Photopharmacology: Beyond Proof of Principle

TLDR

Poor drug selectivity leads to side effects, environmental toxicity, and resistance, largely because drug activity cannot be controlled in time and space. This Perspective reviews photopharmacology, describing how photoswitchable groups are incorporated into bioactive molecules to enable precise control of drug activity and outlining current principles, design challenges, and therapeutic prospects. Photoswitchable groups act as light‑controlled switches that provide highly precise spatiotemporal regulation of pharmacological activity.

Abstract

Pharmacotherapy is often severely hindered by issues related to poor drug selectivity, including side effects, environmental toxicity, and the emergence of resistance. Lack of selectivity is caused by the inability to control drug activity in time and space. Photopharmacology aims at solving this issue by incorporating photoswitchable groups into the molecular structure of bioactive compounds. These switching units allow for the use of light as an external control element for pharmacological activity, which can be delivered with very high spatiotemporal precision. This Perspective presents the reader with the current state and outlook on photopharmacology. In particular, the principles behind photoregulation of bioactivity, the challenges of molecular design, and the possible therapeutic scenarios are discussed.