Microwaves in the presence of enzymes can contribute to the preparation of a variety of medicinally active compounds. Microwave-induced enzymatic reactions are influenced by variables such as frequency, field strength, waveform, duration, and modulation. The activation of enzymes under microwave irradiation allows the study of simple and complex reactions that have never before been reported under these conditions. By combining enzyme catalysis with microwave technology and solvent-free chemical reactions, it is possible to prepare drug-related molecules. This review presents the most interesting microwave reactions performed by enzymes toward medicinally active molecules.