Table 2. Current clinical-stage PROTACs

Compound Target protein Indication Reference
ARV-110 AR Metastatic castration-resistant prostate cancer [65]
ARV-766 AR Metastatic castration-resistant prostate cancer [66]
ARV-471 ER Breast cancer (ER+/HER2-) [67]
DT2216 BCL-XL Hematologic malignancies, solid tumors [68]
NX2127 BTK, IKZF1/3 CLL, NHL [69]
NX5948 BTK B-cell malignant tumors and autoimmune diseases [70]
CFT 1946 Mutant BRAF V600E Melanoma, colorectal cancer [71]
CFT 8634 Bromodomain-containing protein 9 Synovial sarcoma [72]
CFT 8919 Mutant EGFR L858R Non-small cell lung cancer [73]
KT-474 IRAK4 Autoimmune diseases [74]
PROTACs, proteolysis-targeting chimeras; AR, androgen receptor; ER, estrogen receptor; BCL-XL, B-cell lymphoma-extra large; BTK, Bruton tyrosine kinase; IKZF, ikaros; CLL, chronic lymphocytic leukemia; NHL, non-hodgkin’s lymphoma; BRAF, B-Raf proto-oncogene, serine/threonine kinase; EGFR, epidermal growth factor receptor; IRAK4, interleukin-1 receptor-associated kinase 4.