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Therapeutic Drug Monitoring: A New Hope for Individualised Treatment with Venetoclax

Yue Tang1,2, Shuojiao Li3, Peng Rao1,2

  • 1Department of Pharmacy, the First Affiliated Hospital of Anhui Medical University, Hefei, 230022, Anhui Province, China.

Current Drug Targets
|July 18, 2025
PubMed

Insights

Therapeutic drug monitoring (TDM) of venetoclax (VEN), a BCL-2 inhibitor, is crucial for optimizing treatment in hematologic malignancies. Understanding VEN pharmacokinetics and influencing factors aids in personalized therapy and improved patient outcomes.

Area of Science:

  • Pharmacology
  • Oncology
  • Drug Metabolism

Background:

  • B-cell lymphoma-2 (BCL-2) is critical in apoptosis regulation.
  • Venetoclax (VEN), a BCL-2 inhibitor, treats hematologic malignancies.
  • VEN metabolism is influenced by CYP3A, food, and liver function.

Purpose of the Study:

  • To review VEN pharmacokinetics and influencing factors.
  • To explore drug-drug interactions and TDM advancements for VEN.
  • To provide a basis for TDM-guided individualized VEN therapy.

Main Methods:

  • Literature review of VEN pharmacokinetics.
  • Analysis of factors affecting VEN metabolism.
  • Summary of TDM studies and drug interactions.

Main Results:

  • Significant interindividual variability in VEN plasma concentrations exists.
  • VEN exposure correlates with efficacy, but adverse effect link is debated.
  • Optimal therapeutic windows for VEN in different cancers require further research.

Conclusions:

  • TDM can guide individualized VEN therapy.
  • Further research is needed to define optimal therapeutic windows.
  • Understanding VEN pharmacokinetics is key for effective treatment.
Keywords:
CYP3A.Venetoclaxchronic lymphocytic leukemiadrug-drug interactionspharmacokineticstherapeutic drug monitoring

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