Optimizing valganciclovir dosing strategies: a comprehensive review.
1Department of Pharmacy, Kobe University Hospital, Kobe, Japan.
Expert Review of Clinical Pharmacology
|March 2, 2026
Summary
Therapeutic drug monitoring (TDM) for valganciclovir (VGCV) can optimize ganciclovir (GCV) therapy. Exposure-guided dosing improves efficacy and safety, but challenges in limited sampling strategies and microsampling need addressing for widespread clinical use.
Area of Science:
- Pharmacology
- Infectious Diseases
- Clinical Pharmacy
Background:
- Valganciclovir (VGCV) is an oral prodrug rapidly converted to ganciclovir (GCV).
- GCV is crucial for preventing and treating cytomegalovirus (CMV) infections.
- Current clinical practice lacks therapeutic drug monitoring (TDM) for GCV, despite its known impact on efficacy and toxicity.
Purpose of the Study:
- To review current knowledge on GCV pharmacokinetics, exposure-efficacy/toxicity relationships, and TDM evidence.
- To summarize methods for clinical TDM implementation, including limited sampling strategies (LSS) and microsampling.
- To discuss the role of NUDT15 polymorphisms in GCV toxicity.
Main Methods:
- Comprehensive literature review of studies published before 2025.
- Analysis of population pharmacokinetics of oral VGCV.
- Evaluation of evidence supporting TDM for GCV.
Main Results:
- GCV exposure is linked to both therapeutic efficacy and potential toxicity.
- Exposure-guided dosing, targeting an AUC of 40-60 μg·h/mL, shows promise for optimizing VGCV therapy.
- NUDT15 polymorphisms are associated with GCV toxicity.
Conclusions:
- Optimizing VGCV therapy through TDM is feasible and beneficial.
- Standardization of LSS and advancements in microsampling technologies are crucial for practical VGCV dose optimization.
- Further research is needed to overcome implementation challenges for universal application of TDM in VGCV therapy.
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