Characterization of in vitro metabolites of TM‐2, a potential antitumor drug, in rat, dog and human liver microsomes using liquid chromatography/tandem mass spectrometry

Abstract

Hydroxylation is the major biotransformation of the TM-2 pathway in vitro. CYP3A4 may play a dominant role in the formation of M2 in liver microsomes. The knowledge of the metabolic pathways of TM-2 is important to support further research of TM-2.

Identification of metabolites of the novel anti‐tumor drug candidate MDH‐7 in rat urine by liquid chromatography coupled with triple quadrupole linear ion trap mass spectrometry

“…It is well known that unraveling in vivo metabolite profiles are challenging tasks, due to the low concentrations of metabolites, and to the complexity of biological matrices . Liquid chromatography coupled with tandem mass spectrometry (LC/MS/MS) has proven to be a successful approach for the structural elucidation of metabolites in biological matrices due to its high selectivity and sensitivity.…”

Elucidation of a CGP7930 in vitro metabolite by liquid chromatography/electrospray ionization quadrupole time‐of‐flight tandem mass spectrometry

“…The investigations of in vivo and in vitro metabolites are very critical in the development of drug candidates . Liquid chromatography coupled with tandem mass spectrometry (LC/MS/MS) has nowadays become a very important technique to probe and characterize metabolites for drug study .…”

“…Such in vitro studies are significantly useful for the explanation of metabolite generation and the development of toxicology studies. Furthermore, it also provides data for predicting pharmacokinetic variability and potential drug‐drug interactions before clinical trials in humans …”

“…The investigations of in vivo and in vitro metabolites are very critical in the development of drug candidates. [13,14] Liquid chromatography coupled with tandem mass spectrometry (LC/MS/MS) has nowadays become a very important technique to probe and characterize metabolites for drug study. [15,16] Tandem mass spectrometry has been successfully applied to the structural elucidation of metabolites by coupling a HPLC (high-performance liquid chromatography) column with a triple-quadrupole (QQQ), [17,18] a quadrupole ion trap (QIT), [19,20] or a quadrupole time-of-flight (QTOF) [21,22] mass spectrometer.…”

“…Furthermore, it also provides data for predicting pharmacokinetic variability and potential drugdrug interactions before clinical trials in humans. [14,27,28] In this work, we have developed a LC/ESI-QTOF-MS/MS (liquid chromatography/electrospray ionization quadrupole time-of-flight tandem mass spectrometry) method to investigate the major CGP7930 in vitro metabolite by a liver microsomal incubation system. The accurate molecular weight of CGP7930 metabolite was measured by a TOFMS full scan with high resolution.…”