2,396 results match your criteria nilotinib


Intracranial Hemorrhage in a Pediatric Patient with Chronic Myeloid Leukemia in Chronic Phase: A Case Report.

Case Rep Oncol 2021 Jan-Apr;14(1):525-530. Epub 2021 Mar 22.

Department of Pediatric Oncology, Fukushima Medical University, Fukushima, Japan.

Chronic myeloid leukemia (CML) is an uncommon entity in pediatric patients. CML in chronic phase (CML-CP) has a relatively favorable outcome. Leukostasis occurs in 9. Read More

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Therapeutic targeting of Lyn kinase to treat chorea-acanthocytosis.

Acta Neuropathol Commun 2021 May 3;9(1):81. Epub 2021 May 3.

Department of Neuroscience, Biomedicine and Movement Sciences, University of Verona, Verona, Italy.

Chorea-Acanthocytosis (ChAc) is a devastating, little understood, and currently untreatable neurodegenerative disease caused by VPS13A mutations. Based on our recent demonstration that accumulation of activated Lyn tyrosine kinase is a key pathophysiological event in human ChAc cells, we took advantage of Vps13a mice, which phenocopied human ChAc. Using proteomic approach, we found accumulation of active Lyn, γ-synuclein and phospho-tau proteins in Vps13a basal ganglia secondary to impaired autophagy leading to neuroinflammation. Read More

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Nilotinib-induced lichen planopilaris.

Int J Dermatol 2021 May 3. Epub 2021 May 3.

Dermatology Department, Dermo-Respiratory Research Laboratory UR14 SP 03, Fattouma Bourguiba Hospital, University of Medicine, Monastir, Tunisia.

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Development of Pigmentation-Regulating Agents by Drug Repositioning.

Int J Mol Sci 2021 Apr 9;22(8). Epub 2021 Apr 9.

Department of Dermatology, School of Medicine, Gyeongsang National University & Hospital, Jinju 52727, Korea.

Skin color is determined by the processes of melanin synthesis and distribution. Problems in various molecules or signaling pathways involved in melanin synthesis contribute to skin pigmentation defects. Several trials have been conducted on the production of pigmentation-regulating agents, and drug repositioning has emerged as a modern technique to identify new uses for existing drugs. Read More

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Meta-Analysis of Gastrointestinal Adverse Events from Tyrosine Kinase Inhibitors for Chronic Myeloid Leukemia.

Cancers (Basel) 2021 Apr 1;13(7). Epub 2021 Apr 1.

Laboratory for Pathology Dynamics, Department of Biomedical Engineering, Georgia Institute of Technology and Emory University School of Medicine, Atlanta, GA 30332, USA.

Tyrosine kinase inhibitors (TKIs) are the frontline therapy for BCR-ABL (Ph+) chronic myeloid leukemia (CML). A systematic meta-analysis of 43 peer-reviewed studies with 10,769 CML patients compared the incidence of gastrointestinal adverse events (GI AEs) in a large heterogeneous CML population as a function of TKI type. Incidence and severity of nausea, vomiting, and diarrhea were assessed for imatinib, dasatinib, bosutinib, and nilotinib. Read More

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H396P mutation in chronic myeloid leukaemia patient on nilotinib - A case report.

Malays J Pathol 2021 Apr;43(1):63-68

University Kebangsaan Malaysia Medical Centre, Department of Medicine, Kuala Lumpur, Malaysia.

Introduction: The advent of BCR-ABL1-targeted therapy with the tyrosine kinase inhibitor (TKI), for example, imatinib and nilotinib, marked a turning point in the therapy of chronic myeloid leukaemia (CML). However, a substantial proportion of patients experience primary or secondary disease resistance to TKI. There are multifactorial causes contributing to the treatment failure of which BCR-ABL1 kinase domain mutation being the most common. Read More

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Tyrosine Kinase Inhibitors and Beyond for Chronic Myeloid Leukemia in Children.

Paediatr Drugs 2021 Apr 26. Epub 2021 Apr 26.

Division of Pediatric Hematology, Oncology and Stem Cell Transplantation, Columbia University Medical Center, 161 Fort Washington Ave, New York, NY, 10032, USA.

Chronic myeloid leukemia (CML) is rare in children but presents a unique challenge as recent drug innovations have turned CML into a chronic disease with implications for treatment into adulthood. With the approval of newer-generation tyrosine kinase inhibitors (TKIs) in addition to imatinib, providers have more options for the treatment of chronic-phase CML (CML-CP) in children. The second-generation TKIs approved for use in children, nilotinib and dasatinib, have higher response rates than first-generation imatinib; however, overall survival rates appear to be the same. Read More

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Targeted Therapy for Chordoma: Key Molecular Signaling Pathways and the Role of Multimodal Therapy.

Target Oncol 2021 May 24;16(3):325-337. Epub 2021 Apr 24.

Brain Tumor Stem Cell Laboratory, Department of Neurologic Surgery, Mayo Clinic, 4500 San Pablo Rd. S, Jacksonville, FL, 32224, USA.

Background: Chordoma is a rare but devastating tumor that arises in the cranial skull base or spine. There are currently no US Food and Drug Administration-approved targeted therapies for chordoma, and little understanding of whether using more than one therapy has benefit over monotherapy.

Objective: The objective of this study was to systematically review the current status of clinical trials completed for patients with chordoma to determine if multimodal therapy offers a benefit in progression-free survival over monomodal therapy. Read More

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Predictive value of tyrosine phosphatase receptor gamma for the response to treatment tyrosine kinase inhibitors in chronic myeloid leukemia patients.

Sci Rep 2021 Apr 23;11(1):8833. Epub 2021 Apr 23.

School of Life Science, Pharmacy and Chemistry, Faculty of Science, Engineering and Computing, Kingston University London, London, United Kingdom.

Protein tyrosine phosphatase receptor gamma (PTPRG) is a member of the receptor-like family protein tyrosine phosphatases and acts as a tumor suppressor gene in different neoplasms. Recent studies reported the down-regulation of PTPRG expression levels in Chronic Myeloid Leukemia disease (CML). In addition, the BCR-ABL1 transcript level is currently a key predictive biomarker of CML response to treatment with Tyrosine Kinase Inhibitors (TKIs). Read More

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Assessment of Dasatinib Versus Nilotinib as Upfront Therapy for Chronic Phase of Chronic Myeloid Leukemia in Qatar: A Cost-Effectiveness Analysis.

Cancer Control 2021 Jan-Dec;28:10732748211001796

Hematology Department, National Center for Cancer Care and Research, HMC, Doha, Qatar.

Background: The economic outcome research of approved tyrosine kinase inhibitors for treating the chronic phase of chronic myeloid leukemia in developing is scarce. The aim of this study was to assess the cost-effectiveness of dasatinib and nilotinib for newly diagnosed chronic myeloid leukemia patients.

Methods: A decision tree model was developed linking clinical effectiveness (defined as major molecular response) and/or complete cytogenetic response, utility, and cost data over a 12-month period. Read More

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Hodgkin Lymphoma as a Secondary Neoplasm During Therapy for Chronic Myeloid Leukaemia: Case Report and Review of the Literature.

Onco Targets Ther 2021 12;14:2497-2503. Epub 2021 Apr 12.

Department of General Pathology, Pomeranian Medical University, Szczecin, Poland.

Introduction: Incidences of chronic myeloid leukaemia (CML) after treatment of Hodgkin lymphoma (HL) are well described. Here, we report a case of secondary HL in a patient with CML treated with dasatinib as a third-line treatment.

Patient Information: A 64-year-old male was diagnosed with CML and initially treated with imatinib and then with nilotinib due to resistance. Read More

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In silico drug repurposing for filarial infection predicts nilotinib and paritaprevir as potential inhibitors of the Wolbachia 5'-aminolevulinic acid synthase.

Sci Rep 2021 Apr 19;11(1):8455. Epub 2021 Apr 19.

Department of Biochemistry and Biotechnology, Kwame Nkrumah University of Science and Technology, KNUST, Kumasi, Ghana.

Filarial infections affect millions of individuals and are responsible for some notorious disabilities. Current treatment options involve repeated mass drug administrations, which have been met with several challenges despite some successes. Administration of doxycycline, an anti-Wolbachia agent, has shown clinical effectiveness but has several limitations, including long treatment durations and contraindications. Read More

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Interventions to Improve Adherence to Tyrosine Kinase Inhibitors in Chronic Myeloid Leukemia: A Systematic Review.

Am J Clin Oncol 2021 Apr 19. Epub 2021 Apr 19.

College of Nursing Department of Epidemiology & Biostatistics, Arnold School of Public Health Thomas Cooper Library, University of South Carolina Prisma Health-Midlands/USC School of Medicine Columbia, Internal Medicine Residency Program Medical University of South Carolina, Charleston, SC.

Background: Lack of adherence to tyrosine kinase inhibitors (TKIs) is a significant problem resulting in incomplete cytogenetic response and increased mortality in patients with chronic myeloid leukemia (CML). Few studies have been conducted on interventions to improve adherence. The authors conducted a systematic review to explore studies that examined the impact of strategies to improve TKI adherence among individuals with CML. Read More

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Direct interaction of the ATP-sensitive K channel by the tyrosine kinase inhibitors imatinib, sunitinib and nilotinib.

Biochem Biophys Res Commun 2021 Jun 12;557:14-19. Epub 2021 Apr 12.

Department of Molecular Medicine and Surgery, Karolinska Institutet, Sweden; Endocrine and Sarcoma Surgery Unit, Karolinska University Hospital, Sweden. Electronic address:

The ATP-regulated K channel (K) plays an essential role in the control of many physiological processes, and contains a ATP-binding site. Tyrosine kinase inhibitors (TKI) are commonly used drugs, that primarily target ATP-binding sites in tyrosine kinases. Herein, we used the patch-clamp technique to examine the effects of three clinically established TKIs on K channel activity in isolated membrane patches, using a pancreatic β-cell line as a K channel source. Read More

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The Potential Safe Antifibrotic Effect of Stem Cell Conditioned Medium and Nilotinib Combined Therapy by Selective Elimination of Rat Activated HSCs.

Biomed Res Int 2021 28;2021:6678913. Epub 2021 Mar 28.

Egyptian Liver Research Institute and Hospital (ELRIAH), Sherbin, El Mansoura, Egypt.

Hepatic fibrosis is a progressive disease with serious clinical complications that arise from abnormal propagation and activation of multiple inflammatory pathways. Nilotinib is an oral tyrosine kinase inhibitor with antifibrotic activity. Mesenchymal stem cells (MSCs) are blank cells and can differentiate into specific cell types. Read More

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Dasatinib in the Management of Pediatric Patients With Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia.

Front Oncol 2021 25;11:632231. Epub 2021 Mar 25.

Hematology Unit, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (IRST) IRCCS, Meldola, Italy.

Acute leukemia is the most common cancer in childhood; in particular, acute lymphoblastic leukemia (ALL) represents roughly up to 80% of all cases of acute leukemias in children. Survival of children with ALL has dramatically improved over the last few decades, and is now over 90% (versus 40% of adult patients) in developed countries, except for in infants (i.e. Read More

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Fertility considerations in targeted biologic therapy with tyrosine kinase inhibitors: a review.

J Assist Reprod Genet 2021 Apr 7. Epub 2021 Apr 7.

Department of Obstetrics, Gynecology and Women's Health, Spectrum Health Medical Group, Grand Rapids, MI, USA.

Purpose: To review the impact of tyrosine kinase inhibitors (TKIs) on fertility in men and women, embryo development, and early pregnancy, and discuss considerations for fertility preservation in patients taking TKIs.

Methods: A comprehensive literature search using the PubMed database was performed through February 2021 to evaluate the current literature on imatinib, nilotinib, dasatinib, and bosutinib as it relates to fertility and reproduction. Published case series were analyzed for pregnancy outcomes. Read More

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Nilotinib Improves Bioenergetic Profiling in Brain Astroglia in the 3xTg Mouse Model of Alzheimer's Disease.

Aging Dis 2021 Apr 1;12(2):441-465. Epub 2021 Apr 1.

1Division of Neurodegenerative Disorders, St. Boniface Hospital Research, Winnipeg, MB, Canada.

Current treatments targeting amyloid beta in Alzheimer's disease (AD) have minimal efficacy, which results in a huge unmet medical need worldwide. Accumulating data suggest that brain mitochondrial dysfunction play a critical role in AD pathogenesis. Targeting cellular mechanisms associated with mitochondrial dysfunction in AD create a novel approach for drug development. Read More

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Guided Cancer Therapy: Review of the Evidence and Considerations for Clinical Implementation.

Cancers (Basel) 2021 Mar 29;13(7). Epub 2021 Mar 29.

Department of Individualized Cancer Management, Moffitt Cancer Center, Tampa, FL 33612, USA.

Multi-gene assays often include and, in certain instances, may report associated toxicity risks for irinotecan, belinostat, pazopanib, and nilotinib. However, guidance for incorporating results into therapeutic decision-making is mostly lacking for these anticancer drugs. We summarized meta-analyses, genome-wide association studies, clinical trials, drug labels, and guidelines relating to the impact of polymorphisms on irinotecan, belinostat, pazopanib, or nilotinib toxicities. Read More

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Structure-Based Virtual Screening Identifies Multiple Stable Binding Sites at the RecA Domains of SARS-CoV-2 Helicase Enzyme.

Molecules 2021 Mar 7;26(5). Epub 2021 Mar 7.

Department of Biology, College of Science, United Arab Emirates University, Al Ain 15551, United Arab Emirates.

With the emergence and global spread of the COVID-19 pandemic, the scientific community worldwide has focused on search for new therapeutic strategies against this disease. One such critical approach is targeting proteins such as helicases that regulate most of the SARS-CoV-2 RNA metabolism. The purpose of the current study was to predict a library of phytochemicals derived from diverse plant families with high binding affinity to SARS-CoV-2 helicase (Nsp13) enzyme. Read More

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Nilotinib, A Tyrosine Kinase Inhibitor, Suppresses the Cell Growth and Triggers Autophagy in Papillary Thyroid Cancer.

Anticancer Agents Med Chem 2021 Apr 1. Epub 2021 Apr 1.

The Second Hospital of Hebei Medical University, No. 215 Heping West Road, Shijiazhuang 050000, Hebei. China.

Background: Papillary thyroid carcinoma (PTC) represents for the most common thyroid cancer. Until recently, treatment options for PTC patients are limited. Nilotinib is the second-generation tyrosine kinase inhibitor, and has been widely used in the treatment of chronic myeloid leukemia (CML). Read More

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Current status and novel strategy of CML.

Int J Hematol 2021 May 29;113(5):624-631. Epub 2021 Mar 29.

Department of Leukemia, The University of Texas MD Anderson Cancer Center, 1515 Holcombe Boulevard, Unit 428, Houston, TX, 77030, USA.

The advent of tyrosine kinase inhibitors (TKIs) has dramatically improved the outcome of patients with chronic myeloid leukemia (CML). Currently, four TKIs are available for the frontline treatment, including the first-generation TKI (imatinib) and the second-generation TKIs (dasatinib, nilotinib, and bosutinib). The second-generation TKIs lead to a faster and deeper molecular response without a survival benefit compared with imatinib. Read More

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Targeting autophagy as a therapeutic strategy to prevent dopamine neuron loss in early stages of Alzheimer disease.

Autophagy 2021 Apr 5:1-3. Epub 2021 Apr 5.

Department of Medicine and Surgery, Department of Sciences and Technologies for Humans and Environment, University Campus Bio-Medico, Rome, Italy.

Alzheimer disease (AD) is a neurodegenerative disorder for which no approved medication exists. AD is characterized by worsening cognitive and non-cognitive symptoms, and research in the AD field strives to identify very precocious brain alterations leading to an irreversible condition. Recently it has been demonstrated that several early AD symptoms are paralleled with degeneration of neurons producing dopamine (DA), a neurotransmitter involved in the regulation of cognitive and non-cognitive functions. Read More

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High-throughput liquid chromatography/electrospray ionization-tandem mass spectrometry method using in-source collision-induced dissociation for simultaneous quantification of imatinib, dasatinib, bosutinib, nilotinib, and ibrutinib in human plasma.

Biomed Chromatogr 2021 Mar 27:e5124. Epub 2021 Mar 27.

Faculty of Pharmaceutical Sciences, Tohoku University, Sendai, Miyagi, Japan.

Recent studies have shown that therapeutic drug monitoring of tyrosine kinase inhibitors (TKIs) could improve treatment efficacy and safety. A simple analytical method using high-performance LC/electrospray ionization-tandem mass spectrometry has been developed and validated for simultaneous quantification of BCR-ABL and Bruton's TKIs used for chronic leukemia (imatinib, dasatinib, bosutinib, nilotinib, and ibrutinib) in human plasma. Although these structures and physical properties are similar, owing to their different linear ranges, simultaneously determining the plasma levels of these five TKIs by applying optimal MS parameters remains difficult. Read More

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High-grade B-cell lymphoma developed during the treatment of chronic myeloid leukemia with bosutinib.

Clin Case Rep 2021 Mar 13;9(3):1344-1349. Epub 2021 Jan 13.

Department of Hematology Graduate School of Medicine Osaka City University Osaka Japan.

Tyrosine kinase inhibitor (TKI) can help to increase the survival time in chronic myeloid leukemia (CML) patients; however, the risk of secondary malignancies due to TKIs is a growing concern. Only few reports showed clinical course of patients who developed lymphoma during TKI therapies. Herein, we report a case of high-grade B-cell lymphoma diagnosed in the course of CML treatment with bosutinib. Read More

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Ultrasound arterial anomalies in patients exposed to nilotinib therapy for chronic myeloid leukemia.

J Med Vasc 2021 Apr 6;46(2):66-71. Epub 2021 Mar 6.

Unité d'Exploration et de médecine vasculaires, Faculté de Médecine de Marseille, Aix-Marseille Université, Assistance Publique Hôpitaux de Marseille - Hôpital de la Timone, 264, rue Saint-Pierre, 13385 Marseille cedex 05, France; Institut Paoli-Calmettes, département d'Onco-hématologie, 232, boulevard Sainte-Marguerite, BP 156, 13273 Marseille cedex 9, France.

Introduction: Patients exposed to nilotinib for chronic myeloid leukemia (CML) appear to be at risk of arterial complication. The prevalence and aspect of ultrasound asymptomatic arterial lesions are unknown.

Objective: To describe prevalence and characteristics of ultrasound arterial anomalies in patients treated with nilotinib for CML. Read More

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The Discovery of Novel BCR-ABL Tyrosine Kinase Inhibitors Using a Pharmacophore Modeling and Virtual Screening Approach.

Front Cell Dev Biol 2021 4;9:649434. Epub 2021 Mar 4.

College of Pharmacy and Health Sciences, St. John's University, Queens, NY, United States.

Chronic myelogenous leukemia (CML) typically results from a reciprocal translocation between chromosomes 9 and 22 to produce the oncogene that when translated, yields the p210 BCR-ABL protein in more than 90% of all CML patients. This protein has constitutive tyrosine kinase activity that activates numerous downstream pathways that ultimately produces uncontrolled myeloid proliferation. Although the use of the BCR-ABL tyrosine kinase inhibitors (TKIs), such as imatinib, nilotinib, dasatinib, bosutinib, and ponatinib have increased the overall survival of CML patients, their use is limited by drug resistance and severe adverse effects. Read More

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An indirect comparison between bosutinib, nilotinib and dasatinib in first-line chronic phase chronic myeloid leukemia.

Curr Med Res Opin 2021 May 2;37(5):801-809. Epub 2021 Apr 2.

Ingress Health, Rotterdam, The Netherlands.

Objective: Bosutinib, nilotinib and dasatinib are approved for the treatment of patients with newly diagnosed chronic-phase chronic myeloid leukemia (CP-CML). In the absence of head-to-head comparisons between second-generation tyrosine kinase inhibitors (TKIs), the objective of this study was to indirectly compare the efficacy of bosutinib with nilotinib and dasatinib in first-line (1L) CP-CML.

Methods: Cross-trial heterogeneity in terms of patient baseline characteristics and imatinib dose escalation are difficult to adjust for in network meta-analyses and anchored matching-adjusted indirect treatment comparisons (MAICs). Read More

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Efficiency of nilotinib to target chronic phase-chronic myeloid leukaemia primary mature CD34 and immature CD34 cells.

Sci Rep 2021 Mar 17;11(1):6187. Epub 2021 Mar 17.

Hématologie Biologique, CHU Clermont-Ferrand, Hôpital Estaing, 1 place Lucie et Raymond Aubrac, 63003, Clermont-Ferrand Cedex 1, France.

Accumulation in target cells is an essential pharmacokinetic step of targeted therapies. Tyrosine Kinase Inhibitors (TKI) against the BCR-ABL fusion protein in Chronic Phase-Chronic Myeloid Leukaemia (CP-CML) cells constitute a unique model in terms of efficacy, specificity, and in vivo demonstration of response heterogeneity by target cells. The overall therapeutic response to nilotinib is heterogeneous with no satisfactory explanation. Read More

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Chronic Myelogenous Leukemia in Childhood.

Curr Oncol Rep 2021 Mar 14;23(4):40. Epub 2021 Mar 14.

Division of Hematology/Oncology, Department of Pediatrics, Stanford University School of Medicine, CCSR-1215C, 269 Campus Drive, Stanford, CA, USA.

Purpose Of Review: Chronic myelogenous leukemia (CML) is rare in children, requiring extrapolation from treatment of adults. In this review, we explore similarities and differences between adult and pediatric CML with a focus on therapeutic advances and emerging clinical questions.

Recent Findings: Pediatric CML is effectively treated with long-term targeted therapy using tyrosine kinase inhibitors (TKIs). Read More

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