D004791 - Enzyme Inhibitors > D047428 - Protein Kinase Inhibitors
D000970 - Antineoplastic Agents
(E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells[1].
Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer[1][2][3][4].
同义名列表
4 个代谢物同义名
数据库引用编号
11 个数据库交叉引用编号
- ChEBI: CHEBI:61390
- ChEBI: CHEBI:94698
- KEGGdrug: D09724
- PubChem: 10184653
- DrugBank: DB08916
- ChEMBL: CHEMBL1173655
- MeSH: Afatinib
- CAS: 850140-72-6
- CAS: 439081-18-2
- medchemexpress: HY-10261B
- medchemexpress: HY-10261
分类词条
相关代谢途径
Reactome(4)
BioCyc(0)
PlantCyc(0)
代谢反应
3 个相关的代谢反应过程信息。
Reactome(3)
- Disease:
ADORA2B + Ade-Rib ⟶ ADORA2B:Ade-Rib - Diseases of signal transduction by growth factor receptors and second messengers:
H+ + Oxygen + TPNH ⟶ H2O2 + TPN - Signaling by ERBB2 in Cancer:
ERBB2 KD mutants (TKI sensitive):ERBIN:HSP90:CDC37 ⟶ ERBB2 KD mutants:TKIs:ERBIN:HSP90:CDC37
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
- Wen-Chien Cheng, Chi-Chien Lin, Wei-Chih Liao, Yu-Chao Lin, Chia-Hung Chen, Hung-Jen Chen, Chih-Yen Tu, Te-Chun Hsia. The difference between dacomitinib and afatinib in effectiveness and safety in first-line treatment of patients with advanced EGFR-mutant non-small cell lung cancer: a real-world observational study.
BMC cancer.
2024 Feb; 24(1):228. doi:
10.1186/s12885-024-11956-w. [PMID: 38373960] - Gang Wei, Yan Wang, Ping Yang, Shujia Peng, Sensen Duan, Xi'e Hu, Lijuan Yuan, Guoqiang Bao. Enhancing vulnerability of Afatinib using Erastin via xCT-mediated ROS/P38MAPK signaling feedback loop in gastric cancer cells.
Gene.
2023 May; 873(?):147468. doi:
10.1016/j.gene.2023.147468. [PMID: 37169154] - Jiaqian Xu, Lijie Peng, Cuiping Guo, Fang Xu, Dong-Shi Lin, Yi Tang, Zhengqiu Li. Comparison of Different Competitive Proteome Profiling Approaches in Target Identification of Covalent Inhibitors.
Chembiochem : a European journal of chemical biology.
2022 12; 23(24):e202200389. doi:
10.1002/cbic.202200389. [PMID: 36271784] - Pratibha Pandey, Fahad Khan, Prashant Chauhan, Tarun Kumar Upadhyay, Fevzi Bardakci, Md Jahoor Alam, Nujud Almuzaini, Rania Abdeen Hussain Abdalla, Sujeet Kumar Singh, Mohd Saeed. Elucidation of the inhibitory potential of flavonoids against PKP1 protein in non-small cell lung cancer.
Cellular and molecular biology (Noisy-le-Grand, France).
2022 Nov; 68(11):90-96. doi:
10.14715/cmb/2022.68.11.15. [PMID: 37114302] - Jisheng Li, Liping Zhu, Justin Stebbing, Ling Peng. Afatinib treatment in a lung adenocarcinoma patient harboring a rare EGFR L747P mutation.
Journal of cancer research and therapeutics.
2022 Sep; 18(5):1436-1439. doi:
10.4103/jcrt.jcrt_433_22. [PMID: 36204894] - Clément Carbasse, Fanny Leenhardt, William Jacot, Caroline Perrier, Frederic Pinguet, Marie Viala. Oral targeted therapy dose adaptation in older patients with cancer: A real-life French cohort.
British journal of clinical pharmacology.
2022 07; 88(7):3370-3377. doi:
10.1111/bcp.15285. [PMID: 35178745] - Emi Ishikawa, Yuta Yokoyama, Haruna Chishima, Ouki Kuniyoshi, Itaru Sato, Naoki Nakaya, Hideo Nakajima, Motonori Kimura, Jun Hakamata, Naoya Suehiro, Hideo Nakada, Shinnosuke Ikemura, Aya Jibiki, Hitoshi Kawazoe, Hiroshi Muramatsu, Sayo Suzuki, Tomonori Nakamura. Development and validation of a new liquid chromatography-tandem mass spectrometry assay for the simultaneous quantification of afatinib, dacomitinib, osimertinib, and the active metabolites of osimertinib in human serum.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2022 May; 1199(?):123245. doi:
10.1016/j.jchromb.2022.123245. [PMID: 35436724] - Jun Zhao, Hua Bai, Xin Wang, Yuyan Wang, Jianchun Duan, Hanxiao Chen, Zhiyi Xue, Yahui Tian, Agnieszka Cseh, Dennis Chin-Lun Huang, Yi-Long Wu, Jie Wang. Biomarker subset analysis of a phase IIIb, open-label study of afatinib in EGFR tyrosine kinase inhibitor-naive patients with EGFRm+ non-small-cell lung cancer.
Future oncology (London, England).
2022 Apr; 18(12):1485-1497. doi:
10.2217/fon-2021-0394. [PMID: 35114807] - Xin Xiong, Yuanyuan Zhang, Ziyu Wang, Congya Zhou, Ping Yang, Xin Du, Li Yang, Wei Liu. Simultaneous quantitative detection of afatinib, erlotinib, gefitinib, icotinib, osimertinib and their metabolites in plasma samples of patients with non-small cell lung cancer using liquid chromatography-tandem mass spectrometry.
Clinica chimica acta; international journal of clinical chemistry.
2022 Feb; 527(?):1-10. doi:
10.1016/j.cca.2021.12.028. [PMID: 34999058] - D Rodríguez-Abreu, M Cobo, S García-Román, S Viteri-Ramírez, N Jordana-Ariza, B García-Peláez, N Reguart, A Aguilar, J Codony-Servat, A Drozdowskyj, M A Molina-Vila, E d'Hondt, R Rosell. The EPICAL trial, a phase Ib study combining first line afatinib with anti-EGF vaccination in EGFR-mutant metastatic NSCLC.
Lung cancer (Amsterdam, Netherlands).
2022 02; 164(?):8-13. doi:
10.1016/j.lungcan.2021.12.014. [PMID: 34971901] - Wei Cao, Jun Ma, Xuan Jiang, Guangyi Gao. Afatinib Targeted Therapy Affects the Immune Function and Serum Levels of EGFR and Gastrin-Releasing Peptide Precursor (pro-GRP) in Patients with Non-Small-Cell Lung Cancer (NSCLC).
Disease markers.
2022; 2022(?):2869531. doi:
10.1155/2022/2869531. [PMID: 36157204] - Yanhong Wang, Keke Liang, Jing Shi, Cunxian Duan, Hui Li, Haisheng Chen. Determination of Afatinib in Human Plasma by 2-Dimensional Liquid Chromatography.
Pharmacology.
2022; 107(5-6):290-297. doi:
10.1159/000521181. [PMID: 35086096] - Xi Luo, Xiu Jin Zhang, Wen Ling Zhu, Jin Ling Yi, Wen Gang Xiong, Feng Ye, Chao Zheng, Ming Xia Fan. A Sensitive LC-MS/MS Method for the Determination of Afatinib in Human Plasma and Its Application to a Bioequivalence Study.
Journal of chromatographic science.
2022 Jan; 60(1):61-67. doi:
10.1093/chromsci/bmab040. [PMID: 33912896] - Hidenori Mizugaki, Satoshi Oizumi, Yuka Fujita, Toshiyuki Harada, Yoshiro Nakahara, Taichi Takashina, Ryo Ko, Kageaki Watanabe, Takamasa Hotta, Hiroyuki Minemura, Sho Saeki, Hajime Asahina, Keiichi Nakamura, Hiromi Nakamura, Fumie Hosoda, Shigehiro Yagishita, Akinobu Hamada. Pharmacokinetic and pharmacogenomic analysis of low-dose afatinib treatment in elderly patients with EGFR mutation-positive non-small cell lung cancer.
European journal of cancer (Oxford, England : 1990).
2022 01; 160(?):227-234. doi:
10.1016/j.ejca.2021.10.024. [PMID: 34862083] - Chia-Ling Li, Te-Chun Hsia, Su-Tso Yang, Kun-San Clifford Chao, Chih-Yen Tu, Hung-Jen Chen, Chia-Hsiang Li. Efficacy of Prophylactic Traditional Chinese Medicine on Skin Toxicity of Afatinib in EGFR Mutation-Positive Advanced Lung Adenocarcinoma: A Single-Center, Prospective, Double-Blinded, Randomized-Controlled Pilot Trial.
Integrative cancer therapies.
2022 Jan; 21(?):15347354221086663. doi:
10.1177/15347354221086663. [PMID: 35297709] - Zhiwei Tang, XiuHai Ji, Guanghui Zhou, Ruhua Chen, Yan Fen, Hui Ding. Hypotension from afatinib in epidermal growth factor receptor-mutated non-small cell lung cancer: a case report and literature review.
Anti-cancer drugs.
2022 01; 33(1):e840-e841. doi:
10.1097/cad.0000000000001244. [PMID: 34486535] - Yuji Mukai, Azusa Wakamoto, Tae Hatsuyama, Tatsunari Yoshida, Hideki Sato, Akihisa Fujita, Nobuo Inotsume, Takaki Toda. An Liquid Chromatography-Tandem Mass Spectrometry Method for the Simultaneous Determination of Afatinib, Alectinib, Ceritinib, Crizotinib, Dacomitinib, Erlotinib, Gefitinib, and Osimertinib in Human Serum.
Therapeutic drug monitoring.
2021 12; 43(6):772-779. doi:
10.1097/ftd.0000000000000895. [PMID: 33871406] - Fanjie Qu, Shuang Wu, Huacheng Dong, Xin Yan. An elderly advanced non-small cell lung cancer patient harboring rare epidermal growth factor receptor mutations L861R benefited from afatinib: A case report.
Medicine.
2021 Nov; 100(45):e27614. doi:
10.1097/md.0000000000027614. [PMID: 34766562] - Rintaro Noro, Satoshi Igawa, Akihiro Bessho, Takashi Hirose, Tsuneo Shimokawa, Masanao Nakashima, Koichi Minato, Nobuhiko Seki, Takaaki Tokito, Toshiyuki Harada, Shinji Sasada, Shingo Miyamoto, Yosuke Tanaka, Naoki Furuya, Takayuki Kaburagi, Hideki Hayashi, Hirotoshi Iihara, Hiroaki Okamoto, Kaoru Kubota. A prospective, phase II trial of monotherapy with low-dose afatinib for patients with EGFR, mutation-positive, non-small cell lung cancer: Thoracic oncology research group 1632.
Lung cancer (Amsterdam, Netherlands).
2021 11; 161(?):49-54. doi:
10.1016/j.lungcan.2021.08.007. [PMID: 34536731] - Julie C L Fournier, John P Evans, Francesca Zappacosta, Daniel A Thomas, Vipulkumar K Patel, Gemma V White, Sebastien Campos, Nicholas C O Tomkinson. Acetylation of the Catalytic Lysine Inhibits Kinase Activity in PI3Kδ.
ACS chemical biology.
2021 09; 16(9):1644-1653. doi:
10.1021/acschembio.1c00225. [PMID: 34397208] - Yumi Harada, Hitomi Sekine, Kunitsugu Kubota, Daichi Sadatomi, Seiichi Iizuka, Naoki Fujitsuka. Calcium-activated chloride channel is involved in the onset of diarrhea triggered by EGFR tyrosine kinase inhibitor treatment in rats.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie.
2021 Sep; 141(?):111860. doi:
10.1016/j.biopha.2021.111860. [PMID: 34246954] - Alexis B Cortot, Anne Madroszyk, Etienne Giroux-Leprieur, Olivier Molinier, Elisabeth Quoix, Henri Bérard, Josiane Otto, Isabelle Rault, Denis Moro-Sibilot, Judith Raimbourg, Elodie Amour, Franck Morin, José Hureaux, Lionel Moreau, Didier Debieuvre, Hugues Morel, Aldo Renault, Eric Pichon, Benjamin Huret, Sandrine Charpentier, Marc G Denis, Jacques Cadranel. First-Line Afatinib plus Cetuximab for EGFR-Mutant Non-Small Cell Lung Cancer: Results from the Randomized Phase II IFCT-1503 ACE-Lung Study.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2021 08; 27(15):4168-4176. doi:
10.1158/1078-0432.ccr-20-4604. [PMID: 34031056] - Alessandro Leonetti, Mjriam Capula, Roberta Minari, Giulia Mazzaschi, Alessandro Gregori, Btissame El Hassouni, Filippo Papini, Paola Bordi, Michela Verzè, Amir Avan, Marcello Tiseo, Elisa Giovannetti. Dynamic Evaluation of Circulating miRNA Profile in EGFR-Mutated NSCLC Patients Treated with EGFR-TKIs.
Cells.
2021 06; 10(6):. doi:
10.3390/cells10061520. [PMID: 34208765] - Dingding Gao, Nan Jin, Yixian Fu, Yueyue Zhu, Yujie Wang, Ting Wang, Yuehong Chen, Mingming Zhang, Qiang Xiao, Min Huang, Yingxia Li. Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors.
European journal of medicinal chemistry.
2021 Apr; 216(?):113333. doi:
10.1016/j.ejmech.2021.113333. [PMID: 33689932] - Seung Hyeun Lee, Cheol-Kyu Park, Sung Yong Lee, Chang-Min Choi. Treatment outcomes and safety of afatinib in advanced squamous cell lung cancer progressed after platinum-based doublet chemotherapy and immunotherapy (SPACE study).
Thoracic cancer.
2021 04; 12(8):1264-1268. doi:
10.1111/1759-7714.13880. [PMID: 33586312] - Yuko Oya, Tatsuya Yoshida, Kazuhiro Asada, Tetsuya Oguri, Naoki Inui, Sayako Morikawa, Kentaro Ito, Tomoki Kimura, Eiji Kunii, Takashi Matsui, Akihito Kubo, Tatsuo Kato, Takashi Abe, Takeshi Tsuda, Toyoaki Hida. Clinical utility of liquid biopsy for EGFR driver, T790M mutation and EGFR amplification in plasma in patients with acquired resistance to afatinib.
BMC cancer.
2021 Jan; 21(1):57. doi:
10.1186/s12885-020-07777-2. [PMID: 33435905] - Hidetoshi Hayashi, Yuichi Takiguchi, Hironobu Minami, Kohei Akiyoshi, Yoshihiko Segawa, Hiroki Ueda, Yasuo Iwamoto, Chihiro Kondoh, Koji Matsumoto, Shin Takahashi, Hisateru Yasui, Toshiyuki Sawa, Yusuke Onozawa, Yasutaka Chiba, Yosuke Togashi, Yoshihiko Fujita, Kazuko Sakai, Shuta Tomida, Kazuto Nishio, Kazuhiko Nakagawa. Site-Specific and Targeted Therapy Based on Molecular Profiling by Next-Generation Sequencing for Cancer of Unknown Primary Site: A Nonrandomized Phase 2 Clinical Trial.
JAMA oncology.
2020 Dec; 6(12):1931-1938. doi:
10.1001/jamaoncol.2020.4643. [PMID: 33057591] - Xiaoyun Lu, Jeff B Smaill, Ke Ding. Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.
Journal of medicinal chemistry.
2020 10; 63(19):10726-10741. doi:
10.1021/acs.jmedchem.0c00507. [PMID: 32432477] - Hui Jiang, Ningning Luo, Xing Zhang, Chao Song, Jianhua Zang. EGFR L861Q and CDK4 amplification responding to afatinib combined with palbociclib treatment in a patient with advanced lung squamous cell carcinoma.
Lung cancer (Amsterdam, Netherlands).
2020 07; 145(?):216-218. doi:
10.1016/j.lungcan.2020.04.001. [PMID: 32345450] - Marzia Del Re, Iacopo Petrini, Francesca Mazzoni, Simona Valleggi, Giulia Gianfilippo, Daniele Pozzessere, Antonio Chella, Stefania Crucitta, Eleonora Rofi, Giuliana Restante, Mario Miccoli, Marina Chiara Garassino, Romano Danesi. Incidence of T790M in Patients With NSCLC Progressed to Gefitinib, Erlotinib, and Afatinib: A Study on Circulating Cell-free DNA.
Clinical lung cancer.
2020 05; 21(3):232-237. doi:
10.1016/j.cllc.2019.10.003. [PMID: 31735523] - Nahomi Tokudome, Yasuhiro Koh, Hiroaki Akamatsu, Daichi Fujimoto, Isamu Okamoto, Kazuhiko Nakagawa, Toyoaki Hida, Fumio Imamura, Satoshi Morita, Nobuyuki Yamamoto. Differential significance of molecular subtypes which were classified into EGFR exon 19 deletion on the first line afatinib monotherapy.
BMC cancer.
2020 Feb; 20(1):103. doi:
10.1186/s12885-020-6593-1. [PMID: 32028909] - Yanan Tan, Kangna Cao, Guanghui Ren, Zhiying Qin, Di Zhao, Ning Li, Xijing Chen, Yufeng Xia, Yang Lu. Effects of the ABCB1 and ABCG2 polymorphisms on the pharmacokinetics of afatinib in healthy Chinese volunteers.
Xenobiotica; the fate of foreign compounds in biological systems.
2020 Feb; 50(2):237-243. doi:
10.1080/00498254.2019.1610585. [PMID: 31021303] - Hidenobu Ishii, Koichi Azuma, Kazuko Sakai, Yoshiko Naito, Norikazu Matsuo, Takaaki Tokito, Kazuhiko Yamada, Tomoaki Hoshino, Kazuto Nishio. Determination of Somatic Mutations and Tumor Mutation Burden in Plasma by CAPP-Seq during Afatinib Treatment in NSCLC Patients Resistance to Osimertinib.
Scientific reports.
2020 01; 10(1):691. doi:
10.1038/s41598-020-57624-4. [PMID: 31959859] - So-Jung Park, Hwi-Joong Kang, Hyung-Joon Jun, Seong-Hoon Shin, Hwa-Seung Yoo. Multi-center, randomized, double-blind, placebo-controlled, exploratory study to evaluate the efficacy and safety of HAD-B1 for dose-finding in EGFR positive and locally advanced or metastatic NSCLC subjects who need Afatinib therapy: Study protocol clinical trial (SPIRIT Compliant).
Medicine.
2020 Jan; 99(4):e18735. doi:
10.1097/md.0000000000018735. [PMID: 31977865] - Keiko Nakao, Shinji Kobuchi, Shuhei Marutani, Ayano Iwazaki, Akihiro Tamiya, Shunichi Isa, Kyoichi Okishio, Masaki Kanazu, Motohiro Tamiya, Tomonori Hirashima, Kimie Imai, Toshiyuki Sakaeda, Shinji Atagi. Population pharmacokinetics of afatinib and exposure-safety relationships in Japanese patients with EGFR mutation-positive non-small cell lung cancer.
Scientific reports.
2019 12; 9(1):18202. doi:
10.1038/s41598-019-54804-9. [PMID: 31796841] - Wen-Xue Sun, Hong-Wei Han, Min-Kai Yang, Zhong-Ling Wen, Yin-Song Wang, Jiang-Yan Fu, Yun-Ting Lu, Ming-Yue Wang, Jia-Xin Bao, Gui-Hua Lu, Jin-Liang Qi, Xiao-Ming Wang, Hong-Yan Lin, Yong-Hua Yang. Design, synthesis and biological evaluation of benzoylacrylic acid shikonin ester derivatives as irreversible dual inhibitors of tubulin and EGFR.
Bioorganic & medicinal chemistry.
2019 12; 27(23):115153. doi:
10.1016/j.bmc.2019.115153. [PMID: 31648877] - Jinli Wang, Gaoxing Su, Xiaoqin Yin, Jia Luo, Rongrong Gu, Shuang Wang, Jian Feng, Bohua Chen. Non-small cell lung cancer-targeted, redox-sensitive lipid-polymer hybrid nanoparticles for the delivery of a second-generation irreversible epidermal growth factor inhibitor-Afatinib: In vitro and in vivo evaluation.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie.
2019 Dec; 120(?):109493. doi:
10.1016/j.biopha.2019.109493. [PMID: 31586902] - Yao Yang, Zhengwei Huang, Jinyuan Li, Ziran Mo, Ying Huang, Cheng Ma, Wenhao Wang, Xin Pan, Chuanbin Wu. PLGA Porous Microspheres Dry Powders for Codelivery of Afatinib-Loaded Solid Lipid Nanoparticles and Paclitaxel: Novel Therapy for EGFR Tyrosine Kinase Inhibitors Resistant Nonsmall Cell Lung Cancer.
Advanced healthcare materials.
2019 12; 8(23):e1900965. doi:
10.1002/adhm.201900965. [PMID: 31664795] - Yutaro Yamamoto, Tetsuya Saita, Yuta Yamamoto, Rintaro Sogawa, Sakiko Kimura, Yutaka Narisawa, Shinya Kimura, Masashi Shin. Immunohistochemical localization of afatinib in male rat intestines and skin after its oral administration.
Acta histochemica.
2019 Nov; 121(8):151439. doi:
10.1016/j.acthis.2019.09.001. [PMID: 31500866] - Ibrahim A Darwish, Haitham AlRabiah, Mohammed A Hamidaddin. Development of two different formats of heterogeneous fluorescence immunoassay for bioanalysis of afatinib by employing fluorescence plate reader and KinExA 3200 immunosensor.
Scientific reports.
2019 10; 9(1):14742. doi:
10.1038/s41598-019-51288-5. [PMID: 31611565] - Ronilda R D'Cunha, Daryl J Murry, Guohua An. Nilotinib Alters the Efflux Transporter-Mediated Pharmacokinetics of Afatinib in Mice.
Journal of pharmaceutical sciences.
2019 10; 108(10):3434-3442. doi:
10.1016/j.xphs.2019.05.028. [PMID: 31163185] - J Gao, H-R Li, C Jin, J-H Jiang, J-Y Ding. Strategies to overcome acquired resistance to EGFR TKI in the treatment of non-small cell lung cancer.
Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico.
2019 Oct; 21(10):1287-1301. doi:
10.1007/s12094-019-02075-1. [PMID: 30864018] - Shu-Ting Hong, Huaching Lin, Chen-Shen Wang, Chih-Hsien Chang, Anya Maan-Yuh Lin, James Chih-Hsin Yang, Yu-Li Lo. Improving the anticancer effect of afatinib and microRNA by using lipid polymeric nanoparticles conjugated with dual pH-responsive and targeting peptides.
Journal of nanobiotechnology.
2019 Aug; 17(1):89. doi:
10.1186/s12951-019-0519-6. [PMID: 31426807] - Xinwen Wang, Fupeng Zhang, Xi Yang, Meiping Xue, Xiaoli Li, Yu Gao, Likun Liu. Secreted Phosphoprotein 1 (SPP1) Contributes to Second-Generation EGFR Tyrosine Kinase Inhibitor Resistance in Non-Small Cell Lung Cancer.
Oncology research.
2019 Aug; 27(8):871-877. doi:
10.3727/096504018x15426271404407. [PMID: 30832751] - Hideki Hayashi, Hirotoshi Iihara, Chiemi Hirose, Yoshihisa Fukuda, Mika Kitahora, Daizo Kaito, Komei Yanase, Junki Endo, Yasushi Ohno, Akio Suzuki, Tadashi Sugiyama. Effects of pharmacokinetics-related genetic polymorphisms on the side effect profile of afatinib in patients with non-small cell lung cancer.
Lung cancer (Amsterdam, Netherlands).
2019 08; 134(?):1-6. doi:
10.1016/j.lungcan.2019.05.013. [PMID: 31319966] - Manlio Barbarisi, Alfonso Barbarisi, Gabriele De Sena, Emilia Armenia, Caterina Aurilio, Michele Libutti, Rosario Vincenzo Iaffaioli, Gerardo Botti, Nicola Maurea, Vincenzo Quagliariello. Boswellic acid has anti-inflammatory effects and enhances the anticancer activities of Temozolomide and Afatinib, an irreversible ErbB family blocker, in human glioblastoma cells.
Phytotherapy research : PTR.
2019 06; 33(6):1670-1682. doi:
10.1002/ptr.6354. [PMID: 30924205] - Ashiq Masood, Rama Krishna Kancha, Janakiraman Subramanian. Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in non-small cell lung cancer harboring uncommon EGFR mutations: Focus on afatinib.
Seminars in oncology.
2019 06; 46(3):271-283. doi:
10.1053/j.seminoncol.2019.08.004. [PMID: 31558282] - Hiroaki Akamatsu, Yasuhiro Koh, Isamu Okamoto, Daichi Fujimoto, Akihiro Bessho, Koichi Azuma, Satoshi Morita, Nobuyuki Yamamoto, Kazuhiko Nakagawa. Clinical significance of monitoring EGFR mutation in plasma using multiplexed digital PCR in EGFR mutated patients treated with afatinib (West Japan Oncology Group 8114LTR study).
Lung cancer (Amsterdam, Netherlands).
2019 05; 131(?):128-133. doi:
10.1016/j.lungcan.2019.03.021. [PMID: 31027689] - G D Marijn Veerman, Mei H Lam, Ron H J Mathijssen, Stijn L W Koolen, Peter de Bruijn. Quantification of afatinib, alectinib, crizotinib and osimertinib in human plasma by liquid chromatography/triple-quadrupole mass spectrometry; focusing on the stability of osimertinib.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2019 Apr; 1113(?):37-44. doi:
10.1016/j.jchromb.2019.03.011. [PMID: 30889498] - Xiaoyan Lu, Sha Liu, Xiucheng Yang, Meishan Han, Kaoxiang Sun. Determination of tyrosine kinase inhibitor afatinib in rat plasma using LC-MS/MS and its application to in vivo pharmacokinetic studies of afatinib liposomes.
Journal of pharmaceutical and biomedical analysis.
2019 Feb; 164(?):181-186. doi:
10.1016/j.jpba.2018.10.043. [PMID: 30390560] - Francisco Sanchez-Vega, Jaclyn F Hechtman, Pau Castel, Geoffrey Y Ku, Yaelle Tuvy, Helen Won, Christopher J Fong, Nancy Bouvier, Gouri J Nanjangud, Joanne Soong, Efsevia Vakiani, Mark Schattner, David P Kelsen, Robert A Lefkowitz, Karen Brown, Mario E Lacouture, Marinela Capanu, Marissa Mattar, Besnik Qeriqi, Fabiola Cecchi, Yuan Tian, Todd Hembrough, Rebecca J Nagy, Richard B Lanman, Steven M Larson, Neeta Pandit-Taskar, Heiko Schöder, Christine A Iacobuzio-Donahue, David H Ilson, Wolfgang A Weber, Michael F Berger, Elisa de Stanchina, Barry S Taylor, Jason S Lewis, David B Solit, Jorge A Carrasquillo, Maurizio Scaltriti, Nikolaus Schultz, Yelena Y Janjigian. EGFR and MET Amplifications Determine Response to HER2 Inhibition in ERBB2-Amplified Esophagogastric Cancer.
Cancer discovery.
2019 02; 9(2):199-209. doi:
10.1158/2159-8290.cd-18-0598. [PMID: 30463996] - Yusuke Okuma, Kei Morikawa, Hisashi Tanaka, Takuma Yokoyama, Hidetoshi Itani, Kazuya Horiuchi, Hideyuki Nakagawa, Nobumasa Takahashi, Akihiro Bessho, Kenzo Soejima, Kazuma Kishi, Akira Togashi, Yae Kanai, Koji Ueda, Katsuhisa Horimoto, Noriyuki Matsutani, Nobuhiko Seki. Prospective exosome-focused translational research for afatinib study of non-small cell lung cancer patients expressing EGFR (EXTRA study).
Thoracic cancer.
2019 02; 10(2):395-400. doi:
10.1111/1759-7714.12923. [PMID: 30536780] - Xiaohua Gu, Qiang Zhang, Yun-Bo Chu, Yi-Yang Zhao, Yan-Jun Zhang, David Kuo, Betty Su, Bin Wu. Cost-effectiveness of afatinib, gefitinib, erlotinib and pemetrexed-based chemotherapy as first-line treatments for advanced non-small cell lung cancer in China.
Lung cancer (Amsterdam, Netherlands).
2019 01; 127(?):84-89. doi:
10.1016/j.lungcan.2018.11.029. [PMID: 30642557] - Katsuko Kikuchi, Keiko Nozawa, Naoya Yamazaki, Yasuo Nakai, Ayaka Higashiyama, Masayuki Asano, Yutaka Fujiwara, Shintaro Kanda, Yuichiro Ohe, Atsuo Takashima, Narikazu Boku, Akira Inoue, Masanobu Takahashi, Takahiro Mori, Osamu Taguchi, Yasuhiro Inoue, Hitoshi Mizutani. Instrumental evaluation sensitively detects subclinical skin changes by the epidermal growth factor receptor inhibitors and risk factors for severe acneiform eruption.
The Journal of dermatology.
2019 Jan; 46(1):18-25. doi:
10.1111/1346-8138.14691. [PMID: 30402978] - Eiji Iwama, Kazuko Sakai, Koichi Azuma, Daijiro Harada, Kaname Nosaki, Katsuyuki Hotta, Makoto Nishio, Takayasu Kurata, Tatsuro Fukuhara, Hiroaki Akamatsu, Koichi Goto, Takayuki Shimose, Junji Kishimoto, Yoichi Nakanishi, Kazuto Nishio, Isamu Okamoto. Exploration of resistance mechanisms for epidermal growth factor receptor-tyrosine kinase inhibitors based on plasma analysis by digital polymerase chain reaction and next-generation sequencing.
Cancer science.
2018 Dec; 109(12):3921-3933. doi:
10.1111/cas.13820. [PMID: 30289575] - Mary E R O'Brien, Debashis Sarker, Jaishree Bhosle, Kiruthikah Thillai, Timothy A Yap, Martina Uttenreuther-Fischer, Karine Pemberton, Xidong Jin, Sabrina Wiebe, Johann de Bono, James Spicer. A phase I study to assess afatinib in combination with carboplatin or with carboplatin plus paclitaxel in patients with advanced solid tumors.
Cancer chemotherapy and pharmacology.
2018 11; 82(5):757-766. doi:
10.1007/s00280-018-3661-1. [PMID: 30088048] - Akihiro Yoshimura, Junji Uchino, Keiko Tanimura, Yusuke Chihara, Nobuyo Tamiya, Yoshiko Kaneko, Takayuki Takeda, Osamu Hiranuma, Isao Hasegawa, Yutaka Kubota, Shinsuke Shiotsu, Chieko Takumi, Noriya Hiraoka, Tadaaki Yamada, Koichi Takayama. An observational study of the epidermal growth factor receptor-tyrosine kinase inhibitor resistance mechanism in epidermal growth factor receptor gene mutation-positive non-small cell lung cancer.
Medicine.
2018 Oct; 97(40):e12660. doi:
10.1097/md.0000000000012660. [PMID: 30290647] - Rafael Reis, Laurence Labat, Marie Allard, Pascaline Boudou-Rouquette, Jeanne Chapron, Audrey Bellesoeur, Audrey Thomas-Schoemann, Jennifer Arrondeau, Frédérique Giraud, Jérôme Alexandre, Michel Vidal, François Goldwasser, Benoît Blanchet. Liquid chromatography-tandem mass spectrometric assay for therapeutic drug monitoring of the EGFR inhibitors afatinib, erlotinib and osimertinib, the ALK inhibitor crizotinib and the VEGFR inhibitor nintedanib in human plasma from non-small cell lung cancer patients.
Journal of pharmaceutical and biomedical analysis.
2018 Sep; 158(?):174-183. doi:
10.1016/j.jpba.2018.05.052. [PMID: 29883880] - D Ross Camidge, Lecia V Sequist, Pasi A Jänne, Andrew J Weickhardt, Elizabeth S Dowling, Jeanette Alicea, Jean Fan, Geoffrey R Oxnard. Phase Ib Study of High-dose Intermittent Afatinib in Patients With Advanced Solid Tumors.
Clinical lung cancer.
2018 09; 19(5):e655-e665. doi:
10.1016/j.cllc.2018.04.015. [PMID: 29861396] - Mona M Al-Shehri, Manal A El-Gendy, Adel S El-Azab, Mohammed A Hamidaddin, Ibrahim A Darwish. Development and validation of an ELISA with high sensitivity for therapeutic monitoring of afatinib.
Bioanalysis.
2018 Sep; 10(18):1511-1523. doi:
10.4155/bio-2018-0095. [PMID: 30117333] - Alexander Hann, Evelyn Nosalski, Patrick C Hermann, Jan Egger, Thomas Seufferlein, Frieder Keller. Chemotherapeutic agents eligible for prior dosing in pancreatic cancer patients requiring hemodialysis: a systematic review
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Clinical nephrology.
2018 Aug; 90(2):125-141. doi:
10.5414/cn109327. [PMID: 29578402] - Orsolya Dömötör, Karla Pelivan, Attila Borics, Bernhard K Keppler, Christian R Kowol, Éva A Enyedy. Comparative studies on the human serum albumin binding of the clinically approved EGFR inhibitors gefitinib, erlotinib, afatinib, osimertinib and the investigational inhibitor KP2187.
Journal of pharmaceutical and biomedical analysis.
2018 May; 154(?):321-331. doi:
10.1016/j.jpba.2018.03.011. [PMID: 29567575] - Yan Zhang, Changyuan Wang, Zhihao Liu, Qiang Meng, Xiaokui Huo, Qi Liu, Pengyuan Sun, Xiaobo Yang, Huijun Sun, Xiaodong Ma, Kexin Liu. P-gp is involved in the intestinal absorption and biliary excretion of afatinib in vitro and in rats.
Pharmacological reports : PR.
2018 Apr; 70(2):243-250. doi:
10.1016/j.pharep.2017.10.005. [PMID: 29475007] - Jaume Albiol-Chiva, Josep Esteve-Romero, Juan Peris-Vicente. Development of a method to determine axitinib, lapatinib and afatinib in plasma by micellar liquid chromatography and validation by the European Medicines Agency guidelines.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2018 Feb; 1074-1075(?):61-69. doi:
10.1016/j.jchromb.2017.12.034. [PMID: 29331859] - Katsuhiro Masago, Kei Irie, Shiro Fujita, Fumiko Imamichi, Yutaka Okada, Nobuyuki Katakami, Shoji Fukushima, Yasushi Yatabe. Relationship between Paronychia and Drug Concentrations of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors.
Oncology.
2018; 95(4):251-256. doi:
10.1159/000490177. [PMID: 29902802] - Yongchang Lai, Liang Tao, Yifan Zhao, Xiaomin Zhang, Xingjuan Sun, Qin Wang, Chengfang Xu. Cx32 inhibits TNFα-induced extrinsic apoptosis with and without EGFR suppression.
Oncology reports.
2017 Nov; 38(5):2885-2892. doi:
10.3892/or.2017.5950. [PMID: 28901517] - E E W Cohen, L F Licitra, B Burtness, J Fayette, T Gauler, P M Clement, J J Grau, J M Del Campo, A Mailliez, R I Haddad, J B Vermorken, M Tahara, J Guigay, L Geoffrois, M C Merlano, N Dupuis, N Krämer, X J Cong, N Gibson, F Solca, E Ehrnrooth, J-P H Machiels. Biomarkers predict enhanced clinical outcomes with afatinib versus methotrexate in patients with second-line recurrent and/or metastatic head and neck cancer.
Annals of oncology : official journal of the European Society for Medical Oncology.
2017 Oct; 28(10):2526-2532. doi:
10.1093/annonc/mdx344. [PMID: 28961833] - Reo Hamaguchi, Toshihiro Okamoto, Masaaki Sato, Michiko Hasegawa, Hiromi Wada. Effects of an Alkaline Diet on EGFR-TKI Therapy in EGFR Mutation-positive NSCLC.
Anticancer research.
2017 09; 37(9):5141-5145. doi:
10.21873/anticanres.11934. [PMID: 28870946] - Shirish Gadgeel, Glenwood Goss, Jean-Charles Soria, Enriqueta Felip, Vassilis Georgoulias, Shun Lu, Manuel Cobo, Konstantinos Syrigos, Ki Hyeong Lee, Erdem Göker, Salih Z Guclu, Dolores Isla, Alessandro Morabito, Nicholas Dupuis, Claudia Bühnemann, Nicole Krämer, Flavio Solca, Eva Ehrnrooth, Andrea Ardizzoni. Evaluation of the VeriStrat® serum protein test in patients with advanced squamous cell carcinoma of the lung treated with second-line afatinib or erlotinib in the phase III LUX-Lung 8 study.
Lung cancer (Amsterdam, Netherlands).
2017 07; 109(?):101-108. doi:
10.1016/j.lungcan.2017.05.010. [PMID: 28577938] - Sabrina Wiebe, David Schnell, Raimund Külzer, Dietmar Gansser, Anne Weber, Gudrun Wallenstein, Atef Halabi, Anja Conrad, Sven Wind. Influence of Renal Impairment on the Pharmacokinetics of Afatinib: An Open-Label, Single-Dose Study.
European journal of drug metabolism and pharmacokinetics.
2017 Jun; 42(3):461-469. doi:
10.1007/s13318-016-0359-9. [PMID: 27436099] - Stéphanie van Hoppe, Rolf W Sparidans, Els Wagenaar, Jos H Beijnen, Alfred H Schinkel. Breast cancer resistance protein (BCRP/ABCG2) and P-glycoprotein (P-gp/ABCB1) transport afatinib and restrict its oral availability and brain accumulation.
Pharmacological research.
2017 Jun; 120(?):43-50. doi:
10.1016/j.phrs.2017.01.035. [PMID: 28288939] - Sven Wind, David Schnell, Thomas Ebner, Matthias Freiwald, Peter Stopfer. Clinical Pharmacokinetics and Pharmacodynamics of Afatinib.
Clinical pharmacokinetics.
2017 03; 56(3):235-250. doi:
10.1007/s40262-016-0440-1. [PMID: 27470518] - Shi-Rong Zhang, Lu-Cheng Zhu, Yan-Ping Jiang, Jing Zhang, Ru-Jun Xu, Ya-Si Xu, Bing Xia, Sheng-Lin Ma. Efficacy of afatinib, an irreversible ErbB family blocker, in the treatment of intracerebral metastases of non-small cell lung cancer in mice.
Acta pharmacologica Sinica.
2017 Feb; 38(2):233-240. doi:
10.1038/aps.2016.107. [PMID: 27840411] - Yi-Long Wu, Lecia V Sequist, Cheng-Ping Hu, Jifeng Feng, Shun Lu, Yunchao Huang, Wei Li, Mei Hou, Martin Schuler, Tony Mok, Nobuyuki Yamamoto, Kenneth O'Byrne, Vera Hirsh, Neil Gibson, Dan Massey, Miyoung Kim, James Chih-Hsin Yang. EGFR mutation detection in circulating cell-free DNA of lung adenocarcinoma patients: analysis of LUX-Lung 3 and 6.
British journal of cancer.
2017 Jan; 116(2):175-185. doi:
10.1038/bjc.2016.420. [PMID: 28006816] - E Iwama, K Sakai, K Azuma, T Harada, D Harada, K Nosaki, K Hotta, F Ohyanagi, T Kurata, T Fukuhara, H Akamatsu, K Goto, T Shimose, J Kishimoto, Y Nakanishi, K Nishio, I Okamoto. Monitoring of somatic mutations in circulating cell-free DNA by digital PCR and next-generation sequencing during afatinib treatment in patients with lung adenocarcinoma positive for EGFR activating mutations.
Annals of oncology : official journal of the European Society for Medical Oncology.
2017 01; 28(1):136-141. doi:
10.1093/annonc/mdw531. [PMID: 28177428] - Yo Kawaguchi, Jun Hanaoka, Hideki Hayashi, Naoki Mizusaki, Hirotoshi Iihara, Yoshinori Itoh, Tadashi Sugiyama. Clinical Efficacy of Afatinib Treatment for a Patient with Leptomeningeal Carcinomatosis.
Chemotherapy.
2017; 62(3):147-150. doi:
10.1159/000454727. [PMID: 28030859] - J C-H Yang, L V Sequist, C Zhou, M Schuler, S L Geater, T Mok, C-P Hu, N Yamamoto, J Feng, K O'Byrne, S Lu, V Hirsh, Y Huang, M Sebastian, I Okamoto, N Dickgreber, R Shah, A Märten, D Massey, S Wind, Y-L Wu. Effect of dose adjustment on the safety and efficacy of afatinib for EGFR mutation-positive lung adenocarcinoma: post hoc analyses of the randomized LUX-Lung 3 and 6 trials.
Annals of oncology : official journal of the European Society for Medical Oncology.
2016 11; 27(11):2103-2110. doi:
10.1093/annonc/mdw322. [PMID: 27601237] - Rolf W Sparidans, Hilde Rosing, Johannes J M Rood, Jan H M Schellens, Jos H Beijnen. Liquid chromatography-tandem mass spectrometric assay for therapeutic drug monitoring of the B-Raf inhibitor encorafenib, the EGFR inhibitors afatinib, erlotinib and gefitinib and the O-desmethyl metabolites of erlotinib and gefitinib in human plasma.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2016 Oct; 1033-1034(?):390-398. doi:
10.1016/j.jchromb.2016.09.012. [PMID: 27639128] - Peter Ballard, James W T Yates, Zhenfan Yang, Dong-Wan Kim, James Chih-Hsin Yang, Mireille Cantarini, Kathryn Pickup, Angela Jordan, Mike Hickey, Matthew Grist, Matthew Box, Peter Johnström, Katarina Varnäs, Jonas Malmquist, Kenneth S Thress, Pasi A Jänne, Darren Cross. Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2016 Oct; 22(20):5130-5140. doi:
10.1158/1078-0432.ccr-16-0399. [PMID: 27435396] - Oscar Arrieta, Graciela Cruz-Rico, Enrique Soto-Perez-de-Celis, Laura-Alejandra Ramírez-Tirado, Enrique Caballe-Perez, Jorge-Negueb Martínez-Hernández, Ivan Martinez-Alvarez, Giovanny Soca-Chafre, Eleazar Omar Macedo-Pérez, Horacio Astudillo-de la Vega. Reduction in Hepatocyte Growth Factor Serum Levels is Associated with Improved Prognosis in Advanced Lung Adenocarcinoma Patients Treated with Afatinib: a Phase II Trial.
Targeted oncology.
2016 10; 11(5):619-629. doi:
10.1007/s11523-016-0425-x. [PMID: 27033062] - Adnan A Kadi, Ali S Abdelhameed, Hany W Darwish, Mohamed W Attwa, Nasser S Al-Shakliah. A highly efficient and sensitive LC-MS/MS method for the determination of afatinib in human plasma: application to a metabolic stability study.
Biomedical chromatography : BMC.
2016 Aug; 30(8):1248-55. doi:
10.1002/bmc.3674. [PMID: 26683307] - Hideki Hayashi, Yutaro Kita, Hirotoshi Iihara, Koumei Yanase, Yasushi Ohno, Chiemi Hirose, Maya Yamada, Kenichiro Todoroki, Kiyoyuki Kitaichi, Shinya Minatoguchi, Yoshinori Itoh, Tadashi Sugiyama. Simultaneous and rapid determination of gefitinib, erlotinib and afatinib plasma levels using liquid chromatography/tandem mass spectrometry in patients with non-small-cell lung cancer.
Biomedical chromatography : BMC.
2016 Jul; 30(7):1150-1154. doi:
10.1002/bmc.3642. [PMID: 26525154] - Daniel B Costa, Susan E Jorge, Jason P Moran, Jason A Freed, Jessica A Zerillo, Mark S Huberman, Susumu S Kobayashi. Pulse Afatinib for ERBB2 Exon 20 Insertion-Mutated Lung Adenocarcinomas.
Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer.
2016 06; 11(6):918-23. doi:
10.1016/j.jtho.2016.02.016. [PMID: 26964772] - Ji Zhang, David Lok, Jesse Gray, Steve Grossman, Matt Jones. Development of a novel noncapillary plasma microsampling device for ultra-low volume of blood collection.
Bioanalysis.
2016 May; 8(9):871-80. doi:
10.4155/bio.16.26. [PMID: 27072051] - Yuanbiao Tu, Yiqiang OuYang, Shan Xu, Yan Zhu, Gen Li, Chao Sun, Pengwu Zheng, Wufu Zhu. Design, synthesis, and docking studies of afatinib analogs bearing cinnamamide moiety as potent EGFR inhibitors.
Bioorganic & medicinal chemistry.
2016 Apr; 24(7):1495-503. doi:
10.1016/j.bmc.2016.02.017. [PMID: 26906472] - Rolf W Sparidans, Stephanie van Hoppe, Johannes J M Rood, Alfred H Schinkel, Jan H M Schellens, Jos H Beijnen. Liquid chromatography-tandem mass spectrometric assay for the tyrosine kinase inhibitor afatinib in mouse plasma using salting-out liquid-liquid extraction.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2016 Feb; 1012-1013(?):118-23. doi:
10.1016/j.jchromb.2016.01.025. [PMID: 26826475] - Cong Xue, Ying Tian, Jing Zhang, Yuanyuan Zhao, Jianhua Zhan, Wenfeng Fang, Li Zhang. In vitro and in vivo efficacy of afatinib as a single agent or in combination with gemcitabine for the treatment of nasopharyngeal carcinoma.
Drug design, development and therapy.
2016; 10(?):1299-306. doi:
10.2147/dddt.s94432. [PMID: 27099475] - Amer M Alanazi, Ali Saber Abdelhameed. A Spectroscopic Approach to Investigate the Molecular Interactions between the Newly Approved Irreversible ErbB blocker 'Afatinib' and Bovine Serum Albumin.
PloS one.
2016; 11(1):e0146297. doi:
10.1371/journal.pone.0146297. [PMID: 26751077] - Laura Cosmai, Maurizio Gallieni, Camillo Porta. Renal toxicity of anticancer agents targeting HER2 and EGFR.
Journal of nephrology.
2015 Dec; 28(6):647-57. doi:
10.1007/s40620-015-0226-9. [PMID: 26341657] - Kimio Yonesaka, Keita Kudo, Satomi Nishida, Takayuki Takahama, Tsutomu Iwasa, Takeshi Yoshida, Kaoru Tanaka, Masayuki Takeda, Hiroyasu Kaneda, Isamu Okamoto, Kazuto Nishio, Kazuhiko Nakagawa. The pan-HER family tyrosine kinase inhibitor afatinib overcomes HER3 ligand heregulin-mediated resistance to EGFR inhibitors in non-small cell lung cancer.
Oncotarget.
2015 Oct; 6(32):33602-11. doi:
10.18632/oncotarget.5286. [PMID: 26418897] - Yoshihiro Shibata, Masato Chiba. The role of extrahepatic metabolism in the pharmacokinetics of the targeted covalent inhibitors afatinib, ibrutinib, and neratinib.
Drug metabolism and disposition: the biological fate of chemicals.
2015 Mar; 43(3):375-84. doi:
10.1124/dmd.114.061424. [PMID: 25504185] - Paul Slobbe, Albert D Windhorst, Marijke Stigter-van Walsum, Robert C Schuit, Egbert F Smit, Heiko G Niessen, Flavio Solca, Gerd Stehle, Guus A M S van Dongen, Alex J Poot. Development of [18F]afatinib as new TKI-PET tracer for EGFR positive tumors.
Nuclear medicine and biology.
2014 Oct; 41(9):749-57. doi:
10.1016/j.nucmedbio.2014.06.005. [PMID: 25066021] - David Schnell, Susanne Buschke, Holger Fuchs, Dietmar Gansser, Rainer-Georg Goeldner, Martina Uttenreuther-Fischer, Peter Stopfer, Sven Wind, Marc Petersen-Sylla, Atef Halabi, Rüdiger Koenen. Pharmacokinetics of afatinib in subjects with mild or moderate hepatic impairment.
Cancer chemotherapy and pharmacology.
2014 Aug; 74(2):267-75. doi:
10.1007/s00280-014-2484-y. [PMID: 24906422] - Matthias Freiwald, Ulrike Schmid, Angele Fleury, Sven Wind, Peter Stopfer, Alexander Staab. Population pharmacokinetics of afatinib, an irreversible ErbB family blocker, in patients with various solid tumors.
Cancer chemotherapy and pharmacology.
2014 Apr; 73(4):759-70. doi:
10.1007/s00280-014-2403-2. [PMID: 24522402] - Sven Wind, Thomas Giessmann, Arvid Jungnik, Tobias Brand, Kristell Marzin, Julia Bertulis, Julia Hocke, Dietmar Gansser, Peter Stopfer. Pharmacokinetic drug interactions of afatinib with rifampicin and ritonavir.
Clinical drug investigation.
2014 Mar; 34(3):173-82. doi:
10.1007/s40261-013-0161-2. [PMID: 24399452] - Sven Wind, Marion Schmid, Julia Erhardt, Rainer-Georg Goeldner, Peter Stopfer. Pharmacokinetics of afatinib, a selective irreversible ErbB family blocker, in patients with advanced solid tumours.
Clinical pharmacokinetics.
2013 Dec; 52(12):1101-9. doi:
10.1007/s40262-013-0091-4. [PMID: 23813493] - L Rhoda Molife, Sarah M Rudman, Salma Alam, Daniel S-W Tan, Hartmut Kristeleit, Gary Middleton, David Propper, Liz Bent, Peter Stopfer, Martina Uttenreuther-Fischer, Gudrun Wallenstein, Johann de Bono, James Spicer. Phase II, open-label trial to assess QTcF effects, pharmacokinetics and antitumor activity of afatinib in patients with relapsed or refractory solid tumors.
Cancer chemotherapy and pharmacology.
2013 Dec; 72(6):1213-22. doi:
10.1007/s00280-013-2286-7. [PMID: 24085260] - J B Vermorken, S Rottey, E Ehrnrooth, K Pelling, A Lahogue, S Wind, J-P Machiels. A phase Ib, open-label study to assess the safety of continuous oral treatment with afatinib in combination with two chemotherapy regimens: cisplatin plus paclitaxel and cisplatin plus 5-fluorouracil, in patients with advanced solid tumors.
Annals of oncology : official journal of the European Society for Medical Oncology.
2013 May; 24(5):1392-400. doi:
10.1093/annonc/mds633. [PMID: 23293114] - Kazuto Furuyama, Taishi Harada, Eiji Iwama, Yoshimasa Shiraishi, Kyoko Okamura, Kayo Ijichi, Akiko Fujii, Keiichi Ota, Shuo Wang, Heyan Li, Koichi Takayama, Giuseppe Giaccone, Yoichi Nakanishi. Sensitivity and kinase activity of epidermal growth factor receptor (EGFR) exon 19 and others to EGFR-tyrosine kinase inhibitors.
Cancer science.
2013 May; 104(5):584-9. doi:
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