Protein Arginine Methyl Transferase 5 (PRMT5) is a member of a family of enzymes involved in the methylation of arginine residues on histones and other cytosolic and nuclear proteins. Arginine methylation is emerging as an important oncogenic and resistance mechanism by impacting mRNA splicing, cell cycle and signaling. PRMT5 is overexpressed in multiple cancer types and correlates with poor outcomes. PRMT5 inhibitors have demonstrated efficacy in multiple preclinical models, both as single agents and in combination with other approved targeted therapies.
Prelude is advancing novel, selective, potent and orally bioavailable compounds, including PRT543, which target PRMT5. PRT543 is currently being evaluated in a Phase 1 clinical trial in patients with advanced solid tumors, lymphoma and myeloid malignancies.