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∗ Corresponding author at: Jubilant Biosys, Industrial Suburb, Yeshwanthpur,Ġ731-7085/© 2018 Elsevier B.V. Second generation anti-androgen receptor antagonists like enzalutamide (Fig. Such as CYP17A1 inhibitor, abiraterone acetate and new class of Many of the new treatments target androgen receptor signaling Of the disease termed metastatic castration-resistant prostate cancer (mCRPC), with a median survival of less than two years. Or surgical castration, most patients invariably progress to a state It hasīeen established that up to 80% of prostate carcinomas depends Leading cause for cancer deaths among men worldwide. Prostate cancer is the most common malignancy and the second Intravenous pharmacokinetic study in mice. All the analytes were found to be stable under different conditions. The intra- and inter-batch accuracy and precision (% CV) across qualityĬontrols varied from 88.5–111% and 1.13–13.1, 85.4–106% and 3.15–14.3, respectively for all the analytes. The calibration cu rves were linear from 1.07 to 2000 ng/mL Triple quadrupole mass spectrometer following the transitions: m/z 465 → 209, 451 → 195, 478 → 450,ģ99 → 178, 397 → 194 and 481 → 453 for enzalutamide, N-desmethylenzalutamide, apalutamide, darolutamide, ORM-15341 and the I.S. Detection and quantitation was done by multiple reaction monitoring on a The analytes and the internal standard (I.S.: apalutamide-d3 ) were extracted from 50 ␮L mice plasmaīy simple protein precipitation using acetonitrile, followed by chromatographic separation using anĪtlantis C18 column with an isocratic mobile (0.2% formic acid:acetonitrile 30:70, v/v) at a flow rate ofĠ.8 mL/min within 2.5 min. Of enzalutamide, N-desmethylenzalutamide (active metabolite of enzalutamide), apalutamide, darolutamide and ORM-15341 (active metabolite of darolutamide) in mice plasma as per regulatory guidelines. Medicinal Chemistry Department, Jubilant Biosys Ltd, Industrial Suburb, Yeshwanthpur, Bangalore-560 022, IndiaĪ sensitive and rapid LC–MS/MS method was developed and validated for the simultaneous quantitation Sulochana a, Neeraj Kumar Saini a, Prasanthi Daram a, Sai Babu Polina b ,ĭrug Metabolism and Pharmacokinetics, Jubilant Biosys Ltd, Industrial Suburb, Yeshwanthpur, Bangalore-560 022, India Journal homepage: Validation of an LC–MS/MS method for simultaneous quantitation ofĮnzalutamide, N-desmethylenzalutamide, apalutamide, darolutamideĪnd ORM-15341 in mice plasma and its application to a mice Journal of Pharmaceutical and Biomedical Analysis Journal of Pharmaceutical and Biomedical Analysis 156 (2018) 170–180Ĭontents lists available at ScienceDirect