Table 7 The summary of protein-degradation drug candidates based on PROTAC technology in the global clinical and IND stages (data source: https://clinicaltrials.gov updated: 3/20/2022)
From: PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)
NO. | Time | Company | PRORAC | Target | Indications | E3Ligase | Phase | Nation |
|---|---|---|---|---|---|---|---|---|
1 | 2019 | Arvinas | ARV-110 | AR | Metastatic Castration Resistant Prostate Cancer | CRBN | Phase II | America |
2 | 2019 | Arvinas Pfizer | ARV-471 | ER | ER+/HER2- Locally Advanced or Metastatic Breast Cancer | CRBN | Phase II | America |
3 | 2020 | Bristol Myers Squibb | CC-94676 | AR | Metastatic Castration- Resistant Prostate Cancer | CRBN | Phase I | America |
4 | 2021 | BeiGene | BGB-16673 | BTK | B-Cell Malignancies | CRBN | Phase I | China |
5 | 2021 | Nurix Therapeutics | NX-2127 | BTK | Relapsed/Refractory B-cell Malignancies | CRBN | Phase I | America |
6 | 2021 | Nurix Therapeutics | NX-5948 | BTK | Relapsed/Refractory B-cell Malignancies | CRBN | Phase I | America |
7 | 2021 | Haisco | HK29116 | BTK | Relapsed/Refractory B-cell Malignancies | CRBN | Phase I | China |
8 | 2021 | Lynk | LNK-01002 | Ras GTPase | Primary (PMF) or Secondary Myelofibrosis (PV-MF, ET-MF) or Acute Myeloid Leukemia | CRBN | Phase I | China |
9 | 2021 | Accutar Biotech | AC682 | ER | Locally Advanced or Metastatic ER+ Breast Cancer | CRBN | Phase I | America |
10 | 2021 | Arvinas | ARV-766 | AR | Metastatic Castration-Resistant Prostate Cancer | Undisclosed | Phase I | America |
11 | 2021 | Foghorn Therapeutics | FHD-609 | BRD9 | Advanced Synovial Sarcoma | Undisclosed | Phase I | America |
12 | 2021 | Kymera Sanofi | KT-474 | IRAK4 | Atopic Dermatitis (AD) or Hidradenitis Suppurativa (HS) | Undisclosed | Phase I | America |
13 | 2022 | Hinova | HP518 | AR | Metastatic Castration-Resistant Prostate Cancer | CRBN | Phase I | China |
14 | 2022 | Kintor | GT-20029 | AR | Prostate Cancer | CRBN | Phase I | China |
15 | 2022 | Arvinas | ARV-110 | AR | ARV-110 in Combination with Abiraterone | CRBN | Phase I | America |
16 | 2022 | Kymera | KT-413 | IRAK4 | Relapsed or Refractory B-cell NHL | CRBN | Phase I | America |
17 | 2022 | Kymera | KT-333 | STAT3 | Refractory Lymphoma, Large Granular Lymphocytic Leukemia, Solid Tumors | Undisclosed | Phase I | America |
18 | 2022 | C4 Therapeutics | CFT8634 | BRD9 | Synovial Sarcoma | CRBN | IND | America |
19 | 2022 | C4 Therapeutics | CFT8919 | EGFR- L858R | Non-small-cell Lung Cancer | CRBN | IND | America |
20 | 2022 | Cullgen | CG001419 | TRK | Cancer and other indications | CRBN | IND | America |
