Simultaneous Measurement of Sirolimus and Everolimus in Whole Blood by HPLC with Ultraviolet Detection

Khoschsorur, G.

doi:10.1373/clinchem.2005.051151

Cited by 20 publications

(9 citation statements)

References 26 publications

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“…To plot a standard curve, six concentrations of everolimus (156.25, 312.5, 625, 1,250, 2,500, and 5,000 ng/mL) were prepared in whole blood collected from mice that were not given the drug. Everolimus was extracted from blood according to a previously reported method (25). In the extraction process, 800 ng of ascomycin (Wako) was added to the whole blood samples as an internal standard.…”

Section: Determination Of Everolimus Concentration By Hplcmentioning

confidence: 99%

Circadian Regulation of mTOR by the Ubiquitin Pathway in Renal Cell Carcinoma

et al. 2014

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Circadian clock systems regulate many biologic functions, including cell division and hormone secretion in mammals. In this study, we explored the effects of circadian control on the pivot cell growth regulatory mTOR, the activity of which is deregulated in tumor cells compared with normal cells. Specifically, we investigated whether the antitumor effect of an mTOR inhibitor could be improved by changing its dosing schedule in RenCa tumorbearing mice. Active, phosphorylated mTOR displayed a 24-hour rhythm, and levels of total mTOR protein (but not mRNA) also showed a circadian rhythm in RenCa tumor masses. Through investigations of the oscillation mechanism for mTOR expression, we identified the ubiquitination factor Fbxw7 as an mTOR regulator that oscillated in its expression in a manner opposite from mTOR. Fbxw7 transcription was regulated by the circadian regulator D-site-binding protein. Notably, administration of the mTOR inhibitor everolimus during periods of elevated mTOR improved survival in tumor-bearing mice. Our findings demonstrate that the circadian oscillation of mTOR activity is regulated by circadian clock systems, which influence the antitumor effect of mTOR inhibitors. Cancer Res; 74(2); 543-51. Ó2013 AACR.

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Section: Determination Of Everolimus Concentration By Hplcmentioning

confidence: 99%

Circadian Regulation of mTOR by the Ubiquitin Pathway in Renal Cell Carcinoma

et al. 2014

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“…Interestingly, steady-state serum levels reached by this compound in in vivo treated patients [40,41,42] are much higher than those demonstrated to be able to induce γ-globin gene expression in erythroid precursor cells from β-thalassaemia patients. Therefore, everolimus might be considered for pre-clinical trials to determine whether it has an effect on HbF production.…”

Section: Discussionmentioning

confidence: 99%

Everolimus Is a Potent Inducer of Erythroid Differentiation and γ-Globin Gene Expression in Human Erythroid Cells

Zuccato¹,

Bianchi²,

Borgatti³

et al. 2006

Acta Haematol

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We studied the effects of everolimus on the erythroid differentiation of human leukaemic K562 cells and on the cultures of erythroid progenitors derived from the peripheral blood of β-thalassaemia patients. A quantitative real-time reverse-transcription polymerase chain reaction assay was employed for the quantification of the accumulation of globin mRNAs. The results obtained demonstrate that everolimus is a potent inducer of the erythroid differentiation of K562 cells. Erythroid induction is associated with an increase in α- and γ-globin mRNAs. In erythroid precursor cells from 4 β-thalassaemia patients, everolimus stimulated a preferential increase (ranging from 1.8- to 7.2-fold) in γ-globin mRNA. Only minor effects were observed on the expression of α-globin genes. These results, in our opinion, are of interest as this compound is already employed in clinical trials as an anti-rejection agent following kidney transplantation. These data suggest that everolimus warrants further evaluation as a potential therapeutic drug in the treatment of β-thalassaemia.

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“…Therefore, results obtained with the immunoassays are generally higher as compared to those measured with chromatographic methods [7]. For methods using chromatography, there are few using UV detection [8]. Today, mostly tandem MS is used as detection method 1570-0232/$ -see front matter © 2010 Elsevier B.V. All rights reserved.…”

Section: Introductionmentioning

confidence: 99%