Visible and Near-Infrared Photopharmacology: Wavelength-Redshift Strategies for Spatiotemporally Precise Therapeutics

Photopharmacology is an innovative paradigm for spatiotemporally controlled drug activity, offering a novel approach to enhance therapeutic precision through improved selectivity and minimized toxicity. However, conventional photoswitches critically depend on ultraviolet (UV) light, which suffers from poor biocompatibility due to its tissue-damaging properties and inherently limited tissue penetration depth. Therefore, the development of red-shifted photopharmacological agents has emerged as a pivotal research focus, garnering substantial interdisciplinary interest. This review provides a comprehensive overview of recent advances in redshift-light-activated photoswitches and photocages, highlighting their structural design principles, photophysical properties, and mechanistic insights in medicinal chemistry. Focused on current technological frontiers and unresolved challenges, we further elaborate on the applicational potential of photopharmacological strategies for <i>in vivo</i> treatment, thereby illuminating future directions for integrating light-responsive molecular systems into precision medicine.