Therapeutic drug monitoring in highly active antiretroviral therapy

Expert Opin Drug Saf. 2010 Sep;9(5):743-58. doi: 10.1517/14740331003767395.


Importance of the field: Despite the efficacy of combination antiretroviral therapy (ART), a large proportion of patients living with HIV/AIDS on ART does not achieve or maintain adequate virological suppression. Therapeutic drug monitoring (TDM) has been utilised to improve treatment outcomes of ART.

Areas covered in the review: The potential incorporation of TDM into the clinical HIV management is supported by the existing relationship between drug exposure and efficacy/toxicity, the high inter-patient variability pharmacokinetics, and the accurate, specific and rapid method for drug level determination. The current status of TDM in ART is reviewed in this article with discussions on its feasibility, potential use and limitations.

What the reader will gain: Mounting evidence from clinical trials has indicated the potential use of TDM in reducing the rates of treatment failure and adverse effect, avoiding the drug interactions, and special populations, such as children, pregnant women and patients with co-infections. TDM may play an important role even in resource-limited settings, to safeguard expanded use of bioequivalent generic antiretroviral drugs and avoid drug interactions with traditional Chinese medicines.

Take home message: TDM is still in the centre of controversy in that several critical issues need to be addressed, such as limited adherence assessment, inappropriate response predictors, insufficient validation of target concentration windows and lack of the quality control of assay. The utility of TDM will remain experimental until more data are obtained from large clinical trials showing the benefit of TDM.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adult
  • Anti-HIV Agents / adverse effects
  • Anti-HIV Agents / blood
  • Anti-HIV Agents / pharmacokinetics
  • Anti-HIV Agents / therapeutic use
  • Antiretroviral Therapy, Highly Active*
  • Biotransformation
  • Child
  • Clinical Trials as Topic
  • Cytochrome P-450 Enzyme System / metabolism
  • Developing Countries
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Drug Monitoring*
  • Drugs, Chinese Herbal / pharmacokinetics
  • Female
  • Genetic Variation
  • HIV Infections / complications
  • HIV Infections / drug therapy
  • Humans
  • Kidney Diseases / complications
  • Kidney Diseases / metabolism
  • Liver Diseases / complications
  • Liver Diseases / metabolism
  • Male
  • Multicenter Studies as Topic
  • Pregnancy
  • Pregnancy Complications, Infectious / drug therapy
  • Substance Abuse, Intravenous / complications


  • Anti-HIV Agents
  • Drugs, Chinese Herbal
  • Cytochrome P-450 Enzyme System