Table 8.
Major CRL4s targeted therapies
Drug | Mechanism | Function | Preclinical evidence | Clinical trial | FDA approval |
---|---|---|---|---|---|
E7820 | Promoting DCAF15-CAPERα degradation | Anti-growth in colorectal cancer cells247 | Yes | Completed | Not yet |
CQS | Promoting DCAF15-CAPERα degradation | Anti-growth in colorectal cancer cells247 | Yes | Completed | Not yet |
Indisulam | Promoting DCAF15-CAPERα degradation | Anti-growth in colorectal cancer cells173,247 | Yes | Completed | Not yet |
CC-220 | Promoting CRBN- IKZF1 and IKZF3 degradation | Anti-tumor effect against multiple myeloma cells331 | Yes | Ongoing | Not yet |
Lenalidomide | Promoting CRBN- CK1α degradation | Anti-tumor effect against myelodysplastic syndrome164 | Yes | Completed | Approved |
Promoting CRBN- IKZF1 and IKZF3 degradation | Anti-tumor effect against multiple myeloma cells162,208,209 | Yes | Completed | Approved | |
Thalidomide | Promoting CRBN- IKZF1 and IKZF3 degradation | Anti-tumor effect against multiple myeloma cells248 | Yes | Completed | Approved |
Pomalidomide | Promoting CRBN- IKZF1 and IKZF3 degradation | Anti-tumor effect against multiple myeloma cells248 | Yes | Completed | Approved |
CC-885 | Promoting CRBN- GSPT1 degradation | Anti-tumor effect against leukemic cells163 | Yes | Not yet | Not yet |
Pevonedistat | Inactivation of DCAF2-SET8/p21 degradation | Anti-tumor effect against melanoma cells150 | Yes | Completed | Not yet |
Abbreviations: CQS: chloroquinoxaline sulfonamide; CC-220: alias Compound 6.