GDC-9545 (Giredestrant) is an efficient and potent selective estrogen receptor degrader (SERD) and a full antagonist.
GDC-9545 exhibited better antiproliferation activity than known SERDs across multiple cell lines.
GDC-9545 exhibits low drug-drug interaction liability and demonstrates excellent in vitro and in vivo safety profiles.
GDC-9545 induced tumor regressions either as a single agent or in combination with a CDK4/6 inhibitor in an ESR1Y537S mutant PDX or a wild-type ERα tumor model.
