Table 13 Cereblon-based PROTACs in clinical trials
From: Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACs
PROTAC | Chemical Structure | Target | Disease | ROA | NCT number | Phase | Sponsor | Ref. |
|---|---|---|---|---|---|---|---|---|
Vepdegestrant (ARV-471) |
| ER | Breast cancer | Oral | NCT05654623 | III | Arvinas/ Pfizer | |
CC-94676 |
| AR | Prostate cancer | Oral | NCT06764485 NCT04428788 | III I | Bristol-Myers Squibb | |
KT-474 |
| IRAK4 | Autoimmune diseases | Oral | NCT06058156 NCT06028230 | II | Kymera/ Sanofi | |
Bavdegalutamide (ARV-110) |
| AR | Prostate cancer | Oral | NCT03888612 | I/II | Arvinas | |
Luxdegalutamide (ARV-766) |
| AR | Prostate cancer | Oral | NCT05067140 | I/II | Arvinas | |
CFT1946 |
| BRAF V600 | Solid tumors with BRAF V600 mutations | Oral | NCT05668585 | I/II | C4 Therapeutics | |
CFT8634 |
| BRD9 | Synovial sarcoma and SMARCB1-loss tumors | Oral | NCT05355753 | I/II | C4 Therapeutics | |
BGB-16673 |
| BTK | B-cell malignancies | Oral | NCT05006716 NCT05294731 NCT06634589 | I/II | BeiGene | |
NX-2127 |
| BTK + IKZF1/3 | B-cell malignancies | Oral | NCT04830137 | I | Nurix Therapeutics | |
FHD-609 |
| BRD9 | Synovial sarcoma and SMARCB1-loss tumors | I.V. | NCT04965753 | I | Foghorn Therapeutics | |
KT-413 |
| IRAK4 | B-cell non-Hodgkin lymphoma | I.V. | NCT05233033 | I | Kymera Therapeutics | |
NX-5948 |
| BTK | B-cell malignancies | Oral | NCT05131022 | I | Nurix Therapeutics | |
CG001419 | Unknown structure | TRK | Solid tumors | - | CTR20222742 | II | Cullgen | |
BMS-986458 | Unknown structure | BCL6 | Non-Hodgkin lymphoma | - | NCT06090539 | I/II | Bristol-Myers Squibb | |
AC682 | Unknown structure | ER | Breast cancer | Oral | NCT05080842 NCT05489679 | I | Accutar Biotech | |
AC676 | Unknown structure | BTK | B-cell malignancies | Oral | NCT05780034 | I | Accutar Biotech | |
HSK29116 | Unknown structure | BTK | B-cell malignancies | Oral | NCT04861779 | I | Haisco Pharmaceutical Group | |
GT-20029 | Unknown structure | AR | Androgenetic alopecia and acne vulgaris | Topical | NCT05428449 | I | Kintor Pharmaceutical | |
HP518 | Unknown structure | AR | Prostate cancer | Oral | NCT06155084 | I | Hinova Pharmaceuticals |
- Note:
- AR androgen receptor, BCL6 B-cell lymphoma 6, BTK Bruton’s tyrosine kinase, BRAF V600 B-raf proto-oncogene, serine/threonine kinase V600 mutation, BRD9 Bromodomain-containing protein 9, IRAK4 interleukin-1 receptor-associated kinase 4, ER estrogen receptor, IKZF1/3 IKAROS family zinc finger proteins 1/3, TRK tropomyosin receptor kinase.
