The herbicide terbuthylazine (TBA) has displaced atrazine in most of EU countries, becoming one of the most regularly used pesticides and, therefore, frequently detected in natural waters. The affinity of TBA for soil organic matter suggests prolonged contamination; degradation leads to the release of the metabolite desethylterbuthylazine (DET), which has higher water solubility and binds more weakly to organic matter compared to the parent compound, resulting in higher associated risk for contamination of groundwater resources. Additionally, TBA and DET are chemicals of emerging concern because of their persistence and toxicity towards aquatic organisms; moreover, they are known to have significant endocrine disruption capacity to wildlife and humans. Conventional treatments applied during drinking water production do not lead to the complete removal of these chemicals; activated carbon provides the greatest efficiency, whereas ozonation can generate by-products with comparable oestrogenic activity to atrazine. Hydrogen peroxide alone is ineffective to degrade TBA, while UV/HO advanced oxidation and photocatalysis are the most effective processes for oxidation of TBA. It has been determined that direct photolysis gives the highest degradation efficiency of all UV/HO treatments, while most of the photocatalytic degradation is attributed to OH radicals, and TiO solar-photocatalytic ozonation can lead to almost complete TBA removal in ∼30 min. Constructed wetlands provide a valuable buffer capacity, protecting downstream surface waters from contaminated runoff. TBA and DET occurrence are summarized and removal techniques are critically evaluated and compared, to provide the reader with a comprehensive guide to state-of-the-art TBA removal and potential future treatments.