Orally bioavailable
An orally bioavailable MTA-cooperative PRMT5 inhibitor with high selectivity and robust antitumor activity in MTAP-deleted tumors.
Ding, Xiao · Aliper, Alexander M. · Ren, Feng · Zhavoronkov, Alex A.
Journal of Medicinal Chemistry 2025
Strong antiproliferation activity in multiple MTAP-deleted cancer cell lines
Excellent selectivity over MTAP wild-type cell lines
Satisfactory oral pharmacokinetic properties in various preclinical species
Dose-dependent SDMA reduction and robust in vivo antitumor activity in LU99 subcutaneous model