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https://www.readbyqxmd.com/read/28236743/direct-binding-of-microrna-21-pre-element-with-regorafenib-an-alternative-mechanism-for-anti-colorectal-cancer-chemotherapy
#1
Xiaobing Chen, Bojian Xie, Liang Cao, Feng Zhu, Beibei Chen, Huifang Lv, Xingxing Fan, Lili Han, Liangyu Bie, Xinguang Cao, Xiaokun Shen, Feilin Cao
The Regorafenib is a broad-spectrum kinase inhibitor that has been approved to treat colorectal cancer (CRC). However, evidences have shown that the agent is also implicated in drug interaction with microRNA-21 (miR-21), an oncogenic miRNA which plays a key role in resisting programmed cell death in CRC cells. Here, we supposed that, instead of kinase inhibition, Regorafenib can directly bind to and then stabilize miR-21 pre-element, thus preventing RNase Dicer-meditated cleavage of the pre-element to mature miR-21...
February 10, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28223677/-two-cases-of-fournier-s-gangrene-that-occurred-during-chemotherapy-for-rectal-cancer
#2
Makoto Koyama, Masato Kitazawa, Takehito Ehara, Yuta Yamamoto, Akira Suzuki, Yusuke Miyagawa, Shinichi Miyagawa
Two cases of Fournier's gangrene occurred during chemotherapy for advanced rectal cancer. Patients were treated using surgical debridement and antibiotic therapy. Case 1: A 66-year-old man had advanced rectal cancer with para-aortic and inguinal lymph node metastases. He received a sigmoid colostomy and chemotherapy(capecitabine, oxaliplatin, bevacizumab). Due to progression of the rectal mass, we performed radiotherapy(30 Gy)and chemotherapy(irinotecan, S-1, bevacizumab). After 14 days, he was hospitalized with a diagnosis of Fournier's gangrene with anal pain and fever...
February 2017: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/28214672/evaluation-of-molecular-chaperone-drug-function-regorafenib-and-%C3%AE-cyclodextrins
#3
Xiurong Hu, Mengying Sun, Yang Li, Guping Tang
Regorafenib (RG) was an oral multi-kinase inhibitor with poor water solubility. In order to enhance the drug's solubility, dissolution and bioavailability, the binary molecular chaperone drug between RG and β-cyclodetrin (β-CD) had prepared by co-crystallization. The structure of RG-β-CD was characterized by thermal analysis, powder X-ray diffraction, infrared spectroscopy and nuclear magnetic resonance. Phase-solubility study revealed the higher solubility and complexing ability of β-CDwith RG.The solubility and dissolution of RG-β-CD was significantly enhanced in pH 1...
February 7, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28198177/innovative-molecular-targeted-agents-in-hepatocellular-carcinoma-new-gladiators-on-the-arena
#4
Jose Ferri, Yanina Dockx, Luisa Vonghia, Konstantinos Papadimitriou, Marika Rasschaert, Sven Francque, Marc Peeters, Christian Rolfo
Treatment of advanced hepatocellular carcinoma remains a challenge, with discouraging results in terms of survival. Following the approval of the multikinase inhibitor sorafenib, a large number of molecular targeted agents have been tested, but many have failed to demonstrate significant efficacy in clinical trials. However, the deeper knowledge in HCC pathogenesis achieved through the years has enabled us to explore new targetable pathways as well as biomarkers that could lead to treatment personalization...
February 14, 2017: Minerva Chirurgica
https://www.readbyqxmd.com/read/28183254/metastatic-colorectal-cancer-role-of-target-therapies-and-future-perspectives
#5
Anna Nappi, Massimiliano Berretta, Carmela Romano, Salvatore Tafuto, Antonino Cassata, Rossana Casaretti, Lucrezia Silvestro, Chiara De Divitiis, Lara Alessandrini, Francesco Fiorica, Alessandro Ottaiano, Guglielmo Nasti
Today, we are experiencing a real cultural revolution in the therapeutic approach to cancer of the colon - rectum, that, by orphan disease, it is now becoming an important paradigm of scientific innovations and concepts. Survival of patients with metastatic colorectal cancer (m-CRC) has been significantly improved with the introduction of the monoclonal antibodies that have as target the vascular endothelial growth factor (VEGF) and the epidermal growth factor receptor (EGFR). Novel agents such as aflibercept and regorafenib have recently been approved...
February 8, 2017: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/28174418/liver-cancer-regorafenib-as-second-line-therapy-in-hepatocellular-carcinoma
#6
Austin G Duffy, Tim F Greten
No abstract text is available yet for this article.
March 2017: Nature Reviews. Gastroenterology & Hepatology
https://www.readbyqxmd.com/read/28174379/-investigation-of-administration-technique-of-regorafenib-in-our-center
#7
Chu Matsuda, Katsuki Danno, Susumu Miyazaki, Kazumasa Fujitani, Masaru Kubota, Masaaki Motoori, Rie Nakatsuka, Masashige Nishimura, Akihiro Kitagawa, Mari Takagi, Kazuhiro Iwase
Regorafenib is an oral multikinase inhibitor; the CORRECTtrial evaluated its efficacy in patients with metastatic colorectal cancer following disease progression with standard therapies. However, regorafenib has toxicities that develop quickly. Few studies have reported the safe dose and usage of regorafenib to avoid these adverse events in Japanese patients. We examined the side effects and safe administration technique of regorafenib in this study. We administered regorafenib to 15 patients with metastatic colorectal cancer following disease progression with standard therapies...
January 2017: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/28166200/upregulation-of-marcks-in-kidney-cancer-and-its-potential-as-a-therapeutic-target
#8
C-H Chen, L W R Fong, E Yu, R Wu, J F Trott, R H Weiss
Targeted therapeutics, such as those abrogating hypoxia inducible factor (HIF)/vascular endothelial growth factor signaling, are initially effective against kidney cancer (or renal cell carcinoma, RCC); however, drug resistance frequently occurs via subsequent activation of alternative pathways. Through genome-scale integrated analysis of the HIF-α network, we identified the major protein kinase C substrate MARCKS (myristoylated alanine-rich C kinase substrate) as a potential target molecule for kidney cancer...
February 6, 2017: Oncogene
https://www.readbyqxmd.com/read/28157071/association-between-and-polymorphisms-and-adverse-drug-reactions-to-regorafenib-a-preliminary-study%C3%A2
#9
Akimitsu Maeda, Hitoshi Ando, Takashi Ura, Azusa Komori, Ayako Hasegawa, Hiroya Taniguchi, Shigenori Kadowaki, Kei Muro, Masahiro Tajika, Makiko Kobara, Masahide Matsuzaki, Naoya Hashimoto, Mieko Maeda, Yasushi Kojima, Masahiro Aoki, Eisaku Kondo, Akiyoshi Mizutani, Akio Fujimura
OBJECTIVE: Due to the occurrence of severe adverse drug reactions to regorafenib, a drug used in cancer therapy, the identification of a predictive marker(s) is needed to increase the therapeutic applicability of this compound. We therefore investigated whether polymorphisms in the ABCG2 and SLCO1B genes are associated with adverse drug reactions to regorafenib. METHODS: For these analyses, 37 Japanese cancer patients were treated with regorafenib, genotyped for polymorphisms in ABCG2 and SLCO1B, and evaluated for drug-related adverse drug reactions...
February 3, 2017: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28156651/oams-at-the-end-the-end-of-the-beginning-or-the-beginning-of-the-end
#10
Barbara Marie Galligan, Chintan Shah, Iris Chen Zhao, Brian Paciotti, Nathan Fairman, Quy Tran
: 229 Background: In 2001, after three months of review, the FDA approved the oral anticancer agent imatinib, making it the fastest approval in FDA history. Since then, the FDA has approved over 40 oral anti-cancer medications (OAMs) and the number continues to rise, transforming cancer care, improving survival in specific cancers and providing new hope. However, the rapid development of OAMs has produced uncertainty over the best use of these new medications, particularly at the end of life...
October 9, 2016: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28133332/-multidisciplinary-treatment-for-high-risk-gist-of-the-stomach
#11
Tomo Ishida, Shigeyuki Tamura, Atsushi Takeno, Kohei Murakami, Yohei Nose, Ryota Mori, Yasuo Oneda, Ryuichi Kuwahara, Takuya Sakamoto, Atsushi Naito, Yoshiteru Katsura, Yoshiaki Ohmura, Yoshinori Kagawa, Yutaka Takeda, Takeshi Kato
A 59-year-old man underwent total gastrectomy(with D2 dissection)and cholecystectomy for gastric cancer and a submucosal tumor of the stomach. The specimen was immunohistochemically positive for c-kit, the Ki-67 label index was 10%, and the mitotic count was 20/HPF. Finally, the patient was diagnosed with high-risk gastrointestinal stromal cancer with normal type gastric cancer. After discharge from hospital, we started administration of TS-1 as adjuvant therapy for the gastric cancer. As multiple recurrences of the GIST in the abdomen developed, the patient underwent 3 radical local resections...
November 2016: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/28133322/-long-term-survival-of-a-patient-with-recurrent-duodenal-gist-treated-with-various-molecular-targeted-drugs-and-tae-a-case-report
#12
Hikari Chidimatsu, Hiroto Matsui, Michihisa Iida, Shinsuke Kanekiyo, Yukio Tokumitsu, Yoshihiro Tokuhisa, Kazuhiko Sakamoto, Nobuaki Suzuki, Shigeru Takeda, Tomio Ueno, Shigeru Yamamoto, Shigefumi Yoshino, Shoichi Hazama, Hiroaki Nagano
The patient was 66-year-old woman with anemia. A 6 cm GIST was diagnosed in the fourth portion of the duodenum using abdominal CT. Duodenal-jejunal segmental resection was performed for the GIST. Four years after surgery, multiple liver metastatic recurrences ofGIST were diagnosed using abdominal CT. The metastatic tumor was treated with imatinib, but the treatment caused adverse events such as leukocytopenia(Grade 2)and anemia(Grade 3). The treatment continued for 41 months while reduced or discontinued during the administration period...
November 2016: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/28133314/-a-case-of-metastatic-lung-cancer-from-colon-cancer-with-a-long-partial-response-with-regorafenib-treatment
#13
Yasuhito Iseki, Masakazu Yashiro, Masatsune Shibutani, Hisashi Nagahara, Kiyoshi Maeda, Shinji Matsutani, Tatsuro Tamura, Go Ohira, Sadaaki Yamazoe, Kenjiro Kimura, Takahiro Toyokawa, Ryosuke Amano, Hiroaki Tanaka, Kazuya Muguruma, Kosei Hirakawa, Masaichi Ohira
A 66-year-old woman underwent sigmoidectomy for colon cancer. The final diagnosis was early cancer of pT2 pN0 and M0 (fStage I ). A chest CT revealed lung metastasis and lymph node metastasis 6 years after surgery. The patient was treated sequentially with FOLFOX, FOLFIRI, and XELOX regimens. Since these regimens resulted in progressive disease, regorafenib was started as the fourth regimen. After 8 courses, she was evaluated as having a partial response. Her partial response has continued for 18 months of regorafenib treatment...
November 2016: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/28133304/-a-case-of-metastatic-colorectal-cancer-with-her2-overexpression-amplification
#14
Akio Matsumoto, Yoshifumi Shimada, Ryoma Yagi, Kohei Miura, Yosuke Tajima, Takuma Okamura, Masato Nakano, Hitoshi Kameyama, Hitoshi Nogami, Satoshi Maruyama, Yasumasa Takii, Hiroshi Ichikawa, Jun Sakata, Takashi Kobayashi, Toshifumi Wakai
We report a case of panitumumab-resistant rectal cancer with HER2 gene amplification detected by CancerPlex®. A 51- year-old man was diagnosed with an obstructive rectal cancer having lung and adrenal metastases. He underwent the Hartmann 's operation, and KRAS mutations were not detected. After the surgery, 3 courses of CapeOx plus bevacizumab were administered as first-line chemotherapy; however, the lung and adrenal metastases progressed. Subsequently, 24 courses of IRIS/panitumumab was administered as second-line chemotherapy, and the metastases slowly progressed...
November 2016: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/28123730/pseudocirrhosis-caused-by-regorafenib-in-an-advanced-rectal-cancer-patient-with-multiple-liver-metastases
#15
Kensuke Kumamoto, Shungo Endo, Noriyuki Isohata, Azuma Nirei, Daiki Nemoto, Kenichi Utano, Takuro Saito, Kazutomo Togashi
A 70-year-old man who was diagnosed with unresectable advanced rectal cancer with multiple liver metastases, received oxaliplatin-based treatment with bevacizumab as first-line chemotherapy and irinotecan-based treatment with bevacizumab as second-line chemotherapy for a total of 17 months. The patient was treated with regorafenib (160 mg/day for 3 weeks) as third-line chemotherapy. Following completion of one course of regorafenib treatment, the patient complained of abdominal distension. Computed tomography (CT) examination identified liver atrophy and massive ascites, while no such symptoms were observed prior to the regorafenib treatment...
January 2017: Molecular and Clinical Oncology
https://www.readbyqxmd.com/read/28105361/computed-tomograpy-evaluation-of-morphological-changes-clinical-response-and-survival-in-colorectal-cancer-liver-metastasis-treated-by-regorafenib-a-case-report
#16
Nobuhisa Matsuhashi, Takao Takahashi, Junko Kato, Toshiyuki Tanahashi, Satoshi Matsui, Yoshiyuki Sasaki, Hisashi Imai, Yoshihiro Tanaka, Naoki Okumura, Kazuya Yamaguchi, Manabu Futamura, Shinji Osada, Kazuhiro Yoshida
Pathological response to preoperative chemotherapy was recently found to be correlated with improved survival and has been proposed as a new outcome end-point following resection of liver metastases from colorectal cancer (CRC). It was demonstrated that, particularly after therapy with bevacizumab, CRC liver metastases decreased in size and underwent distinct morphological changes on computed tomography (CT). However, morphological changes in response to treatment with regorafenib have not yet been reported...
December 2016: Molecular and Clinical Oncology
https://www.readbyqxmd.com/read/28089507/gastrointestinal-perforation-and-fistula-formation-in-5-patients-with-colorectal-cancer-during-treatment-with-regorafenib
#17
Ayako Doi, Yasutoshi Kuboki, Kohei Shitara, Shota Fukuoka, Hideaki Bando, Wataru Okamoto, Takashi Kojima, Toshihiko Doi, Atsushi Ohtsu, Takayuki Yoshino
No abstract text is available yet for this article.
December 28, 2016: Clinical Colorectal Cancer
https://www.readbyqxmd.com/read/28065859/inhibition-of-human-udp-glucuronosyltransferase-enzymes-by-lapatinib-pazopanib-regorafenib-and-sorafenib-implications-for-hyperbilirubinemia
#18
John O Miners, Nuy Chau, Andrew Rowland, Kushari Burns, Ross A McKinnon, Peter I Mackenzie, Geoffrey T Tucker, Kathleen M Knights, Ganessan Kichenadasse
Kinase inhibitors (KIs) are a rapidly expanding class of drugs used primarily for the treatment of cancer. Data relating to the inhibition of UDP-glucuronosyltransferase (UGT) enzymes by KIs is sparse. However, lapatinib (LAP), pazopanib (PAZ), regorafenib (REG) and sorafenib (SOR) have been implicated in the development of hyperbilirubinemia in patients. This study aimed to characterise the role of UGT1A1 inhibition in hyperbilirubinemia and assess the broader potential of these drugs to perpetrate drug-drug interactions arising from UGT enzyme inhibition...
January 6, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28060884/contrast-enhanced-ultrasound-with-vegfr2-targeted-microbubbles-for-monitoring-regorafenib-therapy-effects-in-experimental-colorectal-adenocarcinomas-in-rats-with-dce-mri-and-immunohistochemical-validation
#19
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
OBJECTIVES: To investigate contrast-enhanced ultrasound (CEUS) with VEGFR2-targeted microbubbles for monitoring therapy effects of regorafenib on experimental colon carcinomas in rats with correlation to dynamic contrast-enhanced MRI (DCE-MRI) and immunohistochemistry. MATERIALS AND METHODS: Human colorectal adenocarcinoma xenografts (HT-29) were implanted subcutaneously in n = 21 (n = 11 therapy group; n = 10 control group) female athymic nude rats (Hsd: RH-Foxn1rnu)...
2017: PloS One
https://www.readbyqxmd.com/read/28052652/anti-angiogenic-therapy-in-patients-with-advanced-gastric-and-gastroesophageal-junction-cancer-a-systematic-review
#20
Li-Tzong Chen, Do-Youn Oh, Min-Hee Ryu, Kun-Huei Yeh, Winnie Yeo, Roberto Carlesi, Rebecca Cheng, Jongseok Kim, Mauro Orlando, Yoon-Koo Kang
Despite advancements in therapy for advanced gastric and gastroesophageal junction cancers, their prognosis remains dismal. Tumor angiogenesis plays a key role in cancer growth and metastasis, and recent studies indicate that pharmacologic blockade of angiogenesis is a promising approach to therapy. In this systematic review, we summarize current literature on the clinical benefit of anti-angiogenic agents in advanced gastric cancer. We conducted a systematic search of PubMed and conference proceedings including the American Society of Clinical Oncology, the European Society for Medical Oncology, and the European Cancer Congress...
January 3, 2017: Cancer Research and Treatment: Official Journal of Korean Cancer Association
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