PZ-128 is primarily investigated for its application in cancer therapy, specifically as a vascular disrupting agent (VDA). It targets and disrupts the existing blood vessels within solid tumors, leading to rapid shutdown of tumor blood flow. This results in extensive tumor cell death due to ischemia and nutrient deprivation.

It has shown promising activity in preclinical models against various solid tumors, including colorectal, ovarian, and breast cancers. Due to its mechanism of action, PZ-128 is often explored in combination with other anticancer therapies such as chemotherapy, radiation, or immunotherapy to enhance overall treatment efficacy. Its ability to selectively affect tumor vasculature while sparing normal blood vessels makes it a valuable candidate in targeted oncology treatments.