Determination of bezafibrate in human plasma by using liquid chromatography-tandem mass spectrometry

Nihal, Saraner; Fikirdesici, Ezgi; Güney, Berrak; Onursal, Saglam

doi:10.15761/brr.1000124

Cited by 2 publications

(2 citation statements)

References 3 publications

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“…Specificity, accuracy, linearity, precision, stability, and recovery were among the validation criteria. [12][13][14][15][16][17][18][19]…”

Section: Validation Of the Analytical Methodsmentioning

confidence: 99%

“…Eight calibration standards with concentrations ranging from 0.2 to 3200 ng/mL in human plasma and four quality control (QC) samples with concentrations of 0.2, 0.6, 1600, and 2400 ng/mL were. 12 produced. After vortexing for one minute and transferring 1.0 mL aliquots into borosilicate glass (13 x 100 mm) culture tubes, the calibration standards and quality control samples were kept at a temperature of -20℃ until they were utilized.…”

Section: Quality Control and Standard Solutionsmentioning

confidence: 99%

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Stability Indicating an LC-MS/MS Method Development and Validation for the Quantification of Capmatinib in Human Plasma

Panigrahi

2023

IJPQA

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A linear and accurate liquid chromatographic tandem mass spectrometric (LC-MS/MS) technique for the quantitation of capmatinib in plasma was developed and subjected for validation. Canagliflogin was employed as an internal standard (IS). Extraction of plasma was executed utilizing 5 mL of ethyl acetate solvent. Analysis was performed Zorbax ODS (50 mm × 2.1 mm x 3 μ) stationary phase at room conditions and a movable solvent composition of 0.1% HCOOH, acetonitrile and methyl alcohol (15:50:35). The flowing rate of the movable phase was 0.4 mL/min. Drug and IS were identified in positive mode of ionization with electrospray mode to get the mass transitions of (m/z): Capmatinib, 413.15/386.14 and canagliflogin (IS), 445.15/267.12. The correlation between capmatinib concentrations and their respective peak proportions to canagliflogin was a straight line over 0.2 to 3200 ng/mL concentration levels. Intra day and inter-day precisions were ≤5.18% for capmatinib. Inter and intra day bias were within the range of −4.17 to 4.53%. The mean measured extraction recovery of capmatinib was 99.23%. Recovery of IS was 98.31%. Capmatinib was subjected for long-term, freeze thaw, bench top, short-term stability, auto-sampler, dry extract, and stock solution stability at low QC and high QC levels and it was stable at all these conditions. The established technique can be utilized to regularly quantitfy of capmatinib in plasma samples in industries, forensic labs, and clinical research organizations.

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“…Specificity, accuracy, linearity, precision, stability, and recovery were among the validation criteria. [12][13][14][15][16][17][18][19]…”

Section: Validation Of the Analytical Methodsmentioning

confidence: 99%

Section: Quality Control and Standard Solutionsmentioning

confidence: 99%

Stability Indicating an LC-MS/MS Method Development and Validation for the Quantification of Capmatinib in Human Plasma

Panigrahi

2023

IJPQA

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A sulfonimide derivative of bezafibrate as a dual inhibitor of cyclooxygenase-2 and PPARα

Ammazzalorso,

Tacconelli,

Contursi

et al. 2024

Front. Pharmacol.

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BackgroundPPARα and cyclooxygenase (COX)-2 are overexpressed in certain types of cancer. Thus, developing a dual inhibitor that targets both could be more effective as an anticancer agent than single inhibitors. We have previously shown that an analog of the bezafibrate named AA520 is a PPARα antagonist. Herein, we report the identification of AA520 as a potent COX-2 inhibitor using in silico approaches. In addition, we performed a thorough pharmacological characterization of AA520 towards COX-1 and COX-2 in different in vitro models.MethodsAA520 was characterized for inhibiting platelet COX-1 and monocyte COX-2 activity in human whole blood (HWB) and for effects on lipidomics of eicosanoids using LC-MS/MS. The kinetics of the interaction of AA520 with COX-2 was assessed in the human colon cancer cell line, HCA-7, expressing only COX-2, by testing the COX-2 activity after extensive washing of the cells. The impact of AA520 on cancer cell viability, metabolic activity, and cytotoxicity was tested using the MTT reagent.ResultsIn HWB, AA520 inhibited in a concentration-dependent fashion LPS-stimulated leukocyte prostaglandin (PG) E2 generation with an IC50 of 0.10 (95% CI: 0.05–0.263) μM while platelet COX-1 was not affected up to 300 μM. AA520 did not affect LPS-induced monocyte COX-2 expression, and other eicosanoids generated by enzymatic and nonenzymatic pathways. AA520 inhibited COX-2-dependent PGE2 generation in the colon cancer cell line HCA7. Comparison of the inhibition of COX-2 and its reversibility by AA520, indomethacin (a time-dependent inhibitor), acetylsalicylic acid (ASA) (an irreversible inhibitor), and ibuprofen (a reversible inhibitor) showed that the compound is acting by forming a tightly bound COX-2 interaction. This was confirmed by docking and molecular dynamics studies. Moreover, AA520 (1 μM) significantly reduced MTT in HCA7 cells.ConclusionWe have identified a highly selective COX-2 inhibitor with a unique scaffold. This inhibitor retains PPARα antagonism at the same concentration range. It has the potential to be effective in treating certain types of cancer, such as hepatocellular carcinoma (HCC) and renal cell carcinoma (RCC), where COX-2 and PPARα are overexpressed.

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Determination of bezafibrate in human plasma by using liquid chromatography-tandem mass spectrometry

Cited by 2 publications

References 3 publications

Stability Indicating an LC-MS/MS Method Development and Validation for the Quantification of Capmatinib in Human Plasma

Stability Indicating an LC-MS/MS Method Development and Validation for the Quantification of Capmatinib in Human Plasma

A sulfonimide derivative of bezafibrate as a dual inhibitor of cyclooxygenase-2 and PPARα

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