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https://www.readbyqxmd.com/read/29046392/nutlin-3-plus-tanshinone-iia-exhibits-synergetic-anti-leukemia-effect-with-imatinib-by-reactivating-p53-and-inhibiting-akt-mtor-pathway-in-ph-all
#1
Yong Guo, Yi Li, Bing Xiang, Xiao-Ou Huang, Hong-Bing Ma, Fang-Fang Wang, Yu-Ping Gong
Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) is triggered by BCR/ABL kinase. Recent efforts focused on the development of more potent tyrosine kinase inhibitors (TKI) that also inhibit mutant tyrosine kinases such as nilotinib and dasatinib. Although major advances in the treatment of this aggressive disease with potent inhibitors of the BCR/ABL kinases, patients in remission frequently relapse due to drug resistance possibly mediated, at least in part, by compensatory activation of growth-signaling pathways and protective feedback signaling of leukemia cells in response to TKI-treatment...
October 18, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/29040935/thermal-stability-study-of-crystalline-and-novel-spray-dried-amorphous-nilotinib-hydrochloride
#2
Maikel Herbrink, Herman Vromans, Jan Schellens, Jos Beijnen, Bastiaan Nuijen
The thermal characteristics and the thermal degradation of crystalline and amorphous nilotinib hydrochloride (NH) were studied. The spray drying technique was successfully utilized for the amorphization of NH and was evaluated by spectroscopic techniques and differential scanning calorimetry (DSC). The ethanolic spray drying process yielded amorphous NH with a glass transition temperature (Tg) of 147°C. Thermal characterization of the amorphous phase was performed by heat capacity measurements using modulated DSC (mDSC)...
October 12, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29036785/wide-transcriptome-analysis-and-cellularity-of-bone-marrow-cd34-lin-cells-of-patients-with-chronic-phase-chronic-myeloid-leukemia-at-diagnosis-vs-12-months-of-first-line-nilotinib-treatment
#3
Alessandra Trojani, Ester Pungolino, Giuseppe Rossi, Mariella D'Adda, Milena Lodola, Barbara Di Camillo, Alessandra Perego, Mauro Turrini, Ester Orlandi, Lorenza Borin, Alessandra Iurlo, Simona Malato, Francesco Spina, Maria Luisa Latargia, Francesco Lanza, Salvatore Artale, Michela Anghilieri, Maria Cristina Carraro, Gabriella De Canal, Enrica Morra, Roberto Cairoli
BACKGROUND: Chronic myeloid leukemia (CML) is a clonal myeloproliferative disorder with heterogeneous biological and clinical features. The biomolecular mechanisms of CML response to tyrosine-kinase inhibitors are not fully defined. OBJECTIVE: We undertook a gene expression profiling (GEP) study of selected bone marrow (BM) CD34+/lin- cells of chronic-phase CML patients at diagnosis and after 12 months of TKI nilotinib to investigate molecular signatures characterizing both conditions...
September 29, 2017: Cancer Biomarkers: Section A of Disease Markers
https://www.readbyqxmd.com/read/29034773/substrate-dependent-effects-of-molecular-targeted-anticancer-agents-on-activity-of-organic-anion-transporting-polypeptide-1b1
#4
Hiroyoshi Koide, Masayuki Tsujimoto, Ai Takeuchi, Miyu Tanaka, Yoko Ikegami, Mayu Tagami, Syoko Abe, Miki Hashimoto, Tetsuya Minegaki, Kohshi Nishiguchi
1. Organic anion-transporting polypeptide 1B1 (OATP1B1) plays an important role in the hepatic uptake of a broad range of substrate drugs. In vitro experiments show that molecular-targeted agents do not always have similar effects on OATP1B1 activity. 2. The purpose of this study was to clarify whether the effects of molecular-targeted agents on OATP1B1 are substrate-dependent. We used OATP1B1-transfected cells to compare the effects of molecular-targeted agents on OATP1B1-mediated uptake of fluorescein (FL), 2',7'-dichlorofluorescein (DCF), atorvastatin, SN-38, and valsartan...
October 16, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29032513/sudden-blast-phase-in-chronic-myeloid-leukemia-developed-during-nilotinib-therapy-after-major-molecular-response-was-achieved
#5
Yosuke Okada, Ken Sato, Shinichi Kobayashi, Shigeki Nagao, Kosuke Takano, Masahiro Teramoto, Noriaki Tachi, Toshikuni Kawamura, Toshikatsu Horiuchi, Shoichiro Kato, Reina Saga, Takaaki Maekawa, Takeshi Yamamura, Junichi Watanabe, Ayako Kobayashi, Fumihiko Kimura
Sudden blast phase (SBP) is a rare event in which patients with chronic myeloid leukemia (CML) in complete cytogenetic response (CCyR) rapidly progress to the blast phase. Few patients on second-generation tyrosine kinase inhibitors (2nd TKIs) have been reported to develop SBP. Here, we report a 45-year-old man diagnosed with CML in the chronic phase in April 2008 and immediately started on imatinib therapy. He achieved CCyR 12 months after starting imatinib therapy. Imatinib was followed by treatment with the 2nd TKIs nilotinib and dasatinib from January 2011 to yield a better response...
October 14, 2017: International Journal of Hematology
https://www.readbyqxmd.com/read/29032022/outcomes-of-newly-diagnosed-chronic-phase-chronic-myeloid-leukemia-following-an-elective-switch-from-second-generation-tyrosine-kinase-inhibitor-to-imatinib
#6
Vamsi K Kota, Jee Hyun Kong, Martha Arellano, Fuad El Rassi, Manila Gaddh, Leonard T Heffner, Elliott F Winton, Anand P Jillella, Morgan L McLemore, H Jean Khoury
The second-generation tyrosine kinase inhibitors (TKIs) (2G-TKIs) dasatinib (DAS) and nilotinib (NIL) yield faster responses in newly diagnosed chronic phase (CP) chronic myeloid leukemia (CML) as compared with imatinib (IM); however, long-term safety of these agents is a growing concern. We identified 20 patients with CP-CML diagnosed between August 2013 and October 2016 who initiated 2G-TKIs and were then switched after optimal response at 3 months to IM. Second-generation TKIs initiated were DAS (n = 15), NIL (n = 3), or both sequentially due to intolerance (n = 1)...
September 19, 2017: Clinical Lymphoma, Myeloma & Leukemia
https://www.readbyqxmd.com/read/29031704/evaluation-of-cooperative-anti-leukemic-effects-of-nilotinib-and-vildagliptin-in-ph-chronic-myeloid-leukemia
#7
Michael Willmann, Irina Sadovnik, Gregor Eisenwort, Martin Entner, Tina Bernthaler, Gabriele Stefanzl, Emir Hadzijusufovic, Daniela Berger, Harald Herrmann, Gregor Hoermann, Peter Valent, Thomas Rülicke
Chronic myeloid leukemia (CML) is a stem cell neoplasm characterized by the BCR/ABL1 oncogene. Although the disease can be kept under control using BCR/ABL1 tyrosine kinase inhibitors (TKI) in most cases, some patients relapse or have resistant disease which points to the need to identify new therapeutic targets in this malignancy. Recent data suggest that leukemic stem cell (LSC) in CML display the SC-mobilizing cell surface enzyme dipeptidyl-peptidase IV (DPPIV=CD26) in an aberrant manner. In the present study, we analyzed the effects of the DPPIV blocker vildagliptin as single agent or in combination with the BCR/ABL1 TKI imatinib or nilotinib on growth and survival of CML LSC in vitro and on LSC engraftment in an in vivo xenotransplantation NSG mouse model...
October 12, 2017: Experimental Hematology
https://www.readbyqxmd.com/read/29027647/dasatinib-associated-reversible-demyelinating-peripheral-polyneuropathy-in-a-case-of-chronic-myeloid-leukemia
#8
Takashi Ishida, Naoyuki Akagawa, Tomomi Miyata, Naomi Tominaga, Takahiro Iizuka, Masaaki Higashihara, Takahiro Suzuki, Koji Miyazaki
Tyrosine kinase inhibitors (TKIs) are essential for the treatment of chronic myeloid leukemia (CML). Adverse effects of dasatinib have been reported; however, few reports have highlighted the association between dasatinib and demyelinating peripheral neuropathy (DPN). We report a patient with CML who developed acute onset of DPN associated with dasatinib therapy. A 46-year-old Japanese woman was treated with dasatinib for 7 months after the diagnosis of CML and she achieved a major molecular response (MMR)...
October 13, 2017: International Journal of Hematology
https://www.readbyqxmd.com/read/29027641/cost-effectiveness-of-imatinib-dasatinib-and-nilotinib-as-first-line-treatment-for-chronic-phase-chronic-myeloid-leukemia-in-china
#9
Na Li, Bin Zheng, Hong-Fu Cai, Jing Yang, Xiao-Feng Luo, Li-Zhu Weng, Feng-Mei Zhan, Mao-Bai Liu
BACKGROUND AND OBJECTIVE: Tyrosine kinase inhibitors (TKIs) have obvious effects on chronic myeloid leukemia (CML), but they are expensive in China. Moreover, the overall cost of treatment of CML is high and the medical economic burden of patients with CML on the government is heavy. This study tested the cost effectiveness of imatinib, nilotinib, and dasatinib as first-line treatment in Chinese patients who were first diagnosed with chronic myeloid leukemia in the chronic phase (CML-CP)...
October 13, 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/29027261/prognostic-significance-of-additional-chromosomal-abnormalities-at-the-time-of-diagnosis-in-patients-with-chronic-myeloid-leukemia-treated-with-frontline-tyrosine-kinase-inhibitors
#10
Ahmad Alhuraiji, Hagop Kantarjian, Prajwal Boddu, Farhad Ravandi, Gautam Borthakur, Courtney DiNardo, Naval Daver, Tapan Kadia, Naveen Pemmaraju, Sherry Pierce, Guillermo Garcia-Manero, William Wierda, Srdan Verstovsek, Elias Jabbour, Jorge Cortes
Additional cytogenetic abnormalities (ACA) are considered a high risk feature in chronic myeloid leukemia (CML). However, its prognostic significance at the time of diagnosis in the setting of new tyrosine kinase inhibitors (TKIs) is less well understood. Patients with CML in CP with or without ACA at diagnosis treated with frontline TKIs in prospective clinical trials were analyzed for outcomes. Among 603 patients treated, 29 (5%) had ACA. Patients with ACA included 2 of 72 (2.8%) treated with imatinib 400 mg, 9 of 207 (4...
October 13, 2017: American Journal of Hematology
https://www.readbyqxmd.com/read/29021516/human-herpesvirus-8-unrelated-primary-effusion-lymphoma-like-lymphoma-following-tyrosine-kinase-inhibitor-treatment-for-chronic-myelogenous-leukemia
#11
Minoru Kojima, Naoya Nakamura, Jun Amaki, Hiroki Numata, Masashi Miyaoka, Tadashi Motoori, Koshi Matsumoto, Kiyoshi Ando
A 69-year-old man was diagnosed with chronic myelogenous leukemia (CML) and treated with dasatinib. After two years on dasatinib, the patient achieved complete molecular response, but dasatinib treatment was discontinued due to exacerbation of pleural effusion. Nilotinib and imatinib were started but stopped due to an increase in pleural effusion. Thoracentesis was performed and he was diagnosed with human herpesvirus 8-unrelated primary effusion lymphoma (PEL)-like lymphoma. Complex chromosomal abnormality, including BCL6 rearrangement, was found on chromosome analysis...
2017: Journal of Clinical and Experimental Hematopathology: JCEH
https://www.readbyqxmd.com/read/28990873/third-line-treatment-with-second-generation-tyrosine-kinase-inhibitors-dasatinib-or-nilotinib-in-patients-with-chronic-myeloid-leukemia-after-two-prior-tkis-real-life-data-on-a-single-center-experience-along-with-the-review-of-the-literature
#12
Seniz Ongoren, Ahmet Emre Eskazan, Veysel Suzan, Sercan Savci, Isil Erdogan Ozunal, Selin Berk, Fevzi Fırat Yalniz, Tugrul Elverdi, Ayse Salihoglu, Yucel Erbilgin, Sibel Aylin Iseri, Muhlis Cem Ar, Zafer Baslar, Yildiz Aydin, Nukhet Tuzuner, Ugur Ozbek, Teoman Soysal
OBJECTIVES: Newer tyrosine kinase inhibitors (TKIs) (bosutinib, ponatinib) and allogeneic hematopoietic stem cell transplantation (allo-HSCT) can be utilized as a salvage therapy in patients with chronic myeloid leukemia (CML) who failed two lines (imatinib → nilotinib or imatinib → dasatinib) of TKI therapy. However, these TKIs are not available in many countries and not all patients can undergo allo-HSCT. METHODS: In this study, CML patients who received dasatinib or nilotinib as a third-line treatment were retrospectively evaluated...
October 9, 2017: Hematology (Amsterdam, Netherlands)
https://www.readbyqxmd.com/read/28969556/ponatinib-a-review-of-efficacy-and-safety
#13
Fulvio Massaro, Matteo Molica, Massimo Breccia
Ponatinib is a third generation kinase inhibitor designed to overcome the gatekeeper T315I mutation. In different trials this drug showed inhibitory activity against native BCR-ABL1 kinase and several ABL1 mutations. For this reason, ponatinib is currently indicated for the treatment of chronic myeloid leukaemia (CML) in every phase of disease resistant and/or intolerant to dasatinib and nilotinib and for whom imatinib is not indicated anymore or for patients with T315I mutation. The drug is also indicated for Ph+ acute lymphoblastic leukaemia (ALL)...
October 2, 2017: Current Cancer Drug Targets
https://www.readbyqxmd.com/read/28965046/development-and-validation-of-a-sensitive-lc-ms-ms-method-for-simultaneous-determination-of-eight-tyrosine-kinase-inhibitors-and-its-application-in-mice-pharmacokinetic-studies
#14
Yu He, Lei Zhou, Song Gao, Taijun Yin, Yifan Tu, Robert Rayford, Xiaoqiang Wang, Ming Hu
The purpose of this study was to develop and validate a robust and sensitive LC-MS/MS method for simultaneous determinations of various tyrosine kinase inhibitors (TKIs) in biological samples and to apply the method to their pharmacokinetic studies. Processed samples were injected into the UHPLC system coupled to an ESI-triple quadrupole mass spectrometer. The compounds were separated on an AcQuity UHPLC BEH C18 column (50mm×2.1mm ID, 1.7μm) using a gradient elution of acetonitrile/0.1% formic acid in water...
September 11, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28954745/spontaneous-intramural-small-bowel-hematoma-in-a-patient-with-acute-myeloid-leukaemia-receiving-chemotherapy-and-nilotinib
#15
Glenda M Delgado Ramos, Guilherme Piovezani Ramos, Thomas G Cotter
Spontaneous intramural small bowel hematoma (SISBH) is a rare, acute abdominal condition, with increasing incidence in recent years. Excessive anticoagulation with vitamin K antagonists is the most common aetiology. We report the case of a large acute jejunal intramural hematoma in a patient with newly diagnosed acute myeloid leukaemia receiving chemotherapy and nilotinib. The patient presented with abdominal pain, haematochezia, acute anaemia and thrombocytopenia. CT of the abdomen and pelvis revealed SISBH...
September 27, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28938160/nilotinib-enhances-tumor-angiogenesis-and-counteracts-vegfr2-blockade-in-an-orthotopic-breast-cancer-xenograft-model-with-desmoplastic-response
#16
Sara Zafarnia, Jessica Bzyl-Ibach, Igor Spivak, Yongping Li, Susanne Koletnik, Dennis Doleschel, Anne Rix, Sibylle Pochon, Isabelle Tardy, Seena Koyadan, Marc van Zandvoort, Moritz Palmowski, Fabian Kiessling, Wiltrud Lederle
Vascular endothelial growth factor (VEGF)/VEGF receptor (VEGFR)-targeted therapies predominantly affect nascent, immature tumor vessels. Since platelet-derived growth factor receptor (PDGFR) blockade inhibits vessel maturation and thus increases the amount of immature tumor vessels, we evaluated whether the combined PDGFR inhibition by nilotinib and VEGFR2 blockade by DC101 has synergistic therapy effects in a desmoplastic breast cancer xenograft model. In this context, besides immunohistological evaluation, molecular ultrasound imaging with BR55, the clinically used VEGFR2-targeted microbubbles, was applied to monitor VEGFR2-positive vessels noninvasively and to assess the therapy effects on tumor angiogenesis...
September 19, 2017: Neoplasia: An International Journal for Oncology Research
https://www.readbyqxmd.com/read/28918995/cutaneous-adverse-events-of-targeted-therapies-for-hematolymphoid-malignancies
#17
REVIEW
Julia D Ransohoff, Bernice Y Kwong
The identification of oncogenic drivers of liquid tumors has led to the rapid development of targeted agents with distinct cutaneous adverse event (AE) profiles. The diagnosis and management of these skin toxicities has motivated a novel partnership between dermatologists and oncologists in developing supportive oncodermatology clinics. In this article we review the current state of knowledge of clinical presentation, mechanisms, and management of the most common and significant cutaneous AEs observed during treatment with targeted therapies for hematologic and lymphoid malignancies...
July 14, 2017: Clinical Lymphoma, Myeloma & Leukemia
https://www.readbyqxmd.com/read/28866691/primary-imatinib-resistance-in-chronic-myeloid-leukemia-patients-in-a-developing-country-bcr-abl-kinase-domain-mutations-or-bcr-abl-independent-mechanisms
#18
E Yap, N R Tumian, R Z Azma, N A Sharifah, S Salwati, N H Hamidah, M H Elias, C L Wong
Clinical resistance to imatinib (IM) in chronic myeloid leukemia (CML) carries adverse consequences. We investigated 22 CML patients who developed IM-resistance for BCR-ABL kinase domain (KD) mutations. The median follow-up for this study was 101.9 months (range: 22.2 to 176.5 months) and the estimated mean overall survival was 150.87 months (95% CI: 130.0 to 171.0). Five out of 22 patients tested positive for BCR-ABL KD mutations: 2 had T315I, 2 had E255K and 1 had V289F mutations. Of the remaining 17 patients who did not harbor BCR-ABL KD mutations, 11 patients received nilotinib while the rest continued on IM...
August 2017: Malaysian Journal of Pathology
https://www.readbyqxmd.com/read/28862704/sustained-deep-molecular-responses-in-patients-switched-to-nilotinib-due-to-persistent-bcr-abl1-on-imatinib-final-enestcmr-randomized-trial-results
#19
T P Hughes, B Leber, F Cervantes, N Spector, R Pasquini, N C D Clementino, A P Schwarer, P E Dorlhiac-Llacer, F-X Mahon, D Rea, A Guerci-Bresler, S Kamel-Reid, I Bendit, S Acharya, T Glynos, D Dalal, S Branford, J H Lipton
No abstract text is available yet for this article.
August 3, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/28854975/ruxolitinib-nilotinib-cotreatment-inhibits-leukemia-propagating-cells-in-philadelphia-chromosome-positive-all
#20
Yuan Kong, Yi-Lin Wu, Yang Song, Min-Min Shi, Xie-Na Cao, Hong-Yan Zhao, Ya-Zhen Qin, Yue-Yun Lai, Hao Jiang, Qian Jiang, Xiao-Jun Huang
BACKGROUND: As one of the major treatment obstacles in Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph(+)ALL), relapse of Ph(+)ALL may result from the persistence of leukemia-propagating cells (LPCs). Research using a xenograft mouse assay recently determined that LPCs were enriched in the CD34(+)CD38(-)CD58(-) fraction in human Ph(+)ALL. Additionally, a cohort study demonstrated that Ph(+)ALL patients with a LPCs phenotype at diagnosis exhibited a significantly higher cumulative incidence of relapse than those with the other cell phenotypes even with uniform front-line imatinib-based therapy pre- and post-allotransplant, thus highlighting the need for novel LPCs-based therapeutic strategies...
August 30, 2017: Journal of Translational Medicine
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