Regorafenib (BioDeep_00000182881)
human metabolite blood metabolite
代谢物信息卡片
4-(4-(((4-chloro-3-(Trifluoromethyl)phenyl)carbamoyl)amino)-3-fluorophenoxy)-N-methylpyridine-2-carboxamide
化学式: C21H15ClF4N4O3 (482.07687580000004)
中文名称: 瑞格非尼
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CNC(=O)C1=CC(OC2=CC(F)=C(NC(=O)NC3=CC=C(Cl)C(=C3)C(F)(F)F)C=C2)=CC=N1
InChI: InChI=1S/C21H15ClF4N4O3/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26/h2-10H,1H3,(H,27,31)(H2,29,30,32)
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
COVID info from clinicaltrial, clinicaltrials, clinical trial, clinical trials
C471 - Enzyme Inhibitor > C129825 - Antineoplastic Enzyme Inhibitor
C274 - Antineoplastic Agent > C1742 - Angiogenesis Inhibitor
C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor
Corona-virus
Coronavirus
SARS-CoV-2
COVID-19
SARS-CoV
COVID19
SARS2
SARS
Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity[1].
同义名列表
数据库引用编号
11 个数据库交叉引用编号
- ChEBI: CHEBI:68646
- ChEBI: CHEBI:68647
- PubChem: 11167602
- HMDB: HMDB0257137
- DrugBank: DB08896
- ChEMBL: CHEMBL1946170
- Wikipedia: Regorafenib
- chemspider: 9342697
- CAS: 835621-08-4
- CAS: 755037-03-7
- medchemexpress: HY-10331
分类词条
相关代谢途径
Reactome(6)
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
- Jing Zhao, Dongming Yan, Yue Li, Xiaoqing Xu, Fengling Li, Shuang Zhang, Jingyi Jin, Furong Qiu. Simultaneous determination of 11 oral targeted antineoplastic drugs and 2 active metabolites by LC-MS/MS in human plasma and its application to therapeutic drug monitoring in cancer patients.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2024 Apr; 1237(?):124100. doi:
10.1016/j.jchromb.2024.124100. [PMID: 38547701] - Hao Yan, Wentong Wu, Yuhuai Hu, Jinjin Li, Jiangxin Xu, Xueqin Chen, Zhifei Xu, Xiaochun Yang, Bo Yang, Qiaojun He, Peihua Luo. Regorafenib inhibits EphA2 phosphorylation and leads to liver damage via the ERK/MDM2/p53 axis.
Nature communications.
2023 May; 14(1):2756. doi:
10.1038/s41467-023-38430-8. [PMID: 37179400] - Dengning Xia, Cunde Hu, Yulin Hou. Regorafenib loaded self-assembled lipid-based nanocarrier for colorectal cancer treatment via lymphatic absorption.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.
2023 Apr; 185(?):165-176. doi:
10.1016/j.ejpb.2023.02.016. [PMID: 36870399] - Wenhui Jia, Hailong Tian, Jingwen Jiang, Li Zhou, Lei Li, Maochao Luo, Ning Ding, Edouard C Nice, Canhua Huang, Haiyuan Zhang. Brain-Targeted HFn-Cu-REGO Nanoplatform for Site-Specific Delivery and Manipulation of Autophagy and Cuproptosis in Glioblastoma.
Small (Weinheim an der Bergstrasse, Germany).
2023 01; 19(2):e2205354. doi:
10.1002/smll.202205354. [PMID: 36399643] - Shabnam Shahidi, Kobra Rostamizadeh, Mojtaba Fathi, Keivan Nedaei, Ali Ramazani. Combination of Quercetin or/and siRNA-loaded DDAB-mPEG-PCL hybrid nanoparticles reverse resistance to Regorafenib in colon cancer cells.
BMC complementary medicine and therapies.
2022 Dec; 22(1):340. doi:
10.1186/s12906-022-03787-8. [PMID: 36575448] - Michael Jeffers, Christian Kappeler, Iris Kuss, Georg Beckmann, Daniel H Mehnert, Johannes Fredebohm, Michael Teufel. Broad spectrum of regorafenib activity on mutant KIT and absence of clonal selection in gastrointestinal stromal tumor (GIST): correlative analysis from the GRID trial.
Gastric cancer : official journal of the International Gastric Cancer Association and the Japanese Gastric Cancer Association.
2022 05; 25(3):598-608. doi:
10.1007/s10120-021-01274-6. [PMID: 35050442] - Jun Arai, Yumi Otoyama, Ken-Ichi Fujita, Kaku Goto, Masayuki Tojo, Atsushi Katagiri, Hisako Nozawa, Yutaro Kubota, Takehiro Takahashi, Hiroo Ishida, Takuya Tsunoda, Natsumi Matsumoto, Keita Ogawa, Ryo Nakagawa, Ryosuke Muroyama, Naoya Kato, Hitoshi Yoshida. Baseline soluble MICA levels act as a predictive biomarker for the efficacy of regorafenib treatment in colorectal cancer.
BMC cancer.
2022 Apr; 22(1):428. doi:
10.1186/s12885-022-09512-5. [PMID: 35443621] - Carlotta Antoniotti, Federica Marmorino, Alessandra Boccaccino, Silvia Martini, Maria Antista, Daniele Rossini, Valentina Zuco, Michele Prisciandaro, Veronica Conca, Gemma Zucchelli, Beatrice Borelli, Paola Cosentino, Marco M Germani, Maria F Bosco, Martina Carullo, Guglielmo Vetere, Roberto Moretto, Mirella Giordano, Gianluca Masi, Filippo Pietrantonio, Nadia Zaffaroni, Chiara Cremolini. Early modulation of Angiopoietin-2 plasma levels predicts benefit from regorafenib in patients with metastatic colorectal cancer.
European journal of cancer (Oxford, England : 1990).
2022 04; 165(?):116-124. doi:
10.1016/j.ejca.2022.01.025. [PMID: 35231767] - Qinghua Yin, Na Guo, Xueli Zhou, Huan Xu, Song Lei, Ping Fu, Hui Zhong. Regorafenib-induced renal-limited thrombotic microangiopathy: a case report and review of literatures.
BMC nephrology.
2022 03; 23(1):112. doi:
10.1186/s12882-021-02656-9. [PMID: 35305559] - Ayaka Kojima, Masayuki Nadai, Miki Katoh. Species and tissue differences in regorafenib glucuronidation.
Xenobiotica; the fate of foreign compounds in biological systems.
2022 Feb; 52(2):129-133. doi:
10.1080/00498254.2022.2055507. [PMID: 35311470] - Sara Muhammad El-Hanboshy, Maged Wasfy Helmy, Mohammad Mahmoud Abd-Alhaseeb. Catalpol synergistically potentiates the anti-tumour effects of regorafenib against hepatocellular carcinoma via dual inhibition of PI3K/Akt/mTOR/NF-κB and VEGF/VEGFR2 signaling pathways.
Molecular biology reports.
2021 Nov; 48(11):7233-7242. doi:
10.1007/s11033-021-06715-0. [PMID: 34596810] - Masahide Fukudo, Keiko Asai, Chikayoshi Tani, Masashi Miyamoto, Katsuyoshi Ando, Nobuhiro Ueno. Pharmacokinetics of the oral multikinase inhibitor regorafenib and its association with real-world treatment outcomes.
Investigational new drugs.
2021 10; 39(5):1422-1431. doi:
10.1007/s10637-021-01115-4. [PMID: 33830408] - Brice Pastor, Thierry André, Julie Henriques, Isabelle Trouilloud, Christophe Tournigand, Marine Jary, Thibault Mazard, Christophe Louvet, Simon Azan, Audrey Bauer, Benoit Roch, Cynthia Sanchez, Dewi Vernerey, Alain R Thierry, Antoine Adenis. Monitoring levels of circulating cell-free DNA in patients with metastatic colorectal cancer as a potential biomarker of responses to regorafenib treatment.
Molecular oncology.
2021 09; 15(9):2401-2411. doi:
10.1002/1878-0261.12972. [PMID: 33934494] - Tianfeng Yang, Jian Huo, Rui Xu, Yanmin Zhang. Synergistic effect of toosendanin and regorafenib against cell proliferation and migration by regulating WWOX signaling pathway in hepatocellular carcinoma.
Phytotherapy research : PTR.
2021 Aug; 35(8):4567-4578. doi:
10.1002/ptr.7174. [PMID: 34058790] - Kazuo Kobayashi, Erika Sugiyama, Eiji Shinozaki, Takeru Wakatsuki, Masataka Tajima, Hiyori Kidokoro, Takeshi Aoyama, Yasuhiro Nakano, Kazuyoshi Kawakami, Koki Hashimoto, Mitsukuni Suenaga, Takashi Ichimura, Mariko Ogura, Keisho Chin, Izuma Nakayama, Akira Ooki, Daisuke Takahari, Wataru Suzuki, Takashi Yokokawa, Yuichi Minowa, Tomoko Hiraoka, Kenichi Suzuki, Hitoshi Sato, Toshihiro Hama, Kensei Yamaguchi. Associations among plasma concentrations of regorafenib and its metabolites, adverse events, and ABCG2 polymorphisms in patients with metastatic colorectal cancers.
Cancer chemotherapy and pharmacology.
2021 06; 87(6):767-777. doi:
10.1007/s00280-021-04237-x. [PMID: 33635392] - Melvika Pereira, Anjali Prakash, Ameya D Puranik, Nilendu Purandare, Sneha Shah, Archi Agrawal, Venkatesh Rangarajan. Regorafenib-Associated Acute Pancreatitis Diagnosed on 18F-FDG PET/CT.
Clinical nuclear medicine.
2021 May; 46(5):e256-e257. doi:
10.1097/rlu.0000000000003449. [PMID: 33315679] - Mitsukuni Suenaga, W U Zhang, Tetsuo Mashima, Marta Schirripa, Shu Cao, Satoshi Okazaki, Martin D Berger, Yuji Miyamoto, Afsaneh Barzi, Toshiharu Yamaguchi, Heinz-Josef Lenz. Potential Molecular Cross Talk Among CCR5 Pathway Predicts Regorafenib Responsiveness in Metastatic Colorectal Cancer Patients.
Cancer genomics & proteomics.
2021 May; 18(3):317-324. doi:
10.21873/cgp.20262. [PMID: 33893084] - Matthias Unseld, Jelena Belic, Kerstin Pierer, Qing Zhou, Tina Moser, Raimund Bauer, Gudrun Piringer, Armin Gerger, Alexander Siebenhüner, Michael Speicher, Ellen Heitzer, Gerald W Prager. A higher ctDNA fraction decreases survival in regorafenib-treated metastatic colorectal cancer patients. Results from the regorafenib's liquid biopsy translational biomarker phase II pilot study.
International journal of cancer.
2021 03; 148(6):1452-1461. doi:
10.1002/ijc.33303. [PMID: 32949150] - Bo Yan, Youwei Ai, Qi Sun, Yan Ma, Yang Cao, Jiawen Wang, Zhiyuan Zhang, Xiaodong Wang. Membrane Damage during Ferroptosis Is Caused by Oxidation of Phospholipids Catalyzed by the Oxidoreductases POR and CYB5R1.
Molecular cell.
2021 01; 81(2):355-369.e10. doi:
10.1016/j.molcel.2020.11.024. [PMID: 33321093] - Hamid Tanzadehpanah, Hanie Mahaki, Mohammadreza Moradi, Saeid Afshar, Neda Hosseinpour Moghadam, Sadegh Salehzadeh, Rezvan Najafi, Razieh Amini, Massoud Saidijam. The Use of Molecular Docking and Spectroscopic Methods for Investigation of The Interaction Between Regorafenib with Human Serum Albumin (HSA) and Calf Thymus DNA (Ct-DNA) In The Presence Of Different Site Markers.
Protein and peptide letters.
2021; 28(3):290-303. doi:
10.2174/0929866527666200921164536. [PMID: 32957871] - John L Marshall. Third-line treatments for the management of metastatic colorectal cancer: why to change the mechanism of action after frontline chemotherapy, and insights into management during the COVID-19 pandemic.
Clinical advances in hematology & oncology : H&O.
2020 10; 18 Suppl 16(10):6-14. doi:
NULL. [PMID: 33843850] - Axel Grothey, Fortunato Ciardiello, John L Marshall. How to incorporate a chemo-free interval into the management of metastatic colorectal cancer.
Clinical advances in hematology & oncology : H&O.
2020 Oct; 18 Suppl 16(10):1-24. doi:
NULL. [PMID: 33843848] - Yingmiao Liu, Jing Lyu, Kirsten Bell Burdett, Alexander B Sibley, Ace J Hatch, Mark D Starr, John C Brady, Kelli Hammond, Federica Marmorino, Daniele Rossini, Richard M Goldberg, Alfredo Falcone, Chiara Cremolini, Kouros Owzar, Anastasia Ivanova, Dominic T Moore, Michael S Lee, Hanna K Sanoff, Federico Innocenti, Andrew B Nixon. Prognostic and Predictive Biomarkers in Patients with Metastatic Colorectal Cancer Receiving Regorafenib.
Molecular cancer therapeutics.
2020 10; 19(10):2146-2154. doi:
10.1158/1535-7163.mct-20-0249. [PMID: 32747417] - Yutaro Kubota, Ken-Ichi Fujita, Takehiro Takahashi, Yu Sunakawa, Hiroo Ishida, Kazuyuki Hamada, Wataru Ichikawa, Takuya Tsunoda, Kazuhiro Shimada, Yusuke Masuo, Yukio Kato, Yasutsuna Sasaki. Higher Systemic Exposure to Unbound Active Metabolites of Regorafenib Is Associated With Short Progression-Free Survival in Colorectal Cancer Patients.
Clinical pharmacology and therapeutics.
2020 09; 108(3):586-595. doi:
10.1002/cpt.1810. [PMID: 32034953] - Valentina Iacuzzi, Martina Zanchetta, Sara Gagno, Ariana Soledad Poetto, Marco Orleni, Elena Marangon, Michela Guardascione, Luisa Foltran, Bianca Posocco, Giuseppe Toffoli. A LC-MS/MS method for therapeutic drug monitoring of sorafenib, regorafenib and their active metabolites in patients with hepatocellular carcinoma.
Journal of pharmaceutical and biomedical analysis.
2020 Aug; 187(?):113358. doi:
10.1016/j.jpba.2020.113358. [PMID: 32460216] - Richard D Kim, Hanna K Sanoff, Andrew S Poklepovic, Heloisa Soares, Jongphil Kim, Jing Lyu, Yingmiao Liu, Andrew B Nixon, Dae Won Kim. A multi-institutional phase 2 trial of regorafenib in refractory advanced biliary tract cancer.
Cancer.
2020 08; 126(15):3464-3470. doi:
10.1002/cncr.32964. [PMID: 32453456] - Jean-Yves Blay, César Serrano, Michael C Heinrich, John Zalcberg, Sebastian Bauer, Hans Gelderblom, Patrick Schöffski, Robin L Jones, Steven Attia, Gina D'Amato, Ping Chi, Peter Reichardt, Julie Meade, Kelvin Shi, Rodrigo Ruiz-Soto, Suzanne George, Margaret von Mehren. Ripretinib in patients with advanced gastrointestinal stromal tumours (INVICTUS): a double-blind, randomised, placebo-controlled, phase 3 trial.
The Lancet. Oncology.
2020 07; 21(7):923-934. doi:
10.1016/s1470-2045(20)30168-6. [PMID: 32511981] - Sunil Kumar Yadava, Suparna Mercy Basu, Meenakshi Chauhan, Kshipra Sharma, Arpan Pradhan, Remya V, Jyotsnendu Giri. Low temperature, easy scaling up method for development of smart nanostructure hybrid lipid capsules for drug delivery application.
Colloids and surfaces. B, Biointerfaces.
2020 Jun; 190(?):110927. doi:
10.1016/j.colsurfb.2020.110927. [PMID: 32169777] - Takeshi Suzuki, Yasutaka Sukawa, Chiyo K Imamura, Toshiki Masuishi, Hironaga Satake, Yosuke Kumekawa, Shinsuke Funakoshi, Masahito Kotaka, Yoshiki Horie, Sadayuki Kawai, Hiroyuki Okuda, Tetsuji Terazawa, Chihiro Kondoh, Ken Kato, Kenichi Yoshimura, Hideki Ishikawa, Yasuo Hamamoto, Narikazu Boku, Hiromasa Takaishi, Takanori Kanai. A Phase II Study of Regorafenib With a Lower Starting Dose in Patients With Metastatic Colorectal Cancer: Exposure-Toxicity Analysis of Unbound Regorafenib and Its Active Metabolites (RESET Trial).
Clinical colorectal cancer.
2020 03; 19(1):13-21.e3. doi:
10.1016/j.clcc.2019.10.004. [PMID: 31732439] - César Serrano, Alessandro Leal, Yanan Kuang, Jeffrey A Morgan, Constance M Barysauskas, Jillian Phallen, Olivia Triplett, Adrián Mariño-Enríquez, Andrew J Wagner, George D Demetri, Victor E Velculescu, Cloud P Paweletz, Jonathan A Fletcher, Suzanne George. Phase I Study of Rapid Alternation of Sunitinib and Regorafenib for the Treatment of Tyrosine Kinase Inhibitor Refractory Gastrointestinal Stromal Tumors.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2019 12; 25(24):7287-7293. doi:
10.1158/1078-0432.ccr-19-2150. [PMID: 31471313] - Massimo Iavarone, Federica Invernizzi, Carolin Czauderna, Marco Sanduzzi-Zamparelli, Sherrie Bhoori, Giuliana Amaddeo, Matteo A Manini, Miguel F López, Margarita Anders, Matthias Pinter, Maria J B Rodríguez, Mario R Cristóbal, Gabriel A Soteras, Federico Piñero, Gerda E Villadsen, Arndt Weinmann, Gonzalo Crespo, Vincenzo Mazzaferro, Helene Regnault, Massimo De Giorgio, Maria L González-Diéguez, Maria F Donato, Maria Varela, Marcus-Alexander Wörns, Jordi Bruix, Pietro Lampertico, Maria Reig. Preliminary experience on safety of regorafenib after sorafenib failure in recurrent hepatocellular carcinoma after liver transplantation.
American journal of transplantation : official journal of the American Society of Transplantation and the American Society of Transplant Surgeons.
2019 11; 19(11):3176-3184. doi:
10.1111/ajt.15551. [PMID: 31365177] - Nikolaos Tsakiris, Malamatenia Papavasileiou, Elia Bozzato, Alessandra Lopes, Arnaud M Vigneron, Véronique Préat. Combinational drug-loaded lipid nanocapsules for the treatment of cancer.
International journal of pharmaceutics.
2019 Oct; 569(?):118588. doi:
10.1016/j.ijpharm.2019.118588. [PMID: 31377406] - Marta Schirripa, Beatrice Borelli, Romina D'Aurizio, Simone Lubrano, Chiara Cremolini, Gemma Zucchelli, Carlotta Antoniotti, Federica Marmorino, Alessandra Anna Prete, Sabina Murgioni, Francesca Bergamo, Vittorina Zagonel, Andrea Tuccoli, Andrea Marranci, Milena Rizzo, Lorena Tedeschi, Letizia Magnoni, Alfredo Falcone, Fotios Loupakis, Laura Poliseno. Early modifications of circulating microRNAs levels in metastatic colorectal cancer patients treated with regorafenib.
The pharmacogenomics journal.
2019 10; 19(5):455-464. doi:
10.1038/s41397-019-0075-3. [PMID: 30686821] - Floor J E Lubberman, Winette T A van der Graaf, Lei Xu, Adriaan Cleton, George D Demetri, Hans Gelderblom, Nielka P van Erp. The effect of gastrectomy on regorafenib exposure and progression-free survival in patients with advanced gastrointestinal stromal tumours.
British journal of clinical pharmacology.
2019 10; 85(10):2399-2404. doi:
10.1111/bcp.14061. [PMID: 31290566] - Jeffrey Melson Clarke, Gerard C Blobe, John H Strickler, Hope Elizabeth Uronis, S Yousuf Zafar, Michael Morse, Evan Dropkin, Leigh Howard, Margot O'Neill, Christel N Rushing, Donna Niedzwiecki, Hollie Watson, Emily Bolch, Christy Arrowood, Yingmiao Liu, Andrew B Nixon, Herbert I Hurwitz. A phase Ib study of the combination regorafenib with PF-03446962 in patients with refractory metastatic colorectal cancer (REGAL-1 trial).
Cancer chemotherapy and pharmacology.
2019 10; 84(4):909-917. doi:
10.1007/s00280-019-03916-0. [PMID: 31444620] - Shengnan Liu, Yang Du, He Ma, Qian Liang, Xu Zhu, Jie Tian. Preclinical comparison of regorafenib and sorafenib efficacy for hepatocellular carcinoma using multimodality molecular imaging.
Cancer letters.
2019 07; 453(?):74-83. doi:
10.1016/j.canlet.2019.03.037. [PMID: 30928380] - Aya Hasan Al-Shammari, Yusuke Masuo, Ken-Ichi Fujita, Yuka Yoshikawa, Noritaka Nakamichi, Yutaro Kubota, Yasutsuna Sasaki, Yukio Kato. Influx and Efflux Transporters Contribute to the Increased Dermal Exposure to Active Metabolite of Regorafenib After Repeated Oral Administration in Mice.
Journal of pharmaceutical sciences.
2019 06; 108(6):2173-2179. doi:
10.1016/j.xphs.2019.01.018. [PMID: 30685396] - Yuanshan Yao, Yinjie Zhou, Qingwang Hua. Comparing efficacy and safety of regorafenib versus pemetrexed in lung cancer: A preliminary clinical trial evaluating effect of inflammatory biomarkers on disease progression.
Pakistan journal of pharmaceutical sciences.
2019 May; 32(3 Special):1293-1299. doi:
NULL. [PMID: 31551206] - Michael Teufel, Henrik Seidel, Karl Köchert, Gerold Meinhardt, Richard S Finn, Josep M Llovet, Jordi Bruix. Biomarkers Associated With Response to Regorafenib in Patients With Hepatocellular Carcinoma.
Gastroenterology.
2019 05; 156(6):1731-1741. doi:
10.1053/j.gastro.2019.01.261. [PMID: 30738047] - Hideaki Bando, Yoshinori Kagawa, Takeshi Kato, Kiwamu Akagi, Tadamichi Denda, Tomohiro Nishina, Yoshito Komatsu, Eiji Oki, Toshihiro Kudo, Hiroshi Kumamoto, Takeharu Yamanaka, Takayuki Yoshino. A multicentre, prospective study of plasma circulating tumour DNA test for detecting RAS mutation in patients with metastatic colorectal cancer.
British journal of cancer.
2019 05; 120(10):982-986. doi:
10.1038/s41416-019-0457-y. [PMID: 31015557] - K Shitara, T Yamanaka, T Denda, Y Tsuji, K Shinozaki, Y Komatsu, Y Kobayashi, J Furuse, H Okuda, M Asayama, K Akiyoshi, Y Kagawa, T Kato, E Oki, T Ando, Y Hagiwara, Y Ohashi, T Yoshino. REVERCE: a randomized phase II study of regorafenib followed by cetuximab versus the reverse sequence for previously treated metastatic colorectal cancer patients.
Annals of oncology : official journal of the European Society for Medical Oncology.
2019 02; 30(2):259-265. doi:
10.1093/annonc/mdy526. [PMID: 30508156] - Akimitsu Maeda, Kei Irie, Hitoshi Ando, Ayako Hasegawa, Hiroya Taniguchi, Shigenori Kadowaki, Kei Muro, Masahiro Tajika, Masahiro Aoki, Kazuhide Inaguma, Masaki Kajita, Akio Fujimura, Shoji Fukushima. Associations among regorafenib concentrations, severe adverse reactions, and ABCG2 and OATP1B1 polymorphisms.
Cancer chemotherapy and pharmacology.
2019 01; 83(1):107-113. doi:
10.1007/s00280-018-3710-9. [PMID: 30368586] - Kenji Tsuchihashi, Mamoru Ito, Toshikazu Moriwaki, Shota Fukuoka, Hiroya Taniguchi, Atsuo Takashima, Yosuke Kumekawa, Takeshi Kajiwara, Kentaro Yamazaki, Taito Esaki, Akitaka Makiyama, Tadamichi Denda, Hironaga Satake, Takeshi Suto, Naotoshi Sugimoto, Kenji Katsumata, Toshiaki Ishikawa, Tomomi Kashiwada, Eiji Oki, Yoshito Komatsu, Hiroyuki Okuyama, Daisuke Sakai, Hideki Ueno, Takao Tamura, Kimihiro Yamashita, Junji Kishimoto, Yasuhiro Shimada, Eishi Baba. Role of Predictive Value of the Modified Glasgow Prognostic Score for Later-line Chemotherapy in Patients With Metastatic Colorectal Cancer.
Clinical colorectal cancer.
2018 12; 17(4):e687-e697. doi:
10.1016/j.clcc.2018.07.004. [PMID: 30149986] - Yi-Kun Wang, Xue-Rong Xiao, Kang-Ping Xu, Fei Li. Metabolic profiling of the anti-tumor drug regorafenib in mice.
Journal of pharmaceutical and biomedical analysis.
2018 Sep; 159(?):524-535. doi:
10.1016/j.jpba.2018.07.039. [PMID: 30055476] - Qiang Fu, Mingqing Chen, Shuiying Hu, Craig A McElroy, Ron H Mathijssen, Alex Sparreboom, Sharyn D Baker. Development and validation of an analytical method for regorafenib and its metabolites in mouse plasma.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2018 Jul; 1090(?):43-51. doi:
10.1016/j.jchromb.2018.05.005. [PMID: 29783173] - Mao-Hua Cai, Xiao-Gang Xu, Shi-Li Yan, Ze Sun, Yin Ying, Bai-Kui Wang, Yue-Xing Tu. Regorafenib suppresses colon tumorigenesis and the generation of drug resistant cancer stem-like cells via modulation of miR-34a associated signaling.
Journal of experimental & clinical cancer research : CR.
2018 Jul; 37(1):151. doi:
10.1186/s13046-018-0836-x. [PMID: 30005681] - Torsten Zimmermann, Joachim Höchel, Michael Becka, Michael K Boettger, Beate Rohde, Barbara Schug, Kathleen S Kunert, Frank Donath. Topical administration of regorafenib eye drops: phase I dose-escalation study in healthy volunteers.
British journal of clinical pharmacology.
2018 05; 84(5):865-875. doi:
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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] - Yang Wang, ShengZhuo Liu, Shan Liu, Xia Li, QiuYan Liu, XiaoLan Zou, Min Zhu, YongXin Jiang. Regorafenib Treatment for Management of Colorectal Cancer: A Systematic Review and Meta-analysis of 6 Randomized Controlled Trials.
American journal of therapeutics.
2018 Mar; 25(2):e276-e278. doi:
10.1097/mjt.0000000000000680. [PMID: 28938279] - Michael Gerisch, Frank-Thorsten Hafner, Dieter Lang, Martin Radtke, Konstanze Diefenbach, Adriaan Cleton, John Lettieri. Mass balance, metabolic disposition, and pharmacokinetics of a single oral dose of regorafenib in healthy human subjects.
Cancer chemotherapy and pharmacology.
2018 01; 81(1):195-206. doi:
10.1007/s00280-017-3480-9. [PMID: 29188322] - M Unseld, M Filip, S Seirl, A Gleiss, D Bianconi, M Kieler, S Demyanets, W Scheithauer, C Zielinski, G Prager. Regorafenib therapy in metastatic colorectal cancer patients: markers and outcome in an actual clinical setting.
Neoplasma.
2018 ; 65(4):599-603. doi:
10.4149/neo_2018_170727n506. [PMID: 29940763] - Ken-Ichi Fujita, Yusuke Masuo, Erina Yamazaki, Toshiki Shibutani, Yutaro Kubota, Noritaka Nakamichi, Yasutsuna Sasaki, Yukio Kato. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites.
Journal of pharmaceutical sciences.
2017 09; 106(9):2632-2641. doi:
10.1016/j.xphs.2017.04.064. [PMID: 28479358] - Yi Yun Pang, Yeong Lan Tan, Han Kiat Ho. Investigation of the effect of plasma albumin levels on regorafenib-induced hepatotoxicity using a validated liquid chromatography-tandem mass spectrometry method.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2017 Sep; 1061-1062(?):220-224. doi:
10.1016/j.jchromb.2017.07.023. [PMID: 28750235] - Kenji Yoshino, Dai Manaka, Ryo Kudo, Shunpei Kanai, Eisei Mitsuoka, Satoshi Kanto, Shinya Hamasu, Sayuri Konishi, Ryuta Nishitai. Metastatic colorectal cancer responsive to regorafenib for 2 years: a case report.
Journal of medical case reports.
2017 Aug; 11(1):227. doi:
10.1186/s13256-017-1366-4. [PMID: 28818109] - Marie Allard, Nihel Khoudour, Benoît Rousseau, Charlotte Joly, Charlotte Costentin, Benoît Blanchet, Christophe Tournigand, Anne Hulin. Simultaneous analysis of regorafenib and sorafenib and three of their metabolites in human plasma using LC-MS/MS.
Journal of pharmaceutical and biomedical analysis.
2017 Aug; 142(?):42-48. doi:
10.1016/j.jpba.2017.04.053. [PMID: 28494338] - Shiro Nakae, Yuya Nogi, Jun Arima, Daiki Okamoto, Naoki Urakawa, Masataka Fujikawa, Hidetoshi Gon, Atsushi Takebe, Makoto Shinzeki, Kenichi Tanaka, Hideto Senzaki. [A Case of Recurrent Colorectal Cancer with Bilateral Ovarian Metastases That Were Reduced with Regorafenib Therapy].
Gan to kagaku ryoho. Cancer & chemotherapy.
2017 Jul; 44(7):607-610. doi:
NULL. [PMID: 28790267] - Yi-Jun Wang, Yun-Kai Zhang, Guan-Nan Zhang, Sweilem B Al Rihani, Meng-Ning Wei, Pranav Gupta, Xiao-Yu Zhang, Suneet Shukla, Suresh V Ambudkar, Amal Kaddoumi, Zhi Shi, Zhe-Sheng Chen. Regorafenib overcomes chemotherapeutic multidrug resistance mediated by ABCB1 transporter in colorectal cancer: In vitro and in vivo study.
Cancer letters.
2017 06; 396(?):145-154. doi:
10.1016/j.canlet.2017.03.011. [PMID: 28302530] - C-H Chen, L W R Fong, E Yu, R Wu, J F Trott, R H Weiss. Upregulation of MARCKS in kidney cancer and its potential as a therapeutic target.
Oncogene.
2017 06; 36(25):3588-3598. doi:
10.1038/onc.2016.510. [PMID: 28166200] - Nao Kakizawa, Koichi Suzuki, Taro Fukui, Yuji Takayama, Kosuke Ichida, Yuta Muto, Fumi Hasegawa, Fumiaki Watanabe, Rina Kikugawa, Shingo Tsujinaka, Kazushige Futsuhara, Yasuyuki Miyakura, Hiroshi Noda, Toshiki Rikiyama. Clinical and molecular assessment of regorafenib monotherapy.
Oncology reports.
2017 Apr; 37(4):2506-2512. doi:
10.3892/or.2017.5456. [PMID: 28259999] - Michela Quirino, Sabrina Rossi, Giovanni Schinzari, Michele Basso, Antonia Strippoli, Alessandra Cassano, Carlo Barone. Unexpected side effect in mCRC: A care-compliant case report of regorafenib-induced hyperammonemic encephalopathy.
Medicine.
2017 Apr; 96(16):e6522. doi:
10.1097/md.0000000000006522. [PMID: 28422839] - Wen-Ji Zhang, Yong Li, Meng-Ning Wei, Yao Chen, Jian-Ge Qiu, Qi-Wei Jiang, Yang Yang, Di-Wei Zheng, Wu-Ming Qin, Jia-Rong Huang, Kun Wang, Wen-Juan Zhang, Yi-Jun Wang, Dong-Hua Yang, Zhe-Sheng Chen, Zhi Shi. Synergistic antitumor activity of regorafenib and lapatinib in preclinical models of human colorectal cancer.
Cancer letters.
2017 02; 386(?):100-109. doi:
10.1016/j.canlet.2016.11.011. [PMID: 27864115] - Shida Yang, Zhiyong Zhu, Xiaobing Zhang, Ning Zhang, Zhicheng Yao. Idelalisib induces PUMA-dependent apoptosis in colon cancer cells.
Oncotarget.
2017 Jan; 8(4):6102-6113. doi:
10.18632/oncotarget.14043. [PMID: 28008149] - Ralf Stefan Eschbach, Dirk-Andre Clevert, Heidrun Hirner-Eppeneder, Michael Ingrisch, Matthias Moser, Jessica Schuster, Dina Tadros, Moritz Schneider, Philipp Maximilian Kazmierczak, Maximilian Reiser, Clemens C Cyran. Contrast-Enhanced Ultrasound with VEGFR2-Targeted Microbubbles for Monitoring Regorafenib Therapy Effects in Experimental Colorectal Adenocarcinomas in Rats with DCE-MRI and Immunohistochemical Validation.
PloS one.
2017; 12(1):e0169323. doi:
10.1371/journal.pone.0169323. [PMID: 28060884] - Azusa Komori, Hiroya Taniguchi, Satoshi Hamauchi, Toshiki Masuishi, Yosuke Kito, Yukiya Narita, Takahiro Tsushima, Makoto Ishihara, Akiko Todaka, Tsutomu Tanaka, Tomoya Yokota, Shigenori Kadowaki, Nozomu Machida, Takashi Ura, Akira Fukutomi, Masashi Ando, Yusuke Onozawa, Masahiro Tajika, Hirofumi Yasui, Kei Muro, Keita Mori, Kentaro Yamazaki. Serum CA19-9 Response Is an Early Predictive Marker of Efficacy of Regorafenib in Refractory Metastatic Colorectal Cancer.
Oncology.
2017; 93(5):329-335. doi:
10.1159/000479280. [PMID: 28866662] - Kazuomi Ueshima, Naoshi Nishida, Masatoshi Kudo. Sorafenib-Regorafenib Sequential Therapy in Advanced Hepatocellular Carcinoma: A Single-Institute Experience.
Digestive diseases (Basel, Switzerland).
2017; 35(6):611-617. doi:
10.1159/000480257. [PMID: 29040994] - Dieter Zopf, Iduna Fichtner, Ajay Bhargava, Wolfram Steinke, Karl-Heinz Thierauch, Konstanze Diefenbach, Scott Wilhelm, Frank-Thorsten Hafner, Michael Gerisch. Pharmacologic activity and pharmacokinetics of metabolites of regorafenib in preclinical models.
Cancer medicine.
2016 11; 5(11):3176-3185. doi:
10.1002/cam4.883. [PMID: 27734608] - Ivan Haralampiev, Holger A Scheidt, Tobias Abel, Madlen Luckner, Andreas Herrmann, Daniel Huster, Peter Müller. The interaction of sorafenib and regorafenib with membranes is modulated by their lipid composition.
Biochimica et biophysica acta.
2016 Nov; 1858(11):2871-2881. doi:
10.1016/j.bbamem.2016.08.014. [PMID: 27581086] - Kazuma Fujita, Masatomo Miura, Hiroyuki Shibata. Quantitative determination of regorafenib and its two major metabolites in human plasma with high-performance liquid chromatography and ultraviolet detection.
Biomedical chromatography : BMC.
2016 Oct; 30(10):1611-7. doi:
10.1002/bmc.3730. [PMID: 27037679] - Nick Pavlakis, Katrin M Sjoquist, Andrew J Martin, Eric Tsobanis, Sonia Yip, Yoon-Koo Kang, Yung-Jue Bang, Thierry Alcindor, Christopher J O'Callaghan, Margot J Burnell, Niall C Tebbutt, Sun Young Rha, Jeeyun Lee, Jae-Yong Cho, Lara R Lipton, Mark Wong, Andrew Strickland, Jin Won Kim, John R Zalcberg, John Simes, David Goldstein. Regorafenib for the Treatment of Advanced Gastric Cancer (INTEGRATE): A Multinational Placebo-Controlled Phase II Trial.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
2016 08; 34(23):2728-35. doi:
10.1200/jco.2015.65.1901. [PMID: 27325864] - Mitsukuni Suenaga, Tetsuo Mashima, Naomi Kawata, Takeru Wakatsuki, Yuki Horiike, Satoshi Matsusaka, Shingo Dan, Eiji Shinozaki, Hiroyuki Seimiya, Nobuyuki Mizunuma, Kensei Yamaguchi, Toshiharu Yamaguchi. Serum VEGF-A and CCL5 levels as candidate biomarkers for efficacy and toxicity of regorafenib in patients with metastatic colorectal cancer.
Oncotarget.
2016 Jun; 7(23):34811-23. doi:
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Molecular cancer therapeutics.
2016 05; 15(5):890-8. doi:
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Bulletin du cancer.
2016 Mar; 103(3):259-72. doi:
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Advances in experimental medicine and biology.
2016; 924(?):187-189. doi:
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Oncotarget.
2015 Oct; 6(32):33982-92. doi:
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Anticancer research.
2015 Sep; 35(9):4681-9. doi:
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The Lancet. Oncology.
2015 Aug; 16(8):937-48. doi:
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Anticancer research.
2015 Jul; 35(7):4037-41. doi:
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Pharmaceutical research.
2015 Jul; 32(7):2205-16. doi:
10.1007/s11095-014-1609-7. [PMID: 25563977] - Marta M Wells, Tommy S Tillman, David D Mowrey, Tianmo Sun, Yan Xu, Pei Tang. Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain.
Journal of medicinal chemistry.
2015 Apr; 58(7):2958-2966. doi:
10.1021/jm501873p. [PMID: 25790278] - Andrea Li Ann Wong, Joline Si Jing Lim, Arvind Sinha, Anil Gopinathan, Robert Lim, Chee-Seng Tan, Thomas Soh, Sudhakar Venkatesh, Christina Titin, Nur Sabrina Sapari, Soo-Chin Lee, Wei-Peng Yong, David Shao Ping Tan, Brendan Pang, Ting-Ting Wang, Ying-Kiat Zee, Richie Soong, Zuzana Trnkova, Chetan Lathia, Jean-Paul Thiery, Scott Wilhelm, Michael Jeffers, Boon-Cher Goh. Tumour pharmacodynamics and circulating cell free DNA in patients with refractory colorectal carcinoma treated with regorafenib.
Journal of translational medicine.
2015 Feb; 13(?):57. doi:
10.1186/s12967-015-0405-4. [PMID: 25889309] - Ralf S Eschbach, Wolfgang P Fendler, Philipp M Kazmierczak, Marcus Hacker, Axel Rominger, Janette Carlsen, Heidrun Hirner-Eppeneder, Jessica Schuster, Matthias Moser, Lukas Havla, Moritz J Schneider, Michael Ingrisch, Lukas Spaeth, Maximilian F Reiser, Konstantin Nikolaou, Clemens C Cyran. Correlation of perfusion MRI and 18F-FDG PET imaging biomarkers for monitoring regorafenib therapy in experimental colon carcinomas with immunohistochemical validation.
PloS one.
2015; 10(2):e0115543. doi:
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PloS one.
2015; 10(9):e0138452. doi:
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Biomedical chromatography : BMC.
2014 Oct; 28(10):1366-70. doi:
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Bioanalysis.
2014; 6(14):1923-37. doi:
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Molecular pharmacology.
2013 Oct; 84(4):562-71. doi:
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British journal of cancer.
2013 Sep; 109(5):1230-42. doi:
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Cancer biology & therapy.
2013 Aug; 14(8):703-10. doi:
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Current oncology reports.
2013 Apr; 15(2):91-7. doi:
10.1007/s11912-013-0292-x. [PMID: 23334510] - Clemens C Cyran, Philipp M Kazmierczak, Heidrun Hirner, Matthias Moser, Michael Ingrisch, Lukas Havla, Alexandra Michels, Ralf Eschbach, Bettina Schwarz, Maximilian F Reiser, Christiane J Bruns, Konstantin Nikolaou. Regorafenib effects on human colon carcinoma xenografts monitored by dynamic contrast-enhanced computed tomography with immunohistochemical validation.
PloS one.
2013; 8(9):e76009. doi:
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American journal of hypertension.
2012 Oct; 25(10):1118-23. doi:
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The Lancet. Oncology.
2012 Oct; 13(10):1055-62. doi:
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The Lancet. Oncology.
2012 Oct; 13(10):970-1. doi:
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Clinical cancer research : an official journal of the American Association for Cancer Research.
2012 May; 18(9):2658-67. doi:
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