SPI-077

SPI-077 is a PEGylated (polyethyleneglycol-modified) or "stealth" liposomal formulation of the platinum-based chemotherapeutic agent cisplatin. Developed by Alza (now part of Johnson & Johnson), it was designed to improve the pharmacokinetic profile of cisplatin by prolonging circulation half-life and enhancing tumor localization through the enhanced permeability and retention (EPR) effect, while minimizing systemic toxicities such as nephrotoxicity and neurotoxicity. The active ingredient, cisplatin, works by binding to and cross-linking DNA, which inhibits replication and induces apoptosis. Despite showing a superior safety profile in Phase I/II clinical trials, SPI-077 demonstrated poor clinical efficacy, particularly in head and neck cancer, likely due to the high stability of the liposomes preventing sufficient release of the active drug at the tumor site. Development was largely halted in its original formulation due to this lack of efficacy.

Other names

PEGylated liposomal cisplatinstealth liposomal cisplatinliposomal cisplatin