Table 1 Comparison of clinically available and experimental SERDs.
Drug | Structure | EC50 of ERα degradation (nM) | Mechanism of action | Effective in ESR1 mutation | Administration |
|---|---|---|---|---|---|
Fulvestrant11 | steroidal | 9.3 | degrader/ down-regulator | no | im. injection |
Elacestrant12 | non-steroidal | 0.6 | degrader/ modulator | yes | oral |
Amcenestrant13 | non-steroidal | 0.2 | degrader/ down-regulator | yes | oral |
Giredestrant14 | non-steroidal | 0.05 | degrader/ down-regulator | yes | oral |
Camizestrant15 | non-steroidal | 0.2 | degrader | yes | oral |
Imlunestrant16 | non-steroidal | 3.0 | degrader | yes | oral |