TABLE 1.
Basic information of the selected articles.
| BET inhibitor (target) | Author | Clinical trial registration number | Phase | Publication year | Number of patients | Study design | Cancer type | Median age (range) |
|---|---|---|---|---|---|---|---|---|
| AZD5153 (BRD4) | Wang et al. (2019) | NCT03205176 | 1 | 2019 | 28 | Single-arm | R/R malignant solid tumor and lymphoma (n = 28) | 66.5 (no mention) |
| ABBV-075 (BRD4) | Piha-Paul et al. (2019) | NCT02391480 | 1 | 2019 | 84 | Single-arm | R/R solid tumors (n = 72), prostate cancer (n = 12) | 62.5 (23–83) |
| BMS-986158 (BRD4) | Hilton et al. (2018) | NCT02419417 | 1/2a | 2018 | 68 | Single-arm | Advanced cancer (n = 68) | 59 (no mention) |
| CPI-0610 (BRD4) | Blum et al. (2018) | NCT01949883 | 1 | 2018 | 64 | Single-arm | R/R lymphomas (n = 64) | No mention |
| CPI-0610 (BRD4) | Kremyanskaya et al. (2018) | NCT02158858 | 2 | 2019 | 44 | Single-arm | Myelofibrosis (n = 44) | 69 (41–83) |
| GSK525762 (BRD2/BRD3/BRD4) | Piha-Paul et al. (2020) | NCT01597703 | 1 | 2019 | 65 | Single-arm | CRC (n = 34), NUT carcinoma (n = 29) | ≥16 |
| GSK525762 (BRD2/BRD3/BRD4) | Dawson et al. (2017) | No mention | 1/2 | 2017 | 46 | Single-arm | R/R AML (n = 41), AML after MDS (n = 4), new AML (n = 1) | 66.5 (24–84) |
| OTX-015 (BRD2/BRD3/BRD4) | Dombret et al. (2014) | No mention | 1 | 2017 | 36 | Single-arm | AML (n = 33), ALL (n = 2), RA with a large number of blasts (n = 1) | 70 (19–85) |
| OTX-015 (BRD2/BRD3/BRD4) | Berthon et al. (2016) | NCT01713582 | 1 | 2016 | 41 | Single-arm | Acute leukemia (n = 40), MDS (n = 1) | 70 (60–75) |
| OTX-015 (BRD2/BRD3/BRD4) | Amorim et al. (2016) | NCT01713582 | 1 | 2016 | 45 | Single-arm | Lymphoma (n = 33), myeloma (n = 12) | 66 (55–72) |
| OTX-015 (BRD2/BRD3/BRD4) | Massard et al. (2016) | No mention | 1b | 2016 | 46 | Single-arm | CRPC (n = 26), NMC (n = 10), KRASmut NSCLC (n = 9), ALK+ NSCLC (n = 1) | No mention |
| OTX-015 (BRD2/BRD3/BRD4) | Lewin et al. (2018) | NCT02259114 | 1b | 2018 | 46 | Single-arm | NMC (n = 10), CRPC (n = 26), NSCLC (n = 10) | 60 (20–79) |
| PLX51107 (BRD4) | Patnaik et al. (2018) | NCT02683395 | 2 | 2018 | 36 | Single-arm | Uveal melanoma (n = 11), sarcoma (n = 6), NSCLC (n = 2), breast cancer (n = 2) and CRPC (n = 2),other solid tumors (n = 13) | 60.5 (no mention) |
| INCB054329 (BRD4) | Falchook et al. (2020) | NCT02431260 | 1/2 | 2020 | 69 | Single-arm | Prostate cancer(n = 9), CRC (n = 8), breast cancer (n = 6), ovarian cancer (n = 5), lymphoma (n = 4), AML (n = 3), pancreatic cancer (n = 2), MDS (n = 1), other (n = 31) | 63 (18–87) |
| INCB057643 (BRD4) | Falchook et al. (2020) | NCT02711137 | 1/2 | 2020 | 134 | Single-arm | Prostate cancer (n = 15), colorectal cancer (n = 9), breast cancer (n = 18), ovarian cancer (n = 16), lymphoma (n = 20), AML (n = 12), pancreatic cancer (n = 7), glioblastoma (n = 7), MDS (n = 5), other (n = 25) | 66 (19–84) |
| FT-1101 (BRD4) | Patel et al. (2019) | NCT02543879 | 1 | 2019 | 94 | Single-arm | AML/MDS (n = 84), NHL (n = 10) | AML/MDS: 74 (35–92), NHL: 7341–82) |
| CC-90010 (BRD2/4) | Moreno et al. (2020) | NCT03220347 | 1 | 2020 | 69 | Single-arm | Solid tumor (n = 67), NHL (n = 2) | 57 (21–80) |
| ODM-207 (BRDT/BRD2/BRD3/BRD4) | Ameratunga et al. (2020) | NCT03035591 | 1 | 2020 | 35 | Single-arm | CRPC (n = 12), melanoma (n = 5), NMC (n = 4), ER+BC (n = 4), other (n = 10) | 60 (17–78) |
Note: R/R, relapsed/refractory; AML, acute myeloid leukemia; ALL, acute lymphoblastic leukemia; MDS, myelodysplastic syndrome; NHL, non-hodgkin’s lymphoma; NSCLC: non-small cell lung cancer; CRPC, castration-resistant prostate cancer; RA, refractory anemia; CRC, colorectal cancer; NUT, Nuclear protein of the testis; NMC, NUT midline carcinoma; ER+BC, estrogen receptor positive breast cancer.