Clinical Trials of Targeted Nanoparticulate Drug Delivery Systems

The use of nanoparticulate drug delivery systems (nano-DDS) in the diagnosis and treatment of diseases has increased in recent years, thanks to successfully completed clinical studies. Many nano-DDS in which a drug is encapsulated are approved, in addition to polyethylene glycol (PEG)ylated drugs and nanocrystals. Despite their promising preclinical results, the drug approval rate for active-targeted and stimuli-sensitive nano-DDS remains relatively lower in comparison to passive-targeted nano-DDS. The chapter provides a detailed status summary of MM-302, ThermoDox, and BIND-014 as sample cases of nano-DDS systems in phase 2/phase 3 trials. MM-302 is a human epidermal growth factor receptor 2 (HER2)-targeted PEGylated antibody–liposomal doxorubicin conjugate. MM-302 allows the targeted delivery of doxorubicin into HER2-overexpressing tumor cells via anti-HER2-directed antibodies, thereby mitigating doxorubicin-related cardiotoxic and other adverse events as well as demonstrating superior activity such tumor cells.