Table 3.
Representative PROTACs under clinical evaluation
| Names | Targets | E3 ligases | Indications | Status | Refs. |
|---|---|---|---|---|---|
| AR-LDD | AR | CRBN | Prostate cancer | Phase I | NCT04428788 |
| ARV-110 | AR | CRBN | Prostate cancer | Phase II | NCT05177042, NCT03888612 |
| ARV-471 | ER | CRBN | Breast cancer | Phase II | NCT05501769, NCT05463952, NCT04072952 |
| ARV-766 | AR | VHL | Prostate cancer | Phase I | NCT05067140 |
| BGB-16673 | BTK | Undisclosed | B cell malignancies | Phase I | NCT05294731, NCT05006716 |
| CFT8634 | BRD9 | CRBN | Synovial sarcoma | Phase I/II | NCT05355753 |
| DT-2216 | BCL-XL | VHL | Liquid and solid tumors | Phase I | NCT04886622 |
| FHD-609 | BRD9 | Undisclosed | Synovial sarcoma | Phase I | NCT04965753 |
| GT20029 | AR | Undisclosed | Androgenetic alopecia and acne | Phase I | NCT05428449 |
| HSK29116 | BTK | Undisclosed | B cell malignancies | Phase I | NCT04861779 |
| KT-333 | STAT3 | Undisclosed | Liquid and solid tumors | Phase I | NCT05225584 |
| KT-413 | IRAK4 | CRBN | B cell lymphomas | Phase I | NCT05233033 |
| KT-474 | IRAK4 | Undisclosed | Atopic dermatitis and hidradenitis suppurativa | Phase I | NCT04772885 |
| LNK01002 | RAS GTPase | Undisclosed | Acute myeloid leukemia | Phase I | NCT04896112 |
| NX-2127 | BTK | CRBN | B cell malignancies | Phase I | NCT04830137 |
| NX-5948 | BTK | CRBN | B cell malignancies and autoimmune diseases | Phase I | NCT05131022 |