This study assesses the presence, fate and effects of five environmentally relevant pharmaceuticals and eight of their corresponding human metabolites in Lake Geneva. Over a 10-month period, lake samples were taken at various depths and locations in the Vidy Bay. Among the targeted metabolites, six were detected with concentrations ranging from 5 to > 100 ng∙L-1. The highest concentrations were detected above the wastewater treatment plant outfall, supporting the assumption that wastewater represents the main source of human metabolites to the lake. The metabolites were less recalcitrant to environmental degradation than their parent. Nevertheless, their presence in the aquatic environment may lead to an increase of the ecotoxicological risk.