Pharmaceutical micropollutants in the environment are seen as a threat to health, water, and food safety. Drug residues present in the environment impose adverse effects to aquatic world. Recent research has shown that this problem cannot be solved with advanced treatment processes. Very often, pharmaceuticals are transformed to other products. Effects and risk assessments are generally performed based on single compounds instead of cocktail mixture which is not the situation in the environment. The sustainable solution for pharmaceutical emerging contaminants in the environment will be benign by design, which can be the paradigm of the future. Benign by design means that easy (bio)degradability of pharmaceuticals (and/or chemicals) after use or application is taken into account even before it is synthesized, that is, during the lead optimization stages. It is an important concept within green and sustainable pharmacy and chemistry and very promising in terms of sustainability.