Data from: A highly sensitive LC-MS/MS method to determine novel Bruton's tyrosine kinase inhibitor spebrutinib: application to metabolic stability evaluation

Spebrutinib (SBT) is a Bruton's tyrosine kinase inhibitor. SBT is
currently in phase II and phase I clinical trials for the management of
rheumatoid arthritis and chronic lymphocytic leukaemia, respectively. We
developed and validated a liquid chromatography tandem mass spectrometry
analytical method to quantify SBT and investigate its metabolic stability.
SBT and the naquotinib as internal standard were isocratically eluted on a
C18 column. The linearity of the developed method is 5-500 ng/mL (r2≥
0.9999) in the human liver microsomes (HLMs) matrix. Good sensitivity was
approved by the very low limit of detection (0.39 ng/mL). Inter- and
intra- assay accuracy values of -1.41 to 12.44 and precision values of
0.71 to 4.78%, were obtained. SBT was found to have an in vitro half-life
(82.52 min) and intrinsic clearance (8.4 µL/min/mg) as computed following
its incubation with HLMs. The latter finding, hypothesize that SBT could
be deliberately expelled from the body unlike other related tyrosine
kinase inhibitors. So, drug plasma level and kidney function should be
monitored because of potential bioaccumulation. To the best of our
knowledge, this is considered the first analytical method for SBT
quantification using LC-MS/MS with application to metabolic stability
evaluation.