Gender and age are characterised by physiological differences, which can affect drug pharmacokinetics. However, these effects cannot be fully quantified for antiretroviral drugs, because women and the elderly are often underrepresented in clinical trials. This lecture will critically review the current literature about gender- and age-related pharmacokinetic differences for HIV drugs and frequent co-medications. Furthermore, gender-related differences in tissue distribution and consequently dosing requirements of PrEP will be discussed. Finally, an outlook will be provided on gender- and age-related differences in drug exposure following intramuscular injection of antiretroviral drugs.