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https://www.readbyqxmd.com/read/28531278/cardiovascular-toxic-effects-of-targeted-cancer-therapy
#1
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
#2
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
#3
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
#4
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
#5
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...
May 5, 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
#6
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
#7
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
#8
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
https://www.readbyqxmd.com/read/28469859/drug-interaction-between-tacrolimus-and-nilotinib-in-a-patient-with-chronic-myeloid-leukemia-after-renal-transplant
#9
Takashi Onaka, Naoto Takahashi, Masatomo Miura, Akihito Yonezawa
Nilotinib, a BCR-ABL tyrosine kinase inhibitor, is a known inhibitor of CYP3A4 and could increase the concentration of drugs metabolized by CYP3A4. An immunosuppressive drug for nilotinib-treated patients following transplant should be administered with careful pharmacokinetic monitoring because of its interaction with nilotinib.
May 2017: Clinical Case Reports
https://www.readbyqxmd.com/read/28467002/the-use-of-imatinib-resistance-mutation-analysis-to-direct-therapy-in-philadelphia-chromosome-bcr-abl1-positive-chronic-myeloid-leukaemia-patients-failing-imatinib-treatment-in-patan-hospital-nepal
#10
REVIEW
Gyan K Kayastha, Nora Ranjitkar, Radha Gurung, Raj Kumar Kc, Sanjit Karki, Roshan Shrestha, Piyush Rajbhandari, Raj K Thapa, Buddhi Poudyal, Paras Acharya, David J Roberts, Bruce Hayes, Mark Zimmerman, Buddha Basnyat
Philadelphia chromosome/BCR-ABL1 positive chronic myeloid leukaemia (CML) can be successfully treated with Glivec (Imatinib), which is available free of cost through the Glivec International Patient Assistance programme (GIPAP) to patients with proven CML without means to pay for the drug. We review the acquired mutations in the tyrosine kinase encoded by the BCR-ABL1 gene underlying Glivec failure or resistance in a cohort of 388 imatinib-treated CML patients (149 Female and 239 male) registered between February 2003 and June 2016 in Nepal...
May 3, 2017: British Journal of Haematology
https://www.readbyqxmd.com/read/28458002/in-silico-drug-repurposing-of-fda-approved-drugs-to-predict-new-inhibitors-for-drug-resistant-t315i-mutant-and-wild-type-bcr-abl1-a-virtual-screening-and-molecular-dynamics-study
#11
Farzin Sohraby, Milad Bagheri, Masoud Aliyar, Hassan Aryapour
The BCR-ABL fusion gene is one of the major causes of 95% of Chronic Myeloid Leukemia (CML). While, BCR-ABL protein is currently being used as a major target to treat CML. Although, current FDA-approved drugs such as; Imatinib and Nilotinib have stupendously improved the patients 5-year's survival rates, the drug resistance has dramatically reduced their effects. So, more accurate and effective alternative treatments are crucially needed. To address this issue, we screened the FDA-approved drugs by virtual screening and binding free energy calculations to identify new inhibitors for the wild-type and T315I gatekeeper mutant ABL1...
April 13, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28446463/the-national-cancer-institute-almanac-a-comprehensive-screening-resource-for-the-detection-of-anticancer-drug-pairs-with-enhanced-therapeutic-activity
#12
Susan L Holbeck, Richard Camalier, James A Crowell, Jeevan Prasaad Govindharajulu, Melinda G Hollingshead, Lawrence W Anderson, Eric C Polley, Larry Rubinstein, Apurva K Srivastava, Deborah F Wilsker, Jerry M Collins, James H Doroshow
To date, over 100 small molecule oncology drugs have been approved by the US Food and Drug Administration.  Due to the inherent heterogeneity of tumors, these small molecules are often administered in combination to prevent emergence of resistant cell subpopulations.  Therefore, new combination strategies to overcome drug resistance in patients with advanced cancer are needed.  In this study, we performed a systematic evaluation of the therapeutic activity of over 5,000 pairs of FDA-approved cancer drugs against a panel of 60 well-characterized human tumor cell lines (NCI-60) to uncover combinations with greater than additive growth-inhibitory activity...
April 26, 2017: Cancer Research
https://www.readbyqxmd.com/read/28446278/-clinical-analysis-for-42-imatinib-resistant-patients-with-chronic-myelogenous-leukemia
#13
Xi Liu, Si-Lin Gan, Jie Ma, Yan-Fang Liu, Xin-Sheng Xie, Zhong-Xing Jiang, Yuan-Dong Cheng, Hui Sun
OBJECTIVE: To analyze the kinase mutation ratio, related factors, effectiveness and safety of the second generation drugs for imatinib-resistant patients with chronic myeloid leukemia(CML). METHODS: COX proportional hazard regression model was used for unvariate and multvariate analysis of various factors affecting the kinase mutation and for evaluating the effectiveness and safety of second generation tyrosine kinase inhibitor(TKI). RESULTS: 13 kinds of mutation were detected in 19 out of 42 cases for 22 times, including 4 times of F359V, 3 times of E255K, 2 time for F359C, F317L, T315I, Y253H, 1 time for D256R, C250R, D276G, F486S, M244V, Y256H and G250E, 3 cases with mixed mutations...
April 2017: Zhongguo Shi Yan Xue Ye Xue za Zhi
https://www.readbyqxmd.com/read/28444644/ponatinib-in-japanese-patients-with-philadelphia-chromosome-positive-leukemia-a-phase-1-2-study
#14
Arinobu Tojo, Taiichi Kyo, Kazuhito Yamamoto, Hirohisa Nakamae, Naoto Takahashi, Yukio Kobayashi, Tetsuzo Tauchi, Shinichiro Okamoto, Koichi Miyamura, Kiyohiko Hatake, Hiromi Iwasaki, Itaru Matsumura, Noriko Usui, Tomoki Naoe, Meera Tugnait, Narayana I Narasimhan, Stephanie Lustgarten, Heinrich Farin, Frank Haluska, Kazuma Ohyashiki
In this ongoing Phase 1/2 study (NCT01667133), we evaluated ponatinib and assessed its recommended dose in Japanese patients with chronic myeloid leukemia (CML) resistant/intolerant to dasatinib or nilotinib, or with Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph(+)ALL) resistant/intolerant to ≥1 tyrosine kinase inhibitor (TKI). The primary endpoints were safety of the recommended dose (Phase 1) and major cytogenetic response (MCyR) by 12 months in chronic-phase CML (CP-CML) patients or major hematologic response (MaHR) by 6 months in patients with advanced phase disease (Phase 2)...
April 25, 2017: International Journal of Hematology
https://www.readbyqxmd.com/read/28444623/treatment-adherence-in-chronic-myeloid-leukaemia-patients-receiving-tyrosine-kinase-inhibitors
#15
Anna Rychter, Piotr Jerzmanowski, Adam Hołub, Zofia Specht-Szwoch, Violetta Kalinowska, Urszula Tęgowska, Ilona Seferyńska, Agnieszka Kołkowska-Leśniak, Ewa Lech-Marańda, Joanna Góra-Tybor
Failure to comply with treatment recommendations is very common in patients, but still poorly recognised by doctors. The current practice of using oral therapy on a large scale has been increasingly adopted for cancer patients. Chronic myeloid leukaemia (CML) is just such an example, where the introduction of taking new oral medications, the tyrosine kinase BCR-ABL inhibitors (TKI), has now revolutionised the treatment. The aim of our study was to assess treatment adherence in a group of Polish CML patients (a survey was conducted on 140 patient aged ≥18 years) treated with oral TKI (imatinib, dasatinib and nilotinib) taking into account the following variables: gender, age, education, place of residence, family circumstances and duration of therapy...
June 2017: Medical Oncology
https://www.readbyqxmd.com/read/28410286/successful-treatment-with-imatinib-after-nilotinib-and-ipilimumab-in-a-c-kit-mutated-advanced-melanoma-patient-a-case-report
#16
Carla Murer, Pascale Kränzlin-Stieger, Lars E French, Reinhard Dummer, Simone M Goldinger
Treatment of melanoma remains a challenge in advanced disease. Recently, the molecular differentiation in BRAF-mutated, NRAS-mutated and c-kit-mutated melanomas led to new treatment strategies. Different trials show that imatinib or nilotinib lead to meaningful responses in c-kit-mutated melanoma patients. There are little published data on sequential inhibition using these two drugs in melanoma. We describe the sequential use of imatinib after nilotinib in a c-kit-mutated melanoma patient, who progressed on interferon, Allovectin, dacarbazine, nilotinib and ipilimumab, and was finally treated with the c-kit inhibitor imatinib...
April 13, 2017: Melanoma Research
https://www.readbyqxmd.com/read/28397975/the-jak2-stat5-signaling-pathway-as-a-potential-therapeutic-target-in-canine-mastocytoma
#17
Alexandra Keller, Bettina Wingelhofer, Barbara Peter, Karin Bauer, Daniela Berger, Susanne Gamperl, Martin Reifinger, Sabine Cerny-Reiterer, Richard Moriggl, Michael Willmann, Peter Valent, Emir Hadzijusufovic
BACKGROUND: Mastocytoma are frequently diagnosed cutaneous neoplasms in dogs. In non-resectable mastocytoma patients, novel targeted drugs are often applied. The transcription factor STAT5 has been implicated in the survival of human neoplastic mast cells (MC). Our study evaluated the JAK2/STAT5 pathway as a novel target in canine mastocytoma. MATERIALS AND METHODS: We employed inhibitors of JAK2 (R763, TG101348, AZD1480, ruxolitinib) and STAT5 (pimozide, piceatannol) and evaluated their effects on 2 mastocytoma cell lines, C2 and NI-1...
April 11, 2017: Veterinary and Comparative Oncology
https://www.readbyqxmd.com/read/28390196/pi3k-isoform-inhibition-associated-with-anti-bcr-abl-drugs-shows-in-vitro-increased-anti-leukemic-activity-in-philadelphia-chromosome-positive-b-acute-lymphoblastic-leukemia-cell-lines
#18
Simona Ultimo, Carolina Simioni, Alberto M Martelli, Giorgio Zauli, Camilla Evangelisti, Claudio Celeghini, James A McCubrey, Giorgia Marisi, Paola Ulivi, Silvano Capitani, Luca M Neri
B-acute lymphoblastic leukemia (B-ALL) is a malignant disorder characterized by the abnormal proliferation of B-cell progenitors. Philadelphia chromosome-positive (Ph+) B-ALL is a subtype that expresses the Bcr-Abl fusion protein which represents a negative prognostic factor. Constitutive activation of the phosphatidylinositol 3-kinase/Akt/mammalian target of rapamycin (PI3K/Akt/mTOR) network is a common feature of B-ALL, influencing cell growth and survival. In the present study, we aimed to investigate the efficacy of PI3K isoform inhibition in B-ALL cell lines harboring the Bcr-Abl fusion protein...
April 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28378056/analysis-of-adverse-events-associated-with-dasatinib-and-nilotinib-treatments-in-chronic-phase-chronic-myeloid-leukemia-patients-outside-clinical-trials
#19
Koung Jin Suh, Ji Yun Lee, Dong-Yeop Shin, Youngil Koh, Soo-Mee Bang, Sung-Soo Yoon, Seonyang Park, Inho Kim, Jeong-Ok Lee
We analyzed adverse events (AEs) in 201 chronic phase CML patients treated with nilotinib (n = 120) or dasatinib (n = 81) as first- or second-line therapy. The dasatinib group had significantly higher grade 3-4 AEs compared to the nilotinib group (22 vs. 54%, p < 0.001), and had more frequent dose reduction, interruption, and discontinuation (p < 0.001, p = 0.004, and p = 0.006, respectively). Of 59 patients who discontinued treatment, 47 (80%) discontinued treatment due to AEs; 50% of the AEs causing drug discontinuation were of grade 2 severity...
April 4, 2017: International Journal of Hematology
https://www.readbyqxmd.com/read/28377326/treatment-and-molecular-monitoring-update-in-chronic-myeloid-leukemia-management
#20
Nathalie Sorel, Émilie Cayssials, Françoise Brizard, Jean-Claude Chomel
Chronic myeloid leukemia (CML) is a myeloproliferative neoplasm resulting from the t(9;22)(q34;q11) translocation. It is characterized by the presence of the BCR-ABL1 fusion gene encoding the BCR-ABL oncoprotein characterized by a deregulated tyrosine kinase activity. Targeted therapies using tyrosine kinase inhibitors (TKI) such as imatinib, dasatinib, nilotinib, bosutinib, or ponatinib have profoundly changed the natural history of the disease with a major impact on survival. Indeed, most patients diagnosed today can enjoy a near normal life expectancy...
April 1, 2017: Annales de Biologie Clinique
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