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https://www.readbyqxmd.com/read/29220734/high-throughput-routine-determination-of-17-tyrosine-kinase-inhibitors-by-lc-ms-ms
#1
Camille Merienne, Marine Rousset, Dominique Ducint, Nadège Castaing, Karine Titier, Mathieu Molimard, Stéphane Bouchet
Several studies have shown that therapeutic drug monitoring of tyrosine kinase inhibitors (TKI) can improve their benefit in cancer. An analytical tool has been developed in order to quantify 17 tyrosine kinase inhibitors and 2 metabolites in human plasma (afatinib, axitinib, bosutinib, crizotinib, dabrafenib, dasatinib, erlotinib, gefitinib, imatinib, lapatinib, nilotinib, ponatinib, regorafenib, regorafenib M2, regorafenib M5, ruxolitinib, sorafenib, sunitinib, vandetanib). Drugs were arranged in four groups, according to their plasma concentration range: 0...
November 28, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29220298/gastrointestinal-stromal-tumors
#2
Margaret von Mehren, Heikki Joensuu
GI stromal tumors (GISTs) are neoplasms with a varying malignancy potential ranging from virtually indolent tumors to rapidly progressing cancers. GISTs occur throughout the intestinal tract, and most harbor an activating mutation in either KIT or platelet-derived growth factor A ( PDGFRA). Diagnosis is made using immunohistochemistry, but molecular testing with mutation analysis is paramount for selection of appropriate therapy. Most small GISTs are cured with surgery. Tyrosine kinase inhibitor (TKI) therapy has led to substantial improvements in survival, both for patients with localized GIST and those with advanced disease...
December 8, 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/29212191/incidence-and-risk-of-hematologic-toxicities-in-cancer-patients-treated-with-regorafenib
#3
Bin Zhao, Hong Zhao
Regorafenib, an oral vascular endothelial growth factor receptor tyrosine-kinase inhibitor, has been approved for the treatment of several malignancies. As a non-traditional cytotoxic chemotherapeutic agent, regorafenib is often associated with hematologic toxicities. Here we searched PubMed and Embase up to June 2017 for relevant clinical trials. Eligible studies include trials in which subjects treated with 160 mg of regorafenib daily during the first 21 days of each 28-day cycle, and adequate safety data profile reporting thrombocytopenia, anemia, neutropenia and leucopenia...
November 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/29211816/clinical-outcome-and-molecular-characterisation-of-chemorefractory-metastatic-colorectal-cancer-patients-with-long-term-efficacy-of-regorafenib-treatment
#4
Erika Martinelli, Vincenzo Sforza, Claudia Cardone, Anna Capasso, Anna Nappi, Giulia Martini, Stefania Napolitano, Anna Maria Rachiglio, Nicola Normanno, Salvatore Cappabianca, Alfonso Reginelli, Maurizio Di Bisceglie, Tiziana Pia Latiano, Evaristo Maiello, Michele Orditura, Fernando De Vita, Floriana Morgillo, Fortunato Ciardiello, Teresa Troiani
HASH(0x524df90) Background: To investigate the potential predictors of response to regorafenib, in chemorefractory metastatic colorectal cancer (mCRC) patients with long-term efficacy from regorafenib treatment. Methods: Retrospective, single institution analysis of patients with chemorefractory mCRC treated with regorafenib, in clinical practice setting. 123 patients were treated and stratified into two groups according to number of cycles received (<7 and ≥7)...
2017: ESMO Open
https://www.readbyqxmd.com/read/29192124/drugs-and-scaffold-that-inhibit-cytochrome-p450-27a1-cyp27a1-in-vitro-and-in-vivo
#5
Morrie Lam, Natalia Mast, Irina Pikuleva
Cytochrome P450 27A1 (CYP27A1) is a ubiquitous enzyme that hydroxylates cholesterol and other sterols. Complete CYP27A1 deficiency due to genetic mutations is detrimental to human health, whereas 50% of activity retention is not and does not affect the whole body cholesterol levels. CYP27A1 is considered as a potential therapeutic target in breast cancer and age-related neurodegenerative diseases; however CYP27A1 inhibition should be 50%. Herein, 131 pharmaceuticals were tested for their effect on CYP27A1-mediated cholesterol 27-hydroxylation by in vitro enzyme assay...
November 30, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29188322/mass-balance-metabolic-disposition-and-pharmacokinetics-of-a-single-oral-dose-of-regorafenib-in-healthy-human-subjects
#6
Michael Gerisch, Frank-Thorsten Hafner, Dieter Lang, Martin Radtke, Konstanze Diefenbach, Adriaan Cleton, John Lettieri
PURPOSE: To evaluate the mass balance, metabolic disposition, and pharmacokinetics of a single dose of regorafenib in healthy volunteers. In addition, in vitro metabolism of regorafenib in human hepatocytes was investigated. METHODS: Four healthy male subjects received one 120 mg oral dose of regorafenib containing approximately 100 µCi (3.7 MBq) [14C]regorafenib. Plasma concentrations of parent drug were derived from HPLC-MS/MS analysis and total radioactivity from liquid scintillation counting (LSC)...
November 29, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/29184856/optimal-therapy-for-patients-with-hepatocellular-carcinoma-and-resistance-or-intolerance-to-sorafenib-challenges-and-solutions
#7
REVIEW
Emily M Ray, Hanna K Sanoff
The only US Food and Drug Administration (FDA)-approved first-line systemic therapy for hepatocellular carcinoma (HCC) is sorafenib; however, resistance or intolerance to sorafenib is unfortunately common. In this review, we briefly describe systemic therapies that can be considered for patients with HCC who show resistance or intolerance to sorafenib. For all patients with HCC who need systemic therapy, we strongly advocate for participation in clinical trials. Cytotoxic chemotherapy plays a minor role in the treatment of advanced HCC, with some data supporting the use of FOLFOX (infusional fluorouracil, leucovorin, and oxaliplatin) and GEMOX (gemcitabine-oxaliplatin)...
2017: Journal of Hepatocellular Carcinoma
https://www.readbyqxmd.com/read/29182165/me-too-drugs-with-limited-benefits-the-tale-of-regorafenib-for-hcc
#8
Bishal Gyawali, Vinay Prasad
This corrects the article DOI: 10.1038/nrclinonc.2017.100.
November 28, 2017: Nature Reviews. Clinical Oncology
https://www.readbyqxmd.com/read/29175677/efficacy-and-safety-of-regorafenib-in-the-treatment-of-metastatic-colorectal-cancer-a-systematic-review
#9
REVIEW
Maria Røed Skårderud, Anne Polk, Kirsten Kjeldgaard Vistisen, Finn Ole Larsen, Dorte Lisbet Nielsen
PURPOSE: Despite advances in the treatment of colorectal cancer, third-line treatment options are still limited. Regorafenib was approved in 2012 for the treatment of patients with metastatic colorectal cancer previously treated with approved standard therapy. The purpose of this review is to present existing clinical data on regorafenib. METHOD: We systematically searched the PubMed and Embase databases, as well as ASCO and ESMO conference abstracts, for studies in English including ≥30 patients, evaluating the efficacy and safety of regorafenib in patients with metastatic colorectal cancer...
November 10, 2017: Cancer Treatment Reviews
https://www.readbyqxmd.com/read/29174481/a-comparison-of-regorafenib-and-tas-102-for-metastatic-colorectal-cancer-a-systematic-review-and-network-meta-analysis
#10
Ana B K Abrahao, Yoo-Joung Ko, Scott Berry, Kelvin K W Chan
BACKGROUND: Regorafenib and TAS-102 have shown to be superior to placebo in refractory metastatic colorectal cancer. However, no studies have directly compared both drugs. Giving the lack of standard options in this scenario, a systematic review to compare the efficacy and safety of regorafenib and TAS-102 was performed. MATERIALS AND METHODS: A systematic review using the PubMed, Medline, Embase, Scopus, and Cochrane databases to identify published and unpublished studies up to November 2015 for randomized controlled trials for patients with metastatic colorectal cancer, involving regorafenib or TAS-102, was performed...
November 21, 2017: Clinical Colorectal Cancer
https://www.readbyqxmd.com/read/29165815/development-and-validation-of-a-liquid-chromatography-tandem-mass-spectrometry-analytical-method-for-the-therapeutic-drug-monitoring-of-eight-novel-anticancer-drugs
#11
M Herbrink, N de Vries, H Rosing, A D R Huitema, B Nuijen, J H M Schellens, J H Beijnen
To support therapeutic drug monitoring (TDM) of patients with cancer, a fast and accurate method for simultaneous quantification of the registered anticancer drugs afatinib, axitinib, ceritinib, crizotinib, dabrafenib, enzalutamide, regorafenib and trametinib in human plasma using liquid chromatography tandem mass spectrometry was developed and validated. Human plasma samples were collected from treated patients and stored at -20 (o) C. Analytes and internal standards (stable isotopically labeled analytes) were extracted with acetonitrile...
November 22, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29137408/incidence-and-risk-of-regorafenib-induced-hepatotoxicity
#12
Bin Zhao, Hong Zhao
Regorafenib, an oral multi-kinase inhibitor, has been approved for the treatments of several malignancies. Unlike traditional cytotoxic chemotherapeutic agents, regorafenib therapy often induces a distinct profile of adverse events (AEs) including hepatotoxicity. Here we conducted an up-to-date meta-analysis to assess the incidence and risk of regorafenib related hepatic toxicities. PubMed and Embase database were reviewed from inception to June 2017 for relevant trials. Eligible studies include subjects with solid tumors treated with 160 mg of regorafenib daily during the first three week of each four-week cycle, and adequate safety data reporting the elevation of aspartate transaminase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP) and bilirubin...
October 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/29137323/nvp-bkm120-inhibits-colon-cancer-growth-via-foxo3a-dependent-puma-induction
#13
Shida Yang, Xin Li, Wenchang Guan, Mingqin Qian, Zhicheng Yao, Xiaoxue Yin, Hongmei Zhao
NVP-BKM120, a potent and highly selective PI3K inhibitor, is currently being investigated in phase I/II clinical trials. The mechanisms of action of NVP-BKM120 in colon cancer cells are unclear. In the present study, we investigated how NVP-BKM120 suppresses colon cancer cells growth and potentiates effects of other chemotherapeutic drugs. We found that NVP-BKM120 treatment enhance PUMA induction irrespective of p53 status through the FoxO3a pathway following AKT inhibition. Furthermore, PUMA is required for NVP-BKM120-induced apoptosis in colon cancer cells...
October 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/29132204/complete-cure-of-advanced-hepatocellular-carcinoma-with-right-adrenal-gland-metastasis-and-portal-vein-thrombosis-by-multiple-applications-of-an-interdisciplinary-therapy-case-report-with-8-year-follow-up
#14
Hojung Jung, Byung Ik Km, Yong Kyun Cho, Woo Kyu Jeon, Hong Joo Kim, Hyun Pyo Hong
Hepatocellular carcinoma (HCC) is the sixth most common cause of death worldwide and the main cause of primary liver cancer. The principle problem of HCC is the poor prognosis, since advanced HCC reportedly has a median survival of only 9 months. The standard therapies are sorafenib and regorafenib, but the outcomes remain unclear. We report a 60-year-old man with advanced HCC with right adrenal gland metastasis and portal vein tumor thrombosis, who showed a complete response to multiple applications of an interdisciplinary therapy...
November 14, 2017: Clinical and Molecular Hepatology
https://www.readbyqxmd.com/read/29128510/enzymes-involved-in-tumor-driven-angiogenesis-a-valuable-target-for-anticancer-therapy
#15
REVIEW
Biagio Ricciuti, Jennifer Foglietta, Vanessa Bianconi, Amirhossein Sahebkar, Matteo Pirro
Angiogenesis plays a pivotal role in cancer progression and is required for tissue invasion and metastasis. Starting with Folkman's initial observations in 1971, basic research continued to shed new molecular insight into this multifaceted process, leading to the development of several anti-angiogenic drugs. To date, anti-vascular endothelial growth factor monoclonal antibodies, such as bevacizumab and ramucirumab, and receptor tyrosine kinase inhibitors (e.g., sorafenib, sunitinib, regorafenib and axitinib) have had a profound impact on the way we treat patients with advanced cancer, providing in some cases unprecedented clinical benefit...
November 8, 2017: Seminars in Cancer Biology
https://www.readbyqxmd.com/read/29110922/cost-effectiveness-of-trifluridine-tipiracil-for-previously-treated-metastatic-colorectal-cancer-in-england-and-wales
#16
Ash Bullement, Stuart Underhill, Ronan Fougeray, Anthony James Hatswell
BACKGROUND: Treatment options at third-line and beyond for patients with late-line metastatic colorectal cancer (mCRC) are limited, and outcomes are poor with best supportive care (BSC). This study investigated the cost-effectiveness of trifluridine/tipiracil and regorafenib relative to BSC alone in patients with mCRC who have been previously treated with, or are not considered candidates for, standard chemotherapies. MATERIALS AND METHODS: A partitioned survival model was constructed to assess the lifetime costs and benefits accrued by patients...
September 28, 2017: Clinical Colorectal Cancer
https://www.readbyqxmd.com/read/29100343/establishment-and-characterization-of-patient-derived-xenograft-models-of-gastrointestinal-stromal-tumor-resistant-to-standard-tyrosine-kinase-inhibitors
#17
Young-Soon Na, Min-Hee Ryu, Changhoon Yoo, Ju-Kyung Lee, Jung Min Park, Chae-Won Lee, Sun Young Lee, Young-Kyoung Shin, Ja-Lok Ku, Sung-Min Ahn, Yoon-Koo Kang
Gastrointestinal stromal tumors (GISTs) with KIT or platelet-derived growth factor receptor alpha (PDGFRa) oncogenic driver gene mutations, respond to tyrosine kinase inhibitors (TKIs) including imatinib, sunitinib, and regorafenib. However, most patients develop TKI resistance; therefore, novel agents are required. We established three TKI-resistant GIST patient-derived xenograft (PDX) models for effective drug development. These were PDX models harboring primary and secondary KIT and additional mutations; KIT exon 11 (p...
September 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/29074353/clinical-features-of-regorafenib-induced-liver-injury-in-japanese-patients-from-postmarketing-experience
#18
Hiroyuki Uetake, Kenichi Sugihara, Kei Muro, Toshiyuki Sunaya, Yuka Horiuchi-Yamamoto, Hajime Takikawa
BACKGROUND: Regorafenib (Stivarga) is an oral multikinase inhibitor currently approved for patients with metastatic colorectal cancer or gastrointestinal stromal tumor. Although hepatotoxicity has been a known product profile feature of regorafenib since its initial approval, its clinical features are limited to those found in the clinical trials. PATIENTS AND METHODS: The present study was conducted in 2 analysis sets: a safety analysis set for metastatic colorectal cancer from solicited postmarketing surveillance (PMS) in Japan (n = 1227) and an analysis set for serious hepatic adverse drug reactions (n = 210) from all patients registered for regorafenib use...
September 28, 2017: Clinical Colorectal Cancer
https://www.readbyqxmd.com/read/29072336/mechanisms-of-toxicity-associated-with-six-tyrosine-kinase-inhibitors-in-human-hepatocyte-cell-lines
#19
Cécile Mingard, Franziska Paech, Jamal Bouitbir, Stephan Krähenbühl
Tyrosine kinase inhibitors have revolutionized the treatment of certain cancers. They are usually well tolerated, but can cause adverse reactions including liver injury. Currently, mechanisms of hepatotoxicity associated with tyrosine kinase inhibitors are only partially clarified. We therefore aimed at investigating the toxicity of regorafenib, sorafenib, ponatinib, crizotinib, dasatinib and pazopanib on HepG2 and partially on HepaRG cells. Regorafenib and sorafenib strongly inhibited oxidative metabolism (measured by the Seahorse-XF24 analyzer) and glycolysis, decreased the mitochondrial membrane potential and induced apoptosis and/or necrosis of HepG2 cells at concentrations similar to steady-state plasma concentrations in humans...
October 26, 2017: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/29061771/a-systematic-review-and-meta-analysis-of-retrospective-series-of-regorafenib-for-treatment-of-metastatic-colorectal-cancer
#20
REVIEW
Joey Mercier, Ioannis A Voutsadakis
BACKGROUND: Metastatic colorectal cancer is a common disease encountered in oncology practice and treatment options beyond fluoropyrimidines, irinotecan, oxaliplatin and monoclonal antibodies against epidermal growth factor receptor and vascular endothelium growth factor (VEGF) are limited. Regorafenib, a new drug that targets tyrosine kinases such as VEGF receptor as well as others, has been added recently to the armamentarium for metastatic colorectal cancer. This report analyzes the published experience with this drug in clinical practice outside of clinical trials...
November 2017: Anticancer Research
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