Table 1.
PROTACs currently in clinical trials. Data from clinicaltrials.gov (https://clinicaltrials.gov/ct2/home; accessed on 20 February 2023). NA—not applicable.
| PROTAC Name (Company) | E3 Ligase | Targeted Protein (Indication) | Trial Phase | Study Number |
|---|---|---|---|---|
| AC682 (Accutar Biotech Inc.) | CRBN | Estrogen receptor; (breast cancer) | Phase 1 | NCT05489679; NCT05080842 |
| ARV-471 (Arvinas) | CRBN | Estrogen receptor; (breast cancer) | Phase 1/2 | NCT05501769; NCT04072952; NCT05549505; NCT05463952; NCT05573555; NCT05548127; NCT05732428 |
| ARV-766 (Arvinas) | unknown | Androgen receptor; (prostate cancer) | Phase 1/2 | NCT05067140 |
| ARV-110 (Arvinas) | CRBN | Androgen receptor; (prostate cancer) | Phase 1/2 | NCT05177042; NCT03888612 |
| CC-94676 (Celgene/Bristol Myers Squibb) | CRBN | Androgen receptor; (prostate cancer) | Phase 1 | NCT04428788 |
| DT2216 (Dialectic Therapeutics) | VHL | BCL-XL; (Solid tumors, hematologic malignancy) | Phase 1 | NCT04886622 |
| FHD-609 (Foghorn Therapeutics) | CRBN | BRD9; (synovial sarcoma) | Phase 1 | NCT04965753 |
| CFT8634 (C4 Therapeutics) | CRBN | BRD9; (synovial sarcoma, soft tissue sarcoma) | Phase 1/2 | NCT05355753 |
| KT-474 (Kymera) | CRBN | IRAK-4; (atopic dermatitis, hidradenitis suppurativa) | Phase 1 | NCT04772885 |
| KT-413 (Kymera) | CRBN | IRAK-4; (non-Hodgkin lymphoma, diffuse large B-cell lymphoma) |
Phase 1 | NCT05233033 |
| KT-333 (Kymera) | unknown | STAT3; (lymphomas, large granular lymphocytic leukemia, solid tumors) | Phase 1 | NCT05225584 |
| NX-2127 (Nurix Therapeutics) | CRBN | BTK; (B-cell malignancies) | Phase 1 | NCT04830137 |
| NX-5948 (Nurix Therapeutics) | CRBN | BTK; (B-cell malignances, chronic lymphocytic leukemia, Waldenstrom macroglobulinemia, primary central nervous system lymphoma) | Phase 1 | NCT05131022 |
| CFT1946 (C4 Therapeutics) | CRBN | BRAFV600X; (solid tumors, melanoma, non-small-cell lung cancer, colorectal cancer, anaplastic thyroid cancer) | Phase 1/2 | NCT05668585 |
| CG001419 (Cullgen) | CRBN | TRK—neurotrophic-factor receptor tyrosine kinase; (advanced solid tumors) | NA | FDA-approved for use in clinical trials. |