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

B-cell lymphoma-2 (BCL-2) plays a key role in regulating apoptosis. Venetoclax(VEN), a BCL-2 inhibitor, has been approved for the treatment of a variety of hematologic malignancies.VEN is primarily metabolized by CYP3A, and a variety of factors (such as CYP3A inhibitors,as well as food and hepatic functions) have been reported to significantly influence themetabolic process. There is significant interindividual variability in VEN plasma concentrations,and studies have shown that its exposure levels are correlated with efficacy, although the relationshipwith adverse effects remains controversial. The value of applying of therapeutic drug monitoring(TDM) in individualized VEN therapy has been confirmed by some studies, but the optimaltherapeutic window for different malignancies is still unclear. This review summarizes the pharmacokineticcharacteristics, along with the factors influencing VEN pharmacokinetics, drug-drug interactions,and advancements in TDM research on VEN, aiming to provide a theoretical basis forTDM-guided individualized therapy.