Abstract: Ritonavir-boosted atazanavir is a victim of drug–drug interaction with rifampicin. In a recent dose escalation clinical trial, we showed that increasing atazanavir/ritonavir to 300/100mg b.i.d. compensates for reduced drug exposure in plasma due to rifampicin, but the intracellular effects remained unexplored. This sub-study investigated the intracellular penetration of atazanavir/ritonavir and dolutegravir into peripheral blood mononuclear cells (PBMC).