mipsagargin

Mipsagargin is a first-in-class, thapsigargin-based prodrug designed to selectively target the tumor microenvironment. It consists of a potent inhibitor of the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) pump, thapsigargin, conjugated to a peptide carrier that is specifically cleaved by prostate-specific membrane antigen (PSMA). PSMA is highly expressed on the surface of prostate cancer cells and the neovasculature of many other solid tumors. Upon cleavage by PSMA, the active thapsigargin analog is released, leading to an increase in intracellular calcium levels, induction of the unfolded protein response, and subsequent apoptosis of both tumor cells and tumor-associated endothelial cells. Developed by Inspyr Therapeutics (formerly GenSpera), mipsagargin has been evaluated in clinical trials for hepatocellular carcinoma, glioblastoma, and prostate cancer.

Other names

12-ADT-Glnthapsigargin-based prodrug