Metabolomics, metabolic flux analysis and cancer pharmacology

Lingfan Liang, Fei Sun, Hongbo Wang, Zeping Hu

Research output: Contribution to journalReview articlepeer-review

44 Scopus citations


Metabolic reprogramming is a hallmark of cancer and increasing evidence suggests that reprogrammed cell metabolism supports tumor initiation, progression, metastasis and drug resistance. Understanding metabolic dysregulation may provide therapeutic targets and facilitate drug research and development for cancer therapy. Metabolomics enables the high-throughput characterization of a large scale of small molecule metabolites in cells, tissues and biofluids, while metabolic flux analysis (MFA) tracks dynamic metabolic activities using stable isotope tracer methods. Recent advances in metabolomics and MFA technologies make them powerful tools for metabolic profiling and characterizing metabolic activities in health and disease, especially in cancer research. In this review, we introduce recent advances in metabolomics and MFA analytical technologies, and provide the first comprehensive summary of the most commonly used isotope tracing methods. In addition, we highlight how metabolomics and MFA are applied in cancer pharmacology studies particularly for discovering targetable metabolic vulnerabilities, understanding the mechanisms of drug action and drug resistance, exploring potential strategies with dietary intervention, identifying cancer biomarkers, as well as enabling precision treatment with pharmacometabolomics.

Original languageEnglish (US)
Article number107827
JournalPharmacology and Therapeutics
StatePublished - Aug 2021
Externally publishedYes


  • cancer
  • drug discovery
  • metabolic flux
  • metabolomics
  • pharmacology

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


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