LC-MS/MS determination of erdafitinib in human plasma after SPE: Investigation of the method greenness

Elawady, Tarek; Khedr, Alaa; El‐Enany, N.; Belal, F.

doi:10.1016/j.microc.2019.104555

Cited by 14 publications

(6 citation statements)

References 10 publications

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“…The mobile phase gradient elution method could complete a detection in 2 min. The detection was faster than that reported ( Elawady et al, 2020 ).…”

Section: Discussioncontrasting

confidence: 53%

“…Improving the pretreatment method could not only protect the detection instrument from pollution and prolong its service life but also reduce the detection matrix and improve the sensitivity and selectivity. It was reported that the plasma was pretreated by solid phase extraction (SPE) in the process of determination of erdafitinib in the human plasma with LC-MS/MS ( Elawady et al, 2020 ). Because SPE needed special extraction column, the treatment process was relatively cumbersome.…”

Section: Discussionmentioning

confidence: 99%

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The Effect of Posaconazole and Isavuconazole on the Pharmacokinetics of Erdafitinib in Beagle Dogs by UPLC-MS/MS

Ruan

Wang

et al. 2021

Front. Pharmacol.

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Objective: A robust, quick, and reliable ultra-performance liquid chromatography–tandem mass spectrometry (UPLC-MS/MS) method for the quantification of erdafitinib in beagle dog plasma was developed and validated to evaluate the changes of posaconazole and isavuconazole on the pharmacokinetics of erdafitinib in beagle dogs, respectively.Methods: This experiment adopted a three-period self-control experimental design. In the first period (group A), erdafitinib was orally administered to six beagle dogs at a dose of 4 mg/kg. In the second period (group B), the same six beagle dogs were orally given posaconazole at a dose of 7 mg/kg, and after 30 min, erdafitinib was orally given. In the third period (group C), isavuconazole at a dose of 7 mg/kg was given orally, and then, erdafitinib was orally given. At the different time points after erdafitinib was given in the three periods, the blood samples were collected. The concentration of erdafitinib was detected by the developed UPLC-MS/MS method. DAS 2.0 was used to calculate the pharmacokinetic parameters of erdafitinib.Results: Erdafitinib had a good linear relationship in the range of 1–500 ng/ml, and the lower limit of quantification was 1 ng/ml. The precision, accuracy, extraction recovery, matrix effect, and stability meet the requirements of the guiding principles. After erdafitinib was combined with posaconazole, the Cmax and AUC0→t of erdafitinib increased by 27.19% and 47.62%, respectively, and the t1/2 was prolonged to 6.33 h. After erdafitinib was combined with isavuconazole, the Cmax and AUC0→t of erdafitinib increased by 23.13% and 54.46%, respectively, and the t1/2 was prolonged to 6.31 h.Conclusion: A robust and reliable UPLC-MS/MS method was fully optimized and developed to detect the plasma concentration of erdafitinib in beagle dogs. Posaconazole and isaconazole could inhibit the metabolism of erdafitinib in beagle dogs and increase the plasma exposure of erdafitinib.

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“…The mobile phase gradient elution method could complete a detection in 2 min. The detection was faster than that reported ( Elawady et al, 2020 ).…”

Section: Discussioncontrasting

confidence: 53%

Section: Discussionmentioning

confidence: 99%

The Effect of Posaconazole and Isavuconazole on the Pharmacokinetics of Erdafitinib in Beagle Dogs by UPLC-MS/MS

Ruan

Wang

et al. 2021

Front. Pharmacol.

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“…LC/MS/MS is a commonly used method in bioequivalence studies [27][28][29][30][31][32][33] for drugs detection in the plasma because of the high accuracy and sensitivity of the mass detector. Additionally, mass spectrophotometric detector is preferred over the UV and Refractive index (RI) detectors in terms of sensitivity as it measures in nano-scale levels [34,35].…”

Section: Resultsmentioning

confidence: 99%

A validated LC–MS/MS method for analysis of Cabergoline in human plasma with its implementation in a bioequivalent study: investigation of method greenness

et al. 2022

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Cabergoline (CAB) is effective prolactin lowering drug. Evaluation of the bioequivalence for the new test product (0.5 mg CAB film-coated tablets) in Egypt is strongly needed for approval of the drug by the official health authority. Therefore, a highly sensitive and rapid (LC–MS/MS) method was validated for CAB analysis in human plasma. CAB was extracted from plasma via diethyl ether using Quetiapine (QUE) as an internal standard. Multiple reaction monitoring (MRM) in positive ion mode was used, m/z 452.3 → 381.2 for CAB and 384.2 → 253.1 for QUE. Separation was accomplished on a reversed-phase C18. FDA procedures for the bio-analytical method were followed. The method was used in the bioequivalence study to compare the test product (0.5 mg CAB) versus Dostinex tablets, on 24 healthy Egyptian volunteers. The total analysis time was 5.5 min for each sample which permits analysis of various samples per day. The linearity range was from 2.00 to 200.00 pg/mL for CAB. LOD and LOQ were found to be 0.5 and 1.6 pg/mL, respectively. The final greenness numerical value was 0.63 using AGREE tool. The results of pharmacokinetic parameter Tmax were 2.17, and 2.33 h; for test and reference products, respectively. The generic formulation of test product is considered bioequivalent to the reference product Dostinex 0.5 mg tablets and satisfies the requirements of the Egyptian market. The merits of the method over the previous published methods are low cost; availability of cheap internal standard; rapidness; use of acetonitrile-free solvents mobile phase.

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“…Successful recapitulation of the nominal mass EPI spectrum in our high-resolution QTOF-MS (Figure ) coupled together with mass accuracies well below the mass tolerance threshold of 5 ppm (Table ) gave us confidence in the predicted elemental compositions of the parent and product ions for structural elucidation of the ERD-derived GSH adduct. Notably, as the fragment ion at m / z 447.2496 as well as 388.1751 and 362.1608 corresponded to the parent and product ions of ERD, it indicated that the glutathionyl moiety was alkylated directly to the ERD core structure. Consequently, we proposed that the bioactivation of ERD resulting in MBI of CYP3A might involve epoxidation of its quinoxaline ring (Scheme ).…”

Section: Discussionmentioning

confidence: 99%

Mechanism-Based Inactivation of Cytochrome P450 3A4 and 3A5 by the Fibroblast Growth Factor Receptor Inhibitor Erdafitinib

Tang

Teng

Koh

et al. 2021

Chem. Res. Toxicol.

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Erdafitinib (ERD) is a first-in-class pan inhibitor of fibroblast growth factor receptor 1–4 that has garnered global regulatory approval for the treatment of advanced or metastatic urothelial carcinoma. Although it has been previously reported that ERD elicits time-dependent inhibition (TDI) of cytochrome P450 (P450) 3A4 (CYP3A4), the exact biochemical nature underpinning this observation remains obfuscated. Moreover, it is also uninterrogated if CYP3A5its highly homologous counterpartcould be susceptible to such interactions. Mechanism-based inactivation (MBI) of P450 is a unique subset of TDI that hinges on prior bioactivation of the drug to a reactive intermediate and possesses profound clinical and toxicological implications due to its irreversible nature. Here, we investigated and confirmed that ERD inactivated both CYP3A isoforms in a time-, concentration-, and NADPH-dependent manner with K I, k inact, and partition ratio of 4.01 and 10.04 μM, 0.120 and 0.045 min–1, and 32 and 55 for both CYP3A4 and CYP3A5, respectively, when rivaroxaban was employed as the probe substrate. Co-incubation with an alternative substrate or direct inhibitor of CYP3A attenuated the rate of inactivation, whereas the addition of glutathione or catalase did not induce such protection. The lack of enzyme activity recovery following dialysis for 4 h and oxidation with potassium ferricyanide combined with the lack of a Soret peak in spectral scans collectively substantiated that ERD is an irreversible covalent MBI of CYP3A. Finally, glutathione trapping and high-resolution mass spectrometry experiments illuminated a plausible bioactivation mechanism of ERD by CYP3A arising from metabolic epoxidation of its quinoxaline ring.

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LC-MS/MS determination of erdafitinib in human plasma after SPE: Investigation of the method greenness

Cited by 14 publications

References 10 publications

The Effect of Posaconazole and Isavuconazole on the Pharmacokinetics of Erdafitinib in Beagle Dogs by UPLC-MS/MS

The Effect of Posaconazole and Isavuconazole on the Pharmacokinetics of Erdafitinib in Beagle Dogs by UPLC-MS/MS

A validated LC–MS/MS method for analysis of Cabergoline in human plasma with its implementation in a bioequivalent study: investigation of method greenness

Mechanism-Based Inactivation of Cytochrome P450 3A4 and 3A5 by the Fibroblast Growth Factor Receptor Inhibitor Erdafitinib

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