Dasatinib: A tyrosine kinase inhibitor for the treatment of chronic myelogenous leukemia and philadelphia chromosome—positive acute lymphoblastic leukemia

Steinberg, Michael

doi:10.1016/j.clinthera.2007.11.005

Cited by 192 publications

(128 citation statements)

References 50 publications

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“…BCR/ABL fusion protein has a constitutive tyrosine kinase activity due to the presence of kinase domain of ABL. This fusion protein operates several signaling pathways causing uncontrolled cellular proliferation, reduction of apoptosis, and decrease in the cellular adhesion (1)(2)(3)(4)(5)(6).…”

Section: Introductionmentioning

confidence: 99%

Combination of Fludarabine and Imatinib Induces Apoptosis Synergistically Through Loss of Mitochondrial Membrane Potential and Increases in Caspase-3 Enzyme Activity in Human K562 Chronic Myleloid Leukemia Cells

Baran

Oztekin

Bassoy

2010

Cancer Investigation

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In this study, we aimed to show the synergistic apoptotic effects of imatinib/fludarabine combination in human K562 chronic myleloid leukemia (CML) cells. There was a significant increase in cytotoxicity of combination of imatinib and fludarabine as compared to any agent alone. On the other hand, combination of both agents induced apoptosis significantly as confirmed by increases in caspase-3 enzyme activity and decreases in mitochondrial membrane potential. As a summary, the results of this study strongly suggest that combination of imatinib and fludarabine induced cell death synergistically comparing to only imatinib or fludarabine in human K562 CML cells.

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Section: Introductionmentioning

confidence: 99%

Combination of Fludarabine and Imatinib Induces Apoptosis Synergistically Through Loss of Mitochondrial Membrane Potential and Increases in Caspase-3 Enzyme Activity in Human K562 Chronic Myleloid Leukemia Cells

Baran

Oztekin

Bassoy

2010

Cancer Investigation

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“…[5] Dasatinib also has activity against other oncogenic tyrosine kinases, such as Src family kinases, c-kit, platelet-derived growth factor receptor, and ephrin-A. [6] While various adverse effects have been reported in patients treated with BCR/ABL kinase inhibitors, there are few reports about their adverse effects on renal function, just as there are only a few cases concerning renal failure associated with imatinib. [7][8][9][10] Kitiyakara and Atichartakarn [7] reported a case in which the use of imatinib for blastic transformation of CML is associated with the development of acute or chronic renal failure.…”

Section: Discussionmentioning

confidence: 99%

Acute Renal Failure under Dasatinib Therapy

et al. 2010

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Dasatinib is a second-generation tyrosine kinase inhibitor that is approved for the treatment of imatinib-resistant or imatinib-intolerant chronic myeloid leukemia. It has a 325 times stronger in vitro activity against to native BCR-ABL when comparing with imatinib. Little is known about the effects of dasatinib on renal function. A literature review revealed only one case with imatinib-resistant chronic myeloid leukemia that developed renal failure after being placed on dasatinib therapy. Here we report a patient with imatinib-resistant chronic myeloid leukemia who developed gastroenteritis and acute renal failure after a short time from the initiation of dasatinib therapy. After dasatinib interruption, these side effects resolved completely in days. In summary, dasatinib is a potent drug in the treatment of chronic myeloid leukemia, but close clinical monitoring and the timely interruption of the therapy in patients who developed acute renal failure are warranted.

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“…However, many factors play a role in determining whether dasatinib may provide benefit to patients. Some of these factors are known, such as BCR-ABL-sensitive mutations, whereas other mechanisms of CML not related to BCR-ABL are unknown or unclear [14]. Another second generation TKI is Nilotinib (Tasigna TM , AMN107).…”

Section: Introductionmentioning

confidence: 99%

HPLC–MS method for the simultaneous quantification of the antileukemia drugs imatinib, dasatinib and nilotinib in human peripheral blood mononuclear cell (PBMC)

D’Avolio¹,

Simiele²,

Francia

et al. 2012

Journal of Pharmaceutical and Biomedical Analysis

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A new method using high performance liquid chromatography coupled with electrospray mass spectrometry is described for the quantification of PBMC concentration of tyrosine kinase inhibitors imatinib, dasatinib and nilotinib. A simple PBMC isolation and extraction procedure were applied on 10-14 mL of blood aliquots. Chromatographic separation of drugs and Internal Standard (quinoxaline) was achieved with a gradient (acetonitrile and water + formic acid 0.05%) on a C18 reverse phase analytical column with 25 min of analytical run, at flow rate of 0.25 mL/min. Mean intra-and inter-day precision for all compounds were 8.76 and 12.20%; mean accuracy was -3.86%; extraction recovery ranged within 79 and 91%. Calibration curves ranged from 50.0 to 0.25 ng. The limit of quantification was set at 0.25 ng for all the analyzed drugs.This novel developed methodology allows a specific, sensitive and reliable simultaneous intracellular determination of the three tyrosine kinase inhibitors imatinib, dasatinib and nilotinib in a single chromatographic run, useful for drugs estimation in PBMC of patients affected by chronic myeloid leukemia.

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Dasatinib: A tyrosine kinase inhibitor for the treatment of chronic myelogenous leukemia and philadelphia chromosome—positive acute lymphoblastic leukemia

Cited by 192 publications

References 50 publications

Combination of Fludarabine and Imatinib Induces Apoptosis Synergistically Through Loss of Mitochondrial Membrane Potential and Increases in Caspase-3 Enzyme Activity in Human K562 Chronic Myleloid Leukemia Cells

Combination of Fludarabine and Imatinib Induces Apoptosis Synergistically Through Loss of Mitochondrial Membrane Potential and Increases in Caspase-3 Enzyme Activity in Human K562 Chronic Myleloid Leukemia Cells

Acute Renal Failure under Dasatinib Therapy

HPLC–MS method for the simultaneous quantification of the antileukemia drugs imatinib, dasatinib and nilotinib in human peripheral blood mononuclear cell (PBMC)

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