Table 1.
The currently studied PROTACs in clinical trials.
| PROTAC | E3 Ligase Targeting Ligand | E3 Ligase | Target | Disease | Phase | No. of Patients | NCT |
|---|---|---|---|---|---|---|---|
| ARV-110 | Lenalidomide-based | Cereblon (CRBN) | Androgen receptor | Metastatic castration-resistant prostate cancer | 1 | 40 | NCT05177042 |
| ARV-110 | thalidomide-based | Cereblon (CRBN) | Androgen receptor | Metastatic castration-resistant prostate cancer | 1/2 | 250 | NCT03888612 |
| ARV-766 | undisclosed | undisclosed | Androgen receptor | Metastatic castration-resistant prostate cancer |
1 | 60 | NCT05067140 |
| CC-94676 | undisclosed | Cereblon (CRBN) | Androgen receptor | Metastatic, castration-resistant prostate cancer | 1 | 70 | NCT04428788 |
| ARV-471 | Lenalidomide-based | Cereblon (CRBN) | Estrogen receptor | ER+/HER- advanced or metastatic breast cancer | 1/2 | 170 | NCT04072952 |
| DT2216 | undisclosed | Von Hippel-Lindau (VHL) | BCL-xL | Solid and hematological malignancies | 1 | 24 | NCT04886622 |
| NX-2127 | IMID-based | Cereblon (CRBN) | BTK | Hematological malignancies (BTK C481-mutated CLL/SLL, WM, MZL, FL, DLBCL) | 1 | 130 | NCT04830137 |
| DKY709 | Pomalidomide-based | Cereblon (CRBN) | IKZF2 | Solid malignancies | 1 | 380 | NCT03891953 |