SR16388: A Novel Drug That Inhibits Tumor Growth by Targeting ERRalpha

A protein called estrogen-related receptor alpha (ERRalpha) has been implicated in various human malignancies, including breast, prostate, ovarian, and colon cancer. ERRalpha is thought to regulate the cell energy metabolism of tumor cells, which have high energy demands because of their rapid growth. Because this protein controls a crucial cellular process in many types of tumors, it represents a promising target for anticancer drugs.

SRI researchers have developed a novel steroidal compound, SR16388, which very selectively binds to and inhibits ERRalpha. This drug also regulates tumor energy metabolism by strongly inhibiting the protein HIF-1alpha, which promotes tumor cell survival in low-oxygen conditions. Through these mechanisms, SR16388 inhibits the growth of new blood vessels in prostate cancer tumors and the proliferation of breast cancer cells.

Studies in preclinical models of advanced prostate cancer, multiple myeloma, and non-small cell lung cancer have shown that the orally active drug suppresses tumor growth, strongly enhances the effectiveness of standard anticancer therapies, and is safe and non-toxic. These results indicate that SR16388 shows considerable promise for safely treating a range of cancers and augmenting the efficacy of current anticancer therapies.

Learn more in the SR16388 product summary slides.