BioCentury
ARTICLE | Distillery Therapeutics

Therapeutics: Protein arginine methyltransferase 5 (PRMT5)

May 7, 2015 7:00 AM UTC

Cell culture and mouse studies suggest a PRMT5 inhibitor could help treat MCL. Screening of a diverse library of small molecules in multiple cellular assays identified a lead compound (EPZ015666) that inhibited PRMT5 with an IC50 of 22 nM. In human MCL cell lines, the lead compound decreased proliferation compared with vehicle. In mice with MCL xenografts, the compound decreased tumor growth. In mice, the compound had 69% oral bioavailability and a good pharmacokinetic profile. Next steps could include optimization and testing the lead compound in animal models of MCL...