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[PDF] Top 20 FLT3 inhibitors in acute myeloid leukemia

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FLT3 inhibitors in acute myeloid leukemia

FLT3 inhibitors in acute myeloid leukemia

... treat FLT3/ITD-mutated AML in vitro and in vivo ...human FLT3/ITD-mutated AML cell ...with FLT3/ITD mutation ...with FLT3/ITD-mutated AML ...and FLT3/ITD was ...with FLT3-mutated ... See full document

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Clinical use of FLT3 inhibitors in acute myeloid leukemia

Clinical use of FLT3 inhibitors in acute myeloid leukemia

... Abstract: Acute myeloid leukemia (AML) is a highly heterogeneous ...of FLT3-ITD delivers poor ...on FLT3 inhibitor use to improve the outcomes of this otherwise difficult ...in ... See full document

12

Use of FLT3 inhibitors in acute myeloid leukemia remission induction or salvage therapy: systematic review and meta-analysis

Use of FLT3 inhibitors in acute myeloid leukemia remission induction or salvage therapy: systematic review and meta-analysis

... on FLT3 inhibitors in AML induction/salvage ...terms: leukemia, myeloid, acute AND FLT3 OR tyrosine kinase inhibitor OR sorafenib OR sunitinib OR midostaurin OR lestaurtinib OR ... See full document

18

FLT3  inhibitors: clinical potential in acute myeloid leukemia

FLT3 inhibitors: clinical potential in acute myeloid leukemia

... Abstract: Acute myeloid leukemia (AML) is an aggressive hematopoietic malignancy that is cured in as few as 15%–40% of ...of leukemia cell ...the FLT3 gene are the ones most commonly ... See full document

9

Downstream molecular pathways of FLT3 in the pathogenesis of acute myeloid leukemia: biology and therapeutic implications

Downstream molecular pathways of FLT3 in the pathogenesis of acute myeloid leukemia: biology and therapeutic implications

... that FLT3 inhibitors may have only a limited role as single-agent therapies, at least in patients with refractory or repeatedly relapsing ...with FLT3-ITD muta- tions can respond if adequate drug ... See full document

10

Spotlight on midostaurin  in the treatment of FLT3-mutated acute myeloid leukemia and systemic mastocytosis: design, development, and potential place in therapy

Spotlight on midostaurin in the treatment of FLT3-mutated acute myeloid leukemia and systemic mastocytosis: design, development, and potential place in therapy

... targeted FLT3 kinase inhibitors tested in clinical trials, and it exhibited sufficient efficacy and a favorable enough toxicity profile to move from testing as a single agent to testing in combina- tion ... See full document

8

CDC25A governs proliferation and differentiation of FLT3-ITD acute myeloid leukemia

CDC25A governs proliferation and differentiation of FLT3-ITD acute myeloid leukemia

... promyelocytic leukemia with all- transretinoic acid or arsenic trioxide, which transformed the prognosis of this ...non-promyelocytic leukemia, the discovery of key mutations this last decade led to intense ... See full document

18

Next-generation sequencing of FLT3 internal tandem duplications for minimal residual disease monitoring in acute myeloid leukemia

Next-generation sequencing of FLT3 internal tandem duplications for minimal residual disease monitoring in acute myeloid leukemia

... in FLT3 interferes with the auto-inhibitory function of the juxtamembrane domaine and constitutively activates the tyrosine kinase, leading to enhanced RAS, MAPK, and STAT5 ...with FLT3 ITD have an ... See full document

10

The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia

The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia

... and FLT3, 2 attractive targets in ...and FLT3 and activa- tion of their downstream effectors, leading to induction of apoptosis and decreased clonal expansion and/ or colony formation in AML cell lines and ... See full document

17

Gilteritinib: a novel FLT3 inhibitor for acute myeloid leukemia

Gilteritinib: a novel FLT3 inhibitor for acute myeloid leukemia

... in acute myeloid leukemia (AML), especially in those with normal ...The FLT3-ITD and FLT3-TKD (tyrosine kinase domain) mutations are biomarkers for high risk AML and are associated with ... See full document

6

Targeting Oncogenic Signaling in Mutant FLT3 Acute Myeloid Leukemia: the Path to Least Resistance

Targeting Oncogenic Signaling in Mutant FLT3 Acute Myeloid Leukemia: the Path to Least Resistance

... chronic myeloid leukemia (CML) ...of FLT3 TKIs for ...for FLT3 TKI monotherapy have seen the development of treatment resistance and relapse in less than 3 months of ...generation FLT3 ... See full document

35

Isocitrate dehydrogenase inhibitors in acute myeloid leukemia

Isocitrate dehydrogenase inhibitors in acute myeloid leukemia

... Approximately 40–45% of young and 10–20% of elderly AML patients treated with standard therapy will be cured. There are no more than 10% of relapsed or refractory (R/ R) AML [1–4]. Advancements in next-generation sequen- ... See full document

8

Activation of protein phosphatase 2A in FLT3+ acute myeloid leukemia cells enhances the cytotoxicity of FLT3 tyrosine kinase inhibitors

Activation of protein phosphatase 2A in FLT3+ acute myeloid leukemia cells enhances the cytotoxicity of FLT3 tyrosine kinase inhibitors

... and FLT3 inhibitors. (A) BaF3/FLT3-ITD cells were grown in methylcellulose medium for 7 days in the presence of AAL(S) ± Sorafenib, CEP701, PKC412 or ...BaF3/ FLT3-ITD or (C) MV4-11 cells ... See full document

14

Structural and functional Alterations of FLT3 in 
Acute Myeloid Leukemia

Structural and functional Alterations of FLT3 in Acute Myeloid Leukemia

... of FLT3/ALM in pediatric and adult AML. Prevalence of FLT3/ALM is 6-8%, regardless of age and the presence of FLT3/ALM and FLT3/ITD appears to be mutually ...of FLT3/ALM is not ... See full document

16

PIM 1 mRNA expression is a potential prognostic biomarker in acute myeloid leukemia

PIM 1 mRNA expression is a potential prognostic biomarker in acute myeloid leukemia

... Results: We observed that expression of PIM-1 mRNA was higher in AML patients than in healthy individuals and in complete remission AML patients (P = 0.0177). Further, high PIM-1 mRNA levels were more associated with ... See full document

9

Pim kinase inhibition sensitizes FLT3-ITD acute myeloid leukemia cells to topoisomerase 2 inhibitors through increased DNA damage and oxidative stress

Pim kinase inhibition sensitizes FLT3-ITD acute myeloid leukemia cells to topoisomerase 2 inhibitors through increased DNA damage and oxidative stress

... in FLT3-ITD AML is complex. FLT3-ITD cells have high baseline ROS levels [50] which are associated with increased DNA ...in FLT3-ITD cells also inactivate the protein tyrosine phosphatase DEP-1/PTPRJ ... See full document

16

A Morphological Study of Acute Myeloid Leukemia and Correlation With Clinical and Laboratory Findings, Including Results of Cytogenetic Analysis and Mutation Screening

A Morphological Study of Acute Myeloid Leukemia and Correlation With Clinical and Laboratory Findings, Including Results of Cytogenetic Analysis and Mutation Screening

... Verhaak et al(105) reported the mean age of patients with AML and NPM1 mutations to be 47.3 years (±10.7 years) and that of AML with wild-type NPM1 to be 39.7 years (±13.3 years). A similar trend was seen in our study ... See full document

136

Cost-effectiveness analysis for midostaurin versus standard of care in acute myeloid leukemia in the United Kingdom

Cost-effectiveness analysis for midostaurin versus standard of care in acute myeloid leukemia in the United Kingdom

... The economic evaluation, conducted from a UK healthcare system perspective, expanded on data from RATIFY and incorporated costs from local data sources. OS with or without the addition of MIDO to the SOC was extrapolated ... See full document

13

An essential pathway links FLT3-ITD, HCK and CDK6 in acute myeloid leukemia

An essential pathway links FLT3-ITD, HCK and CDK6 in acute myeloid leukemia

... In acute myeloid leukemia (AML), the activity of the CDK/Cyclin D complex is ...carrying FLT3-ITD mutations are dependent on CDK6 for cell proliferation while CDK4 is not ...that ... See full document

11

The Philadelphia chromosome in leukemogenesis

The Philadelphia chromosome in leukemogenesis

... kinase inhibitors (TKIs) targeting the BCR-ABL1 protein are the most successful targeted therapy for Ph-positive ...positive leukemia [8–10]. Leukemia stem cells and BCR- ABL kinase domain mutations ... See full document

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