Approved anthracyclines and anthracenediones repurposed as single-molecule photosensitizers
- TD-DFT screening of a curated library of approved anticancer drugs picked out chromophore-bearing candidates with favourable photophysics.
- Mitoxantrone, pixantrone, daunorubicin and epirubicin generated reactive oxygen species on irradiation and showed enhanced cytotoxicity in breast cancer cells.
- One molecule thus supplies both the chemotherapy and the photodynamic effect, avoiding a two-component conjugate.
💡 Points
Starting from compounds with known PK and safety is the smart part: the CMC and tox story is already written. The catch is that these chromophores absorb at wavelengths that penetrate tissue poorly, and ROS from an anthracycline adds to cardiotoxicity worries. I'd want in vivo light-dose windows before getting excited.