keyword
MENU ▼
Read by QxMD icon Read
search

Midostaurin

keyword
https://www.readbyqxmd.com/read/29713444/personalizing-initial-therapy-in-acute-myeloid-leukemia-incorporating-novel-agents-into-clinical-practice
#1
REVIEW
Christin B DeStefano, Christopher S Hourigan
While the past decade has seen a revolution in understanding of the genetic and molecular etiology of the disease, in clinical practice, initial therapy for acute myeloid leukemia (AML) patients has been a relatively straightforward choice between intensive combination cytotoxic induction therapy as used for decades or less-intensive hypomethylating therapy. The year 2017, however, witnessed US Food and Drug Administration approvals of midostaurin, enasidenib, gemtuzumab ozogamicin and CPX-351 for AML patients, with many other promising agents currently in clinical trials...
May 2018: Therapeutic Advances in Hematology
https://www.readbyqxmd.com/read/29704617/the-role-of-small-molecule-kit-protein-tyrosine-kinase-inhibitors-in-the-treatment-of-neoplastic-disorders
#2
REVIEW
Robert Roskoski
The Kit proto-oncogene was found as the consequence of the discovery of the feline v-kit sarcoma oncogene. Stem cell factor (SCF) is the Kit ligand and it mediates Kit dimerization and activation. The Kit receptor contains an extracellular segment that is made up of five immunoglobulin-like domains (D1/2/3/4/5), a transmembrane segment, a juxtamembrane segment, a protein-tyrosine kinase domain that contains an insert of 77 amino acid residues, and a carboxyterminal tail. Activating somatic mutations in Kit have been documented in various neoplasms including gastrointestinal stromal tumors (GIST), mast cell overexpression (systemic mastocytosis), core-binding factor acute myeloid leukemias (AML), melanomas, and seminomas...
April 25, 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/29618463/stone-rm-manley-pw-larson-ra-capdeville-r-midostaurin-its-odyssey-from-discovery-to-approval-for-treating-acute-myeloid-leukemia-and-advanced-systemic-mastocytosis-blood-adv-2017-2-4-444-453
#3
https://www.readbyqxmd.com/read/29568385/persistent-dna-strand-breaks-induce-a-caf-like-phenotype-in-normal-fibroblasts
#4
Arnaud J Legrand, Mattia Poletto, Daniela Pankova, Elena Clementi, John Moore, Francesc Castro-Giner, Anderson J Ryan, Eric O'Neill, Enni Markkanen, Grigory L Dianov
Cancer-associated fibroblasts (CAFs) are an emerging target for cancer therapy as they promote tumour growth and metastatic potential. However, CAF targeting is complicated by the lack of knowledge-based strategies aiming to selectively eliminate these cells. There is a growing body of evidence suggesting that a pro-inflammatory microenvironment (e.g. ROS and cytokines) promotes CAF formation during tumorigenesis, although the exact mechanisms involved remain unclear. In this study, we reveal that a prolonged pro-inflammatory stimulation causes a de facto deficiency in base excision repair, generating unrepaired DNA strand breaks and thereby triggering an ATF4-dependent reprogramming of normal fibroblasts into CAF-like cells...
March 2, 2018: Oncotarget
https://www.readbyqxmd.com/read/29558838/isavuconazole-therapy-in-an-flt3-mutated-acute-myeloid-leukemia-patient-receiving-midostaurin-a-case-report
#5
Eris Tollkuci
Midostaurin is the first approved FMS-related tyrosine kinase 3 (FLT3) inhibitor indicated for FLT3 mutated acute myeloid leukemia. Midostaurin is a major cytochrome P450 3A4 (CYP3A4) substrate. Coadministration with a strong CYP3A4 inhibitor or inducer can lead to a potential increase or decrease in midostaurin exposure. This report describes a 43-year-old patient with FLT3-internal tandem duplication (FLT3-ITD) positive acute myeloid leukemia who initially presented with leukocytosis and concern for acute leukemia...
January 1, 2018: Journal of Oncology Pharmacy Practice
https://www.readbyqxmd.com/read/29487059/midostaurin-its-odyssey-from-discovery-to-approval-for-treating-acute-myeloid-leukemia-and-advanced-systemic-mastocytosis
#6
REVIEW
Richard M Stone, Paul W Manley, Richard A Larson, Renaud Capdeville
Midostaurin was a prototype kinase inhibitor, originally developed as a protein kinase C inhibitor and subsequently as an angiogenesis inhibitor, based on its inhibition of vascular endothelial growth factor receptor. Despite promising preclinical data, early clinical trials in multiple diseases showed only modest efficacy. In 1996, the relatively frequent occurrence of fms-like tyrosine kinase 3 ( FLT3 ) activating mutations in acute myeloid leukemia (AML) was first recognized. Several years later, midostaurin was discovered to be a potent inhibitor of the FLT3 tyrosine kinase and to have activity against mutant forms of KIT proto-oncogene receptor tyrosine kinase, which drive advanced systemic mastocytosis (SM)...
February 27, 2018: Blood Advances
https://www.readbyqxmd.com/read/29416774/flow-cytometric-characterization-of-acute-leukemia-reveals-a-distinctive-blast-gate-of-murine-t-lymphoblastic-leukemia-lymphoma
#7
Zengkai Pan, Min Yang, Kezhi Huang, Guntram Büsche, Silke Glage, Arnold Ganser, Zhixiong Li
Immunophenotypic analysis using multiparameter flow cytometry is an indispensable tool for diagnosis and management of acute leukemia. Mouse models have been widely used for medical research for more than 100 years and are indispensable for leukemia research. However, immunophenotypic analysis of murine leukemia was not always performed in published studies, and blast gating for isolation of blasts was shown only in very few studies. No systemic characterization of all types of murine acute leukemia in large cohorts by flow cytometry has been reported...
January 5, 2018: Oncotarget
https://www.readbyqxmd.com/read/29350920/crystal-structures-and-human-leukemia-cell-apoptosis-inducible-activities-of-parthenolide-analogues-isolated-from-piptocoma-rufescens
#8
Yulin Ren, Judith C Gallucci, Xinxin Li, Lichao Chen, Jianhua Yu, A Douglas Kinghorn
The molecular structures of three parthenolide analogues, (-)-goyazensolide (1), (-)-15-deoxygoyazensolide (2), and (-)-ereglomerulide (3), isolated from the leaves of Piptocoma rufescens in a previous study were determined by X-ray analysis, and the absolute configuration of (-)-goyazensolide (1) was confirmed crystallographically using Cu Kα radiation at low temperature. Compounds 1-3, (+)-rufesolide A (4), and commercial parthenolide were found to be growth inhibitory toward MOLM-13 and EOL-1 human acute myeloid leukemia cells using PKC412 (midostaurin) as the positive control, with 1-3 being more active than parthenolide...
March 23, 2018: Journal of Natural Products
https://www.readbyqxmd.com/read/29343975/spotlight-on-midostaurin-in-the-treatment-of-flt3-mutated-acute-myeloid-leukemia-and-systemic-mastocytosis-design-development-and-potential-place-in-therapy
#9
REVIEW
Ellen Weisberg, Martin Sattler, Paul W Manley, James D Griffin
The Fms-like tyrosine kinase-3 (FLT3; fetal liver kinase-2; human stem cell tyrosine kinase-1; CD135) is a class III receptor tyrosine kinase that is normally involved in regulating the proliferation, differentiation, and survival of both hematopoietic cells and dendritic cells. Mutations leading it to be constitutively activated make it an oncogenic driver in ~30% of acute myeloid leukemia (AML) patients where it is associated with poor prognosis. The prevalence of oncogenic FLT3 and the dependency on its constitutively activated kinase activity for leukemia growth make this protein an attractive target for therapeutic intervention...
2018: OncoTargets and Therapy
https://www.readbyqxmd.com/read/29339551/inhibition-of-flt3-and-pim-kinases-by-ec-70124-exerts-potent-activity-in-preclinical-models-of-acute-myeloid-leukemia
#10
Noelia Puente-Moncada, Paula Costales, Isaac Antolín, Luz Elena Núñez, Patricia Oro, Maria Ana Hermosilla, Jhudit Perez-Escuredo, Nicolas Rios-Lombardia, Ana M Sanchez-Sanchez, Elisa Luño, Carmen Rodriguez, Vanesa Martin, Francisco Moris
Internal tandem duplication (ITD) or tyrosine kinase domain mutations of FLT3 is the most frequent genetic alteration in acute myeloid leukemia (AML) and are associated with poor disease outcome. Despite considerable efforts to develop single-target FLT3 drugs, so far, the most promising clinical response has been achieved using the multikinase inhibitor midostaurin. Here we explore the activity of the indolocarbazole EC-70124, from the same chemical space as midostaurin, in preclinical models of AML, focusing on those bearing FLT3-ITD mutations...
January 16, 2018: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/29327871/midostaurin-in-flt3-mutated-acute-myeloid-leukemia
#11
Richard M Stone, Richard A Larson, Hartmut Döhner
No abstract text is available yet for this article.
November 9, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/29327870/midostaurin-in-flt3-mutated-acute-myeloid-leukemia
#12
Ranjit K Sahoo, Lalit Kumar
No abstract text is available yet for this article.
November 9, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/29327869/midostaurin-in-flt3-mutated-acute-myeloid-leukemia
#13
A Emre Eskazan
No abstract text is available yet for this article.
November 9, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/29296877/the-role-of-targeted-therapy-in-the-management-of-patients-with-aml
#14
REVIEW
Alexander E Perl
Drug therapy for acute myeloid leukemia (AML) is finally undergoing major changes in 2017. This is due to the US Food and Drug Administration's approval of several new, targeted agents (midostaurin, enasidenib, and gemtuzumab ozogamicin). Paired with the recent approval of a novel liposomal formulation of daunorubicin/cytarabine (CPX-351/Vyxeos), the standard of care is changing rapidly in AML for subgroups. This review will focus on currently approved agents and promising novel agents in development and will highlight controversial areas in targeted treatment...
November 14, 2017: Blood Advances
https://www.readbyqxmd.com/read/29286055/midostaurin-for-the-treatment-of-adult-patients-with-newly-diagnosed-acute-myeloid-leukemia-that-is-flt3-mutation-positive
#15
REVIEW
J S Garcia, M E Percival
Midostaurin is a multitargeted tyrosine kinase inhibitor (TKI) that potently inhibits activated fms-related tyrosine kinase 3 (FLT3) in the nanomolar range and other kinases including platelet-derived growth factor receptors α (PDGFR- α) and β (PDGFR- β), cyclin-dependent kinase, proto-oncogene tyrosine-protein kinase Src, tyrosine-protein kinase Fgr, spleen tyrosine kinase (Syk), KIT proto-oncogene receptor tyrosine kinase and the major vascular endothelial growth factor receptor (VEGFR). Activating mutations in FLT3, which is one of the more common acute myeloid leukemia (AML) mutations, particularly those that result in an FLT3-ITD (internal tandem duplication) mutation, confer poor prognosis and represent a therapeutic target...
October 2017: Drugs of Today
https://www.readbyqxmd.com/read/29277359/soho-state-of-the-art-update-and-next-questions-mpn
#16
REVIEW
Prithviraj Bose, Jason Gotlib, Claire N Harrison, Srdan Verstovsek
The discovery of the activating Janus kinase (JAK)2V617F mutation in 2005 in most patients with the classic Philadelphia chromosome-negative myeloproliferative neoplasms (MPN) spurred intense interest in research into these disorders, culminating in the identification of activating mutations in MPL in 2006 and indels in the gene encoding calreticulin (CALR) in 2013, thus providing additional mechanistic explanations for the universal activation of JAK-signal transducer and activator of transcription (JAK-STAT) observed in these conditions, and the success of the JAK1/2 inhibitor ruxolitinib, which first received regulatory approval in 2011...
January 2018: Clinical Lymphoma, Myeloma & Leukemia
https://www.readbyqxmd.com/read/29276274/formulary-drug-review-naldemedine
#17
Danial E Baker
Each month, subscribers to The Formulary Monograph Service receive 5 to 6 well-documented monographs on drugs that are newly released or are in late phase 3 trials. The monographs are targeted to Pharmacy & Therapeutics Committees. Subscribers also receive monthly 1-page summary monographs on agents that are useful for agendas and pharmacy/nursing in-services. A comprehensive target drug utilization evaluation/medication use evaluation (DUE/MUE) is also provided each month. With a subscription, the monographs are available online to subscribers...
July 2017: Hospital Pharmacy
https://www.readbyqxmd.com/read/29249817/drug-induced-inhibition-of-phosphorylation-of-stat5-overrides-drug-resistance-in-neoplastic-mast-cells
#18
B Peter, S Bibi, G Eisenwort, B Wingelhofer, D Berger, G Stefanzl, K Blatt, H Herrmann, E Hadzijusufovic, G Hoermann, T Hoffmann, J Schwaab, M Jawhar, M Willmann, W R Sperr, J Zuber, K Sotlar, H-P Horny, R Moriggl, A Reiter, M Arock, P Valent
Systemic mastocytosis (SM) is a mast cell (MC) neoplasm with complex pathology and a variable clinical course. In aggressive SM (ASM) and MC leukemia (MCL), responses to conventional drugs are poor and the prognosis is dismal. R763 is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT and FLT3. We examined the effects of R763 on proliferation and survival of neoplastic MC. R763 produced dose-dependent inhibition of proliferation in the human MC lines HMC-1.1 (IC50 5-50 nM), HMC-1...
November 29, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/29231051/midostaurin-in-combination-with-standard-chemotherapy-for-treatment-of-newly-diagnosed-fms-like-tyrosine-kinase-3-flt3-mutation-positive-acute-myeloid-leukemia
#19
Miryoung Kim, Sherry Williams
OBJECTIVE: To evaluate the efficacy and safety of midostaurin in combination with standard cytarabine and daunorubicin induction and cytarabine consolidation in newly diagnosed FLT3-mutated acute myeloid leukemia (AML). DATA SOURCE: A literature search of PubMed and MEDLINE (September 2017) was performed using the terms midostaurin, PKC412, FLT3 gene, and acute myeloid leukemia. STUDY SELECTION/DATA EXTRACTION: Clinical trials evaluating the efficacy and safety of midostaurin in combination with standard cytarabine and daunorubicin induction and cytarabine consolidation were reviewed for the treatment of newly diagnosed FLT3-mutated AML...
April 2018: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/29222237/the-role-of-targeted-therapy-in-the-management-of-patients-with-aml
#20
REVIEW
Alexander E Perl
Drug therapy for acute myeloid leukemia (AML) is finally undergoing major changes in 2017. This is due to the US Food and Drug Administration's approval of several new, targeted agents (midostaurin, enasidenib, and gemtuzumab ozogamicin). Paired with the recent approval of a novel liposomal formulation of daunorubicin/cytarabine (CPX-351/Vyxeos), the standard of care is changing rapidly in AML for subgroups. This review will focus on currently approved agents and promising novel agents in development and will highlight controversial areas in targeted treatment...
December 8, 2017: Hematology—the Education Program of the American Society of Hematology
keyword
keyword
81349
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"