The application of TiO₂ nanoparticles as photocatalyst is extensively used for the removal of micropollutants in water treatment and as an alternate to the traditional disinfection techniques. TiO₂ photocatalysis is a more efficient method for the degradation of a lot of pharmaceuticals micropollutants as compared to photolysis. Photocatalysis often degrades micropollutants incompletely generating new molecules, the so-called transformation products (TPs). These TPs can retain the pharmacological activity, can be even more bioaccumulative and toxic than the parent compound, and/or can resist biodegradation. Thus, it is required to evaluate the risk associated with the presence of TPs generated during the treatment process. In this study, authors review recent research on the efficiency of TiO₂ photocatalysis for the removal of selected pharmaceuticals and possible formation of TPs. The review also discusses the existing knowledge gaps and addresses the need for further research into photocatalytic water treatment technology in the near future.