Insects and the substances extracted from them have been used as medicinal resources by human cultures all over the world. Besides medicine, these organisms have also played mystical and magical roles in the treatment of several illnesses in a range of cultures. Science has already proven the existence of immunological, analgesic, antibacterial, diuretic, anesthetic, and antirheumatic properties in the bodies of insects. Several authors have surveyed the therapeutic potential of insects, either recording traditional medical practices or employing insects and their products at the laboratory and/or clinical level. Thus, insects seem to constitute an almost inexhaustible source for pharmacological research. Chemical studies are needed to discover which biologically active compounds are actually present within insect bodies. The therapeutic potential of insects represents a significant contribution to the debate on biodiversity conservation, as well as opening perspectives for the economic and cultural valorization of animals traditionally regarded as useless. Their use needs to be at a sustainable level to avoid overexploitation.