Development of AVE-8063-Bearing Pt(IV) Prodrug for Dual-Action Light-Controlled Chemotherapy

Platinum-based drugs remain a cornerstone of cancer therapy. The antitumor efficacy of platinum complexes can be significantly enhanced by combining them with bioactive compounds that exert antiproliferative effects through different mechanisms of action. We report herein a novel photoactive Pt(IV) prodrug with tubulin polymerization inhibitor AVE8063 as well as NIR light absorbing carbocyanine moiety in axial positions, which demonstrate efficient intracellular accumulation, light-responsive antiproliferative activity and ability to inhibit cellular mobility. To the best of our knowledge, this is the first example of dual photoactive carboplatin-AVE8063 Pt(IV) prodrug.