Table 3.
Summary of PROTACs under clinical evaluation for cancer therapy. Yellow: recruiting; violet: not yet recruiting. AR: androgen receptor; BCL-xL: B-cell lymphoma-extra large; BRAF: v-raf murine sarcoma viral oncogene homolog B1; BRD: bromodomain-containing protein; BTK: Bruton’s tyrosine kinase; DLBCL: diffuse large B cell lymphoma; EGFR: epidermal growth factor receptor; ER: estrogen receptor; IND: investigational new drug; LGL: large granular lymphocyte; mCRPC: metastatic castration-resistant prostate cancer; MDM2: mouse double minute 2; NSCLC: non-small cell lung cancer; R/R: relapsed/refractory; STAT3: signal transducer and activator of transcription 3; NTRK: neurotrophic tyrosine receptor kinase; 2H2022: Second half of the year 2022.
| Time | Degrader | Target | Indication | NCT Number | Phase |
|---|---|---|---|---|---|
| 2019 2022 |
ARV-110 | AR | mCRPC |
NCT03888612
NCT05177042 |
Phase I/II Phase I |
| 2021 | ARV-766 | AR | mCRPC | NCT05067140 | Phase I |
| 2020 | CC-94676 | AR | mCRPC | NCT04428788 | Phase I |
| 2022 | HP518 | AR | mCRPC | NCT05252364 | Phase I |
| 2022 | AC176 | AR | mCRPC | NCT05241613 | Phase I |
| 2021 | DT2216 | BCL-xL | R/R malignancies | NCT04886622 | Phase I |
| 2022 | RNK05047 | BRD4 | Advanced solid tumors/ DLBCL | NCT05487170 | Phase I/II |
| 2022 | CFT8634 | BRD9 | Synovial sarcoma and SMARCB1-null tumors | NCT05355753 | Phase I/II |
| 2021 | FHD-609 | BRD9 | Advanced synovial sarcoma or advanced SMARCB1-null tumors | NCT04965753 | Phase I |
| 2021 | NX-2127 | BTK | R/R B-cell malignancies | NCT04830137 | Phase I |
| 2021 | NX-5948 | BTK | R/R B-cell malignancies | NCT05131022 | Phase I |
| 2021 2022 |
BGB-16673 | BTK | B-cell malignancies |
NCT05006716
NCT05294731 |
Phase I Phase I |
| 2021 | HSK29116 | BTK | R/R B-cell malignancies | NCT04861779 | Phase I |
| 2019 2022 2022 2022 2022 |
ARV-471 | ER | ER+/HER2- locally advanced or metastatic breast cancer |
NCT04072952
NCT05501769 NCT05463952 NCT05549505 NCT05548127 |
Phase I/II Phase I Phase I Phase II Phase I/II |
| 2021 2022 |
AC682 | ER | ER+/HER2- locally advanced or metastatic breast cancer |
NCT05080842
NCT05489679 |
Phase I Phase I |
| 2022 | KT-333 | STAT3 | Refractory lymphoma, LGL leukemia and solid tumors | NCT05225584 | Phase I |
| 2022 | CFT1946 | BRAFV600E | BRAF-V600E mutant solid tumors | IND | |
| Planned for (2H2022) | CFT8919 | EGFRL858R | NSCLC | IND | |
| Planned for (2H2022) | KT-253 | MDM2 | Liquid and solid tumors | IND | |
| 2022 | CG001419 | NTRK | Advanced solid tumors | IND |