Table 1.
Degrader | Target | Company | E3 ligase | Highest phase | Ref. |
---|---|---|---|---|---|
ARV-110 | AR | Arvinas | CRBN | Phase VII | [65] |
ARV-471 | ER | Arvinas; Pizer | CRBN | Phase VII | [66] |
CFT7455 | IKZF3, IKZF1 | C4 Therapeutics | CRBN | Phase VII | [67] |
AC0682 | ER α | Accutar Biotech | CRBN | Phase I | [68] |
AC0176 | AR | Accutar Biotech | Undisclosed | Phase I | [68] |
ARV-766 | AR | Arvinas | Undisclosed | Phase I | [69] |
BGB-16673 | BTK | Beigene | CRBN | Phase I | [70] |
CC-94676 | AR | BMS | CRBN | Phase I | [71] |
DT2216 | BCL-XL | Dialectic Therapeutics; University of Florida | VHL | Phase I | [72] |
FHD-609 | BRD9 | Foghorn Therapeutics | Undisclosed | Phase I | [73] |
HP518 | AR | Hinova | Undisclosed | Phase I | [74] |
KPG-818 | IKZF 1/3 | Kangpu | CRBN | Phase Ib/2a | [75] |
KPG-121 | IKZF 1/3; CK 1a | Kangpu | CRBN | Phase I | [76] |
KT-333 | STAT3 | Kymera | Undisclosed | Phase I | [77] |
KT-413 | IRK4 | Kymera | CRBN | Phase I | [78] |
KT-474 | IRK4 | Kymera; Sanofi | Undisclosed | Phase I | [79] |
NX-2127 | BTK | Nurix Therapeutics | CRBN | Phase I | [80] |
NX-5948 | BTK | Nurix Therapeutics | CRBN | Phase I | [81] |
AC0676 | BTK | Accutar Biotech | Undisclosed | IND-Enabling | [68] |
CFT8634 | BRD9 | C4 Therapeutics | CRBN | IND-Enabling | [82] |
CFT8919 | EGFR-L858R | C4 Therapeutics | CRBN | IND-Enabling | [83] |
CG001419 | TRK | Cullgen | CRBN | IND-Enabling | [84] |