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. Author manuscript; available in PMC: 2020 Apr 23.
Published in final edited form as: Biochim Biophys Acta Rev Cancer. 2018 Dec 30;1871(1):138–159. doi: 10.1016/j.bbcan.2018.11.007

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.