Photopharmacology is a novel innovative approach ultimately aiming for precise activation of a drug in space and time making use of light. One of the major issues in drug development programs worldwide is how to reach high selectivity for a specific target. For instance, in chemotherapy towards cancer treatment precise dosing with high selectivity while reducing side effects and enhancing quality of life for the patient. Similar increased selectivity in antimicrobial treatment will lower environmental release of antibiotics and as a consequence it is expected to decrease antibiotic resistance development. Based on our Nobel Prize winning discoveries of light-powered molecular machines we aim to show proof of principle of smart pharmaceuticals, in particular antibiotics and antitumor agents, that can be precisely activated by light irradiation. In this POC study we explored photoswitches to control reversibly antibiotic activity. Specifically, it was demonstrated that antibiotic activity can be with near-infrared light, essential for future in vivo and clinical studies. Furthermore, photoactive quorum sensing molecules essential in bacterial communication were designed for potential future biofilm treatment targeting surgery implants. Towards oncology potential antitumor compounds were designed, the activity of which can be control by photoswitching as well as well as systems that can be activated by photochemical deprotection. Novel coumarin -protecting groups were specifically designed and applied for selected promising chemotherapeutic compounds. This POC project established a fundamental basis en route to show the viability of the photopharmacology approach towards precision chemotherapeutic and antimicrobial agents in future drug development. Currently a spin-off company Lumento is initiated and active cooperation with potential industrial (pharmaceutical) partners pursued.