cabozantinib-chlorin e6 conjugate

This investigational, first-in-class prodrug conjugate, referred to as conjugate 3, is designed for the selective treatment of bladder cancer. It consists of two therapeutic modules—a chlorin-e6 photosensitizer and a derivative of the multi-target tyrosine kinase inhibitor cabozantinib—connected by a β-glucuronidase-responsive linker. The drug is engineered to remain inactive until it reaches tumor cells that overexpress the lysosomal enzyme β-glucuronidase. Upon enzymatic cleavage within the lysosomes of bladder cancer cells, the conjugate releases both the chlorin derivative and the cabozantinib derivative. This dual-action approach combines targeted therapy, which inhibits kinases such as c-Met, VEGFR2, AXL, RET, and FLT3, with photodynamic therapy (PDT). Upon light exposure, the released chlorin-e6 generates reactive oxygen species (ROS) to induce tumor cell death. Preclinical studies in human bladder carcinoma (T-24) cells and 3D tumor models have demonstrated synergistic suppression of tumor proliferation at submicromolar concentrations.

Other names

cabozantinib-chlorin e6-glucuronide conjugatechlorin e6-cabozantinib conjugate