Anticancer drug discovery continues to grow to meet new needs and complement existing treatments. Prodrug strategies like the light-based photodynamic therapy (PDT) are promising routes towards adjuvant strategies, wherein light potentiates an otherwise nontoxic drug or photosensitizer (PS) to destroy tumors and their vasculature. To date, the only US-based and FDA-approved PS for cancer therapy is Photofrin, an oligomeric porphyrin-based mixture, which has limited PDT’s mainstream adoption due to various shortcomings. Over the years, metal-based coordination complexes have emerged as promising PDT agents that can be rationally designed and tuned from a tumor- or disease-centered approach with optimal chemical, photophysical, and photobiological properties. Ruthenium- and osmium-polypyridyl complexes serve as examples, with our own TLD1433 having recently advanced to a phase II clinical trial for bladder cancer. Herein, we report the development of a highly potent and hypoxia-active osmium PS with a focus on its photobiological and photophysical properties.

Breaking the barrier to hypoxia-active photodynamic therapy with an osmium photosensitizer

ACS Spring Meeting 2021

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.