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Large Scale Non-targeted Metabolomic Profiling of Serum by Ultra Performance Liquid Chromatography-Mass Spectrometry UPLC-MS
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Update on metabolism of abemaciclib: In silico, in vitro, and in vivo metabolite identification and characterization

Disha Thakkar1, Abhijeet S Kate1

  • 1National Institute of Pharmaceutical Education and Research-Ahmedabad, Palaj Gandhinagar Gujarat, India.

Drug Testing and Analysis
|November 8, 2019
PubMed

Insights

This study investigated the metabolic fate of abemaciclib, a breast cancer drug. Researchers identified 12 metabolites, including human-specific ones, through in vitro and in vivo analyses.

Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Mass Spectrometry

Background:

  • Abemaciclib is an FDA-approved treatment for metastatic breast cancer.
  • Limited information exists on abemaciclib's metabolites.
  • Understanding drug metabolism is crucial for efficacy and safety.

Purpose of the Study:

  • To investigate the in vitro and in vivo metabolic fate of abemaciclib.
  • To identify and characterize abemaciclib metabolites and their pathways.
  • To compare metabolism across different species and matrices.

Main Methods:

  • Prediction of metabolism sites using Xenosite web predictor.
  • Identification of in vitro metabolites using rat liver microsomes, S9 fractions, and human liver microsomes.
  • Detection of in vivo metabolites in rat plasma, urine, and feces using high-resolution mass spectrometry.

Main Results:

  • A total of 12 putative metabolites (11 phase I, 1 phase II) were identified.
  • Metabolism occurred via hydroxylation, N-oxidation, N-dealkylation, oxidative deamination, reduction, and sulfate conjugation.
  • Eleven metabolites were found in human liver microsomes, with four (M7, M8, M9, M11) being human-specific.

Conclusions:

  • The study elucidated the metabolic pathways of abemaciclib.
  • Identified human-specific metabolites provide insights into species differences.
  • This research contributes to a better understanding of abemaciclib's pharmacokinetic profile.
Keywords:
S9 fractionsabemaciclibhigh resolution mass spectrometryliver microsomesmetabolite identification

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