Table 2.
Next-generation ER-targeting agents in clinical trials
| Drug | Type of inhibitor | Source | Stage of Development | Clinical Trial Identifier (ER+ MBC) | References |
|---|---|---|---|---|---|
| Bazedoxifene | SERM/SERD hybrid (oral) | Pfizer | Approved (osteoporosis) | NCT02448771 | (Fanning et al., 2018; Komm et al., 2005; Wardell et al., 2015a) |
| Lasofoxifene | SERM (oral) | Sermonix | Phase III (osteoporosis) | NCT03781063 | (Laine et al., 2019; Rosati et al., 1998) |
| Elacestrant (RAD1901) | SERM/SERD hybrid (oral) | Radius Health | Phase III | NCT03778931 | (Bihani et al., 2017; Garner et al., 2015; Kaklamani et al., 2020; Wardell et al., 2015b) |
| SAR439859 | SERD (oral) | Sanofi | Phase II | NCT04059484; NCT03284957 (with palbociclib) | (El-Ahmad et al., 2020; Shomali et al., 2017) |
| Rintodestrant (G1T48) | SERD (oral) | G1 Therapeutics | Phase I/II | NCT03455270 | (Andreano et al., 2020; Dees et al., 2019; Wardell et al., 2017) |
| LSZ102 | SERD (oral) | Phase I | NCT02734615 (single agent or with ribociclib or alpelisib) | (Jhaveri et al., 2019; Juric et al., 2018; Tria et al., 2018) | |
| GDC-9545 | SERD (oral) | Genentech | Phase I | NCT03332797 | (Jhaveri et al., 2020) |
| AZD9496 | SERD (oral) | Astra Zeneca | Phase I | NCT03236974 | (De Savi et al., 2015; Hamilton et al., 2018; Weir et al., 2016) |
| ZN-c5 | SERD (oral) | Zeno Alpha | Phase I/II | NCT03560531 | |
| D-0502 | SERD (oral) | InventisBio | Phase I | NCT03471663 | (Wang et al., 2018) |
| SHR9549 | SERD (oral) | Jiangsu Hengrui Medicine | Phase I | NCT03596658 | |
| LY3484356 | SERD (oral) | Eli Lilly | Phase I | NCT04188548 | |
| H3B-6545 | Selective estrogen receptor covalent antagonist (SERCA; oral) | H3 Biomedicine | Phase I/II | NCT03250676 | (Puyang et al., 2018) |
| ARV-471 | PROTAC (oral) | Arvinas | Phase I | NCT04072952 | (Flanagan et al., 2019) |
Next-generation ER-targeting agents currently in clinical trials for advanced/metastatic ER+ breast cancer (www.ClinicalTrials.gov).