The estrogen-related receptor α (ERRα), a nuclear receptor, is a key transcriptional master regulator of mitochondrial function and flexibility by controlling an intricate network of mitochondrial and metabolic genes. ERRα upregulation and activation is associated with poor prognosis, recurrence of cancer, therapy resistance and metastasis of several indications including melanoma, breast and colon cancer. Lead Pharma's ERRα inverse agonists are thus targeting one of the emerging hallmarks in cancer, the deregulation of energetics in cancer cells.
Lead Pharma has developed potent, non-covalent, non-steroidal ERRα inverse agonists with first-in-class potential.
This project is currently in pre-clinical development.