The investigation of new sensing principles and technologies for the detection of molecular binding events has created great expectations on numerous major industrial sectors, such as healthcare, food, water and agriculture. Combining many of these advances with the potential of the immunochemical systems has allowed developing novel biosensors that provide interesting advantages against the traditional strategies for analysis, such as the possibility of multianalysis, development of field analytical methods and fabrication of easy end-user devices. Specifically, many efforts have been lately invested to control residues of pharmaceuticals in food and environmental samples, as an indication of the impact of the human activity in the media. Human and veterinary drugs, such as antibiotics, hormones, analgesics, cytostatics or β-blockers, show a high potential risk of negative effects in the environment and public health. Thus, there is a great need for low-cost and highly efficient tools for quick, reliable, and accurate detection of these contaminating bioactive agents. In particular, the scope of the present chapter is addressed to provide an overview of the potential of novel micro(nano)technology approaches to develop biosensors useful for the analysis of emerging pollutants.