Novel Bruton Tyrosine Kinase Inhibitor Acalabrutinib Quantification by validated LC-MS/MS method: An Application to Pharmacokinetic Study in Sprague Dawley rats

Publication date: Available online 11 November 2018Source: Journal of Pharmaceutical and Biomedical AnalysisAuthor(s): Shruti Surendran, David Paul, Sunil Pokharkar, Sagar Choulwar, Abhijeet Deshpande, Sanjeev Giri, N. SatheeshkumarAbstractUSFDA has approved a novel bruton tyrosine kinase (BTK) inhibitor acalabrutinib (ACA) for the treatment of mantle cell lymphoma in adults. ACA is more potent and selective with fewer side effects compared to other bruton tyrosine kinase inhibitors. In the current work a highly sensitive, selective and specific LC-MS/MS method for the estimation of acalabrutinib (ACA) in rat plasma was developed. Agilent Eclipse Plus C 8 column (50 mm × 4.6 mm, μm), with gradient elution using 10 mM ammonium formate and acetonitrile as mobile phase at a flow rate of 0.6 mL/min was used for the chromatographic separation. The ion transitions were quantified in positive mode with MRM transition of 466.1→372.3 for ACA and 236.8→194.0 for internal standard (IS). Solid phase extraction process was used as sample preparation approach. The method was validated according to US FDA bioanalytical guidelines. The method provided good linearity over the range of 0.2-199.14 ng/mL for ACA with short run time of 4 min.. The method offers very high sensitivity (0.2 ng/mL) and was free from matrix interferences. The validated LC-MS/MS method was successfully applied for in vivo pharmacokinetic ...
Source: Journal of Pharmaceutical and Biomedical Analysis - Category: Drugs & Pharmacology Source Type: research

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