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Nilotinib

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https://www.readbyqxmd.com/read/28643375/dried-blood-spot-sampling-of-nilotinib-in-patients-with-chronic-myeloid-leukaemia-a-comparison-with-venous-blood-sampling
#1
Christel C L M Boons, Abdel Chahbouni, Anneliene M Schimmel, Abraham J Wilhelm, Yvonne M den Hartog, Jeroen J W M Janssen, N Harry Hendrikse, Jacqueline G Hugtenburg, Eleonora L Swart
OBJECTIVES: To compare nilotinib concentrations obtained by venous blood sampling and dried blood spot (DBS) in patients with chronic myeloid leukaemia (CML). It was investigated how to predict nilotinib plasma levels on the basis of DBS. METHODS: Forty duplicate DBS and venous blood samples were collected from 20 patients. Capillary blood was obtained by finger prick and spotted on DMPK-C Whatman sampling paper, simultaneously with venous blood sampling. Plasma concentrations were predicted from DBS concentrations using three methods: (1) individual and (2) mean haematocrit correction and (3) the bias between plasma and DBS concentrations...
June 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28626381/nilotinib-induced-acute-pancreatitis-in-a-patient-with-chronic-myeloid-leukemia
#2
Vihang Patel, Anil Pattisapu, Karim Attia, John Weiss
Nilotinib, a second-generation tyrosine kinase inhibitor, is used for treatment of chronic myeloid leukemia (CML); it has been widely used especially for imatinib-resistant CML. Despite being a novel drug in this therapeutic class, it has the potential to be harmful. We present the case of an elderly woman who developed life-threatening acute pancreatitis as an adverse event after having started the drug. There is only one reported case in the literature of nilotinib-induced acute pancreatitis. The purpose of this case report is to educate physicians who prescribe this medication to be aware of potential life-threatening adverse events...
May 2017: Case Reports in Gastroenterology
https://www.readbyqxmd.com/read/28623111/reversal-of-abcb1-mediated-efflux-by-imatinib-and-nilotinib-in-cells-expressing-various-transporter-levels
#3
Petr Mlejnek, Petr Kosztyu, Petr Dolezel, Susan E Bates, Eliska Ruzickova
Recently, it has been suggested that imatinib (IM) and nilotinib (NIL) could be studied beyond their original application, as inhibitors of the drug efflux pump ABCB1 (P-glycoprotein, MDR1). Since the reversal of ABCB1-mediated resistance has never been successfully demonstrated in the clinic, we addressed the question of whether IM and NIL may actually serve as efficient inhibitors of ABCB1. Here we define an efficient inhibitor as a compound that achieves full (90-100%) reversal of drug efflux at a concentration that does not exhibit significant off-target toxicity in vitro...
June 13, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28601294/the-c-abl-inhibitor-nilotinib-as-a-potential-therapeutic-agent-for-chronic-cerebellar-ataxia
#4
Woo-Jin Lee, Jangsup Moon, Tae-Joon Kim, Jin-Sun Jun, Han Sang Lee, Young Jin Ryu, Soon-Tae Lee, Keun-Hwa Jung, Kyung-Il Park, Ki-Young Jung, Manho Kim, Sang Kun Lee, Kon Chu
Nilotinib is a potent inhibitor of tyrosine kinase BCR-ABL that penetrates the blood-brain barrier. To evaluate the effect of nilotinib in chronic cerebellar ataxia, twelve patients with chronic cerebellar ataxia nonresponsive to other treatment options (modified Rankin scale [mRS] scores: >2) and received nilotinib therapy (daily doses: 150-300mg) for >4 (range 5-16) weeks were reviewed. At follow-up, improved mRS scores were found in 7/12 (58.3%) patients and favorable mRS scores (≤2) were found in 6/12 (50...
August 15, 2017: Journal of Neuroimmunology
https://www.readbyqxmd.com/read/28592197/cardiovascular-effects-of-the-addition-of-nilotinib-to-standard-therapy-for-acute-myeloid-leukemia
#5
Carolyn M Larsen, Hector R Villarraga, Kebede H Begna, Mark R Litzow, Aref Al-Kali, Joerg Herrmann
No abstract text is available yet for this article.
June 8, 2017: Leukemia & Lymphoma
https://www.readbyqxmd.com/read/28584790/ameliorative-effects-of-nilotinib-on-ccl4-induced-liver-fibrosis-via-attenuation-of-rage-hmgb1-gene-expression-and-oxidative-stress-in-rat
#6
Vahid Khanjarsim, Jamshid Karimi, Iraj Khodadadi, Adel Mohammadalipour, Mohammad Taghi Goodarzi, Ghasem Solgi, Mohammad Hashemnia
Nilotinib as a tyrosine kinase inhibitor has been recently used to improve the liver fibrosis process, but the exact mechanisms still require further clarification. In this study, we investigated the anti-fibrotic effects of Nilotinib via RAGE/HMGB1axis and antioxidant mechanisms. This experimental study was performed in the Hamadan University of Medical Sciences, Iran, from May 2015 to December 2016. Liver fibrosis was induced in Wistar male rats by CCL4. Rats were gavaged daily with Nilotinib (10 mg/kg). RAGE, HMGB1, TNF-α and TGF-β mRNA expression were evaluated by quantitative RT-PCR...
May 2017: Chonnam Medical Journal
https://www.readbyqxmd.com/read/28583043/intracranial-stenting-for-nilotinib-treatment-associated-cerebrovascular-stenosis-in-chronic-myeloid-leukemia
#7
Tomohiko Ozaki, Hajime Nakamura, Nobuyuki Izutsu, Hiroaki Masaie, Jun Ishikawa, Manabu Kinoshita
One of the second-generation tyrosine kinase inhibitors (TKIs), nilotinib, is increasingly used for imatinib-resistant or intolerant chronic myeloid leukemia (CML). Nilotinib is considered well tolerated with few side effects including hyperglycemia, hyperbilirubinemia and elevated levels of pancreatic enzymes. However, there is growing evidence that nilotinib accelerates atherosclerosis and causes peripheral arterial occlusive disease such as stroke, transient ischemic attack (TIA) and cardiovascular diseases...
January 1, 2017: Interventional Neuroradiology
https://www.readbyqxmd.com/read/28566209/de-escalation-of-tyrosine-kinase-inhibitor-dose-in-patients-with-chronic-myeloid-leukaemia-with-stable-major-molecular-response-destiny-an-interim-analysis-of-a-non-randomised-phase-2-trial
#8
Richard E Clark, Fotios Polydoros, Jane F Apperley, Dragana Milojkovic, Christopher Pocock, Graeme Smith, Jenny L Byrne, Hugues de Lavallade, Stephen G O'Brien, Tony Coffey, Letizia Foroni, Mhairi Copland
BACKGROUND: Discontinuation of tyrosine kinase inhibitor (TKI) therapy is feasible for some patients with chronic myeloid leukaemia with deep molecular responses; however, patients with stable major molecular response (MMR), but not MR4, have not been studied, nor has the effect of treatment de-escalation rather than outright cessation. We aimed to examine the effects of treatment de-escalation as a prelude to complete cessation, not only in patients with MR4 or greater, but also in those with MMR but not MR4...
May 26, 2017: Lancet Haematology
https://www.readbyqxmd.com/read/28557248/ponatinib-induced-widespread-ichthyosiform-eruption
#9
F Derlino, S Barruscotti, P Zappasodi, V Brazzelli, C Vassallo
Ponatinib is a new potent third-generation tyrosine kinase inhibitor (TKI), developed for the treatment of chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphocytic leukaemia (ALL) resistant to first (imatinib) and second generation (dasatinib and nilotinib) TK-inhibitors. Aimed at wild type and mutant BCR-ABL, ponatinib demonstrates significant anti-leukemic activity and holds much promise in treating other malignancies, including gastrointestinal stromal tumors (GIST)(1;2). This article is protected by copyright...
May 30, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
https://www.readbyqxmd.com/read/28551768/an-analysis-of-the-kinetics-of-molecular-response-during-the-first-trimester-of-treatment-with-nilotinib-in-newly-diagnosed-chronic-myeloid-leukemia-patients-in-chronic-phase
#10
Juan Luis Steegmann, Dolors Colomer, Maria-Teresa Gómez-Casares, Valentín García-Gutiérrez, Guillermo Ortí, Angel Ramírez-Payer, Eduardo Olavarria, Ferrán Vall-Llovera, Pilar Giraldo, Eulogio Conde, Rolando Vallansot, Jose Luis López-Lorenzo, Luis Palomera, Alberto Álvarez-Larrán, Venancio Conesa, Guiomar Bautista, Laura Casas, Frank Giles, Andreas Hochhaus, Luis Felipe Casado-Montero
PURPOSE: This study was aimed to analyze the association of very early molecular response to nilotinib with the achievement of deep molecular response (MR4) at 18 months. We hypothesized that the BCR-ABL1 levels during the first 3 months of therapy, and the kinetics of their descent in this period, could be predictive of deep molecular response thereafter. METHODS: This substudy of the ENEST1st trial included 60 patients with chronic myeloid leukemia in chronic phase treated with front-line nilotinib, and BCR-ABL1IS levels were measured using GUS as the control gene...
May 27, 2017: Journal of Cancer Research and Clinical Oncology
https://www.readbyqxmd.com/read/28551620/impact-of-small-molecules-on-%C3%AE-catenin-and-e-cadherin-expression-in-hpv16-positive-and-negative-squamous-cell-carcinomas
#11
Benedikt Kramer, Clemens Hock, Johannes David Schultz, Anne Lammert, Beatrice Kuhlin, Richard Birk, Karl Hörmann, Christoph Aderhold
BACKGROUND: The validation of potential molecular targets in head and neck squamous cell carcinoma (SCC) is mandatory. β-Catenin and E-cadherin are crucial for cancer progression through epithelial-mesenchymal transition. We analyzed the effect of the tyrosine kinase inhibitors nilotinib, dasatinib, erlotinib and gefitinib on β-catenin and E-cadherin expression in SCC with respect to human papillomavirus (HPV) status. MATERIALS AND METHODS: Expression of β-catenin and E-cadherin in cell lines UMSCC 11A, UMSCC 14C and CERV196 under the influence of tyrosine kinase inhibitors were analyzed by enzyme-linked immunosorbent assay...
June 2017: Anticancer Research
https://www.readbyqxmd.com/read/28549238/risk-factors-and-mechanisms-contributing-to-tki-induced-vascular-events-in-patients-with-cml
#12
REVIEW
Peter Valent, Emir Hadzijusufovic, Gregor Hoermann, Wolfgang Füreder, Gerit-Holger Schernthaner, Wolfgang R Sperr, Rudolf Kirchmair, Dominik Wolf
Vascular adverse events (VAE) are an emerging problem in patients with chronic myeloid leukemia (CML) receiving second-generation BCR-ABL1 tyrosine kinase inhibitors (TKI). Relevant VAE comprise peripheral, cerebral, and coronary artery changes in patients receiving nilotinib, venous and arterial occlusive events during ponatinib therapy, and pulmonary hypertension in patients receiving dasatinib. Although each TKI binds to a unique profile of molecular targets in leukemic cells and vascular cells, the exact etiology of drug-induced vasculopathies remains uncertain...
May 12, 2017: Leukemia Research
https://www.readbyqxmd.com/read/28531278/cardiovascular-toxic-effects-of-targeted-cancer-therapy
#13
Kazuko Tajiri, Kazutaka Aonuma, Ikuo Sekine
Over the past decade, there has been a major shift in chemotherapy from non-specific cytotoxic drugs to molecular targeted drug therapies. As more molecular targeted therapies are developed, new types of cardiovascular toxicities induced by targeted therapies are a growing problem. Cardiotoxicity induced by the human epidermal growth factor receptor-2 inhibitor trastuzumab manifests as decreased left ventricular ejection fraction. In contrast to anthracycline treatment, most cardiac events occur during trastuzumab treatment, but are reversed quickly when treatment is interrupted and cardiac intervention is established...
May 20, 2017: Japanese Journal of Clinical Oncology
https://www.readbyqxmd.com/read/28522574/single-cell-immune-profiling-by-mass-cytometry-of-newly-diagnosed-chronic-phase-chronic-myeloid-leukaemia-treated-with-nilotinib
#14
Stein-Erik Gullaksen, Jørn Skavland, Sonia Gavasso, Vinko Tosevski, Krzysztof Warzocha, Claudia Dumrese, Augustin Ferrant, Tobias Gedde-Dahl, Andrzej Hellmann, Jeroen Janssen, Boris Labar, Alois Lang, Waleed Majeed, Georgi Mihaylov, Jesper Stentoft, Leif Stenke, Josef Thaler, Noortje Thielen, Gregor Verhoef, Jaroslava Voglova, Gert Ossenkoppele, Andreas Hochhaus, Henrik Hjorth-Hansen, Satu Mustjoki, Sieghart Sopper, Francis Giles, Kimmo Porkka, Dominik Wolf, Bjørn Tore Gjertsen
Monitoring of single cell signal transduction in leukemic cellular subsets has been proposed to provide deeper understanding of disease biology and prognostication, but has so far not been tested in a clinical trial of targeted therapy. We developed a complete mass cytometry analysis pipeline for characterization of intracellular signal transduction patterns in the major leukocyte subsets of chronic phase chronic myeloid leukaemia. Changes in phosphorylated Bcr-Abl1 and its involved signalling pathways were readily identifiable in peripheral blood single cells already within 3 hours of per oral nilotinib dosing...
May 18, 2017: Haematologica
https://www.readbyqxmd.com/read/28521433/effect-of-selective-small-molecule-inhibitors-on-mmp-9-and-vegfr-1-expression-in-p16-positive-and-negative-squamous-cell-carcinoma
#15
Benedikt Kramer, Johannes David Schultz, Clemens Hock, Alexander Sauter, Boris A Stuck, Karl Hörmann, Richard Birk, Christoph Aderhold
The identification of molecular targets in the therapy of human papilloma virus (HPV)-associated head and neck squamous cell carcinoma (HNSCC) is a primary aim of cancer research. Matrix metalloproteinase 9 (MMP-9) and vascular endothelial growth factor receptor (VEGFR) have important roles in the development of HNSCC. The tyrosine kinase inhibitors, nilotinib, dasatinib, erlotinib and gefitinib are well established in the targeted therapy of tumors other than HNSCC. The present study aimed to investigate the alteration of MMP-9 and VEGFR-1 expression patterns following treatment with these tyrosine kinase inhibitors in p16-positive and -negative squamous carcinoma cells...
May 2017: Oncology Letters
https://www.readbyqxmd.com/read/28508322/use-patterns-of-first-line-inhibitors-of-tyrosine-kinase-and-time-to-change-to-second-line-therapy-in-chronic-myeloid-leukemia
#16
Jorge Enrique Machado-Alba, Manuel Enrique Machado-Duque
Background Chronic myeloid leukemia (CML) has a low incidence but a high burden of disease, and is treated with high-cost tyrosine kinase inhibitors (TKI). Objective To determine the time from the start of a first-line TKI until it passes to second-line, and to establish the reasons for the change of therapy time. Setting Patients with Philadelphia-positive CML treated with some TKI. Methods Retrospective cohort study, between January 1 2007 and July 31 2015, with information obtained from medical records, the time to change initial drugs to secondline therapy, and the reasons for change, were identified...
May 15, 2017: International Journal of Clinical Pharmacy
https://www.readbyqxmd.com/read/28501737/the-bcr-abl-tyrosine-kinase-inhibitor-nilotinib-stimulates-expression-of-il-1%C3%AE-in-vascular-endothelium-in-association-with-downregulation-of-mir-3p
#17
Masumi Sukegawa, Xiangmin Wang, Chie Nishioka, Bin Pan, Kailin Xu, Hiroshi Ohkawara, Yoichi Hamasaki, Masayuki Mita, Kenichi Nakamura, Masatoshi Okamoto, Hiromi Shimura, Masatsugu Ohta, Takayuki Ikezoe
BCR/ABL tyrosine kinase inhibitors (TKIs) have significantly improved the prognosis for in dividuals with chronic myeloid leukemia (CML). However, many patients treated with TKIs suffer from TKI-related complications. In particular, vascular events such as peripheral artery occlusive disease have become aserious clinical problem for patients who receive the TKI, nilotinib. At present, the molecular mechanisms by which TKIs cause vascular endothelial cell insults remain unknown.This study explored the effects of the TKIs, imatinib, nilotinib and dasatinib, on vascular endothelial cells in vitro, and found that only nilotinib induced expression of interleukin-1β (IL-1β) by vascular endothelial cells...
July 2017: Leukemia Research
https://www.readbyqxmd.com/read/28490048/simultaneous-determination-of-imatinib-dasatinib-and-nilotinib-by-liquid-chromatography-tandem-mass-spectrometry-and-its-application-to-therapeutic-drug-monitoring
#18
Aneta Wojnicz, Beatriz Colom-Fernández, Juan L Steegmann, Cecilia Muñoz-Calleja, Francisco Abad-Santos, Ana Ruiz-Nuño
BACKGROUND: Imatinib, dasatinib, and nilotinib are tyrosine kinase inhibitors (TKIs) used as first-line treatment of chronic myeloid leukemia. Therapeutic drug monitoring is important to achieve treatment efficacy in the case of imatinib and nilotinib, and to control toxicity in the case of dasatinib. New high-sensitivity methods to monitor those drugs are needed, especially for dasatinib. Thus, a simple method to determine plasma levels of imatinib, dasatinib, and nilotinib for application in clinical practice was developed...
June 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/28484463/immune-effector-recovery-in-chronic-myeloid-leukemia-and-treatment-free-remission
#19
REVIEW
Amy Hughes, Agnes S M Yong
Chronic myeloid leukemia (CML) is a hematological cancer, characterized by a reciprocal chromosomal translocation between chromosomes 9 and 22 [t(9;22)], producing the Bcr-Abl oncogene. Tyrosine kinase inhibitors (TKIs) represent the standard of care for CML patients and exert a dual mode of action: direct oncokinase inhibition and restoration of effector-mediated immune surveillance, which is rendered dysfunctional in CML patients at diagnosis, prior to TKI therapy. TKIs such as imatinib, and more potent second-generation nilotinib and dasatinib induce a high rate of deep molecular response (DMR, BCR-ABL1 ≤ 0...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28475010/computational-analysis-of-abl-kinase-mutations-allows-predicting-drug-sensitivity-against-selective-kinase-inhibitors
#20
Swapna Kamasani, Sravani Akula, Sree Kanth Sivan, Vijjulatha Manga, Justus Duyster, Dashavantha Reddy Vudem, Rama Krishna Kancha
The ABL kinase inhibitor imatinib has been used as front-line therapy for Philadelphia-positive chronic myeloid leukemia. However, a significant proportion of imatinib-treated patients relapse due to occurrence of mutations in the ABL kinase domain. Although inhibitor sensitivity for a set of mutations was reported, the role of less frequent ABL kinase mutations in drug sensitivity/resistance is not known. Moreover, recent reports indicate distinct resistance profiles for second-generation ABL inhibitors. We thus employed a computational approach to predict drug sensitivity of 234 point mutations that were reported in chronic myeloid leukemia patients...
May 2017: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
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