Table 1.
List of BETi in preclinical and clinical phase. So far, Apabetalone is the only one in clinical trials for CVD
| Drugs | Targets | Stage |
|---|---|---|
| Apabetalone (RVX-208) | BD2 domain | Clinical phase 3 for CVD |
| BI 2536 | BRD4 | Clinical phase 2 |
| I-BET-762 (Malibresib) | BRD2, BRD3, BRD4, BRDT | Clinical phase 2 |
| CPI-0610 | BD1 domain, BRD2, BRD4 | Clinical phase 2 |
| INCB054329 | BRD2, BRD3, BRD4, BRDT | Clinical phase 1/2 |
| PLX51107 | BRD2, BRD3, BRD4, BRDT | Clinical phase 1 |
| AZD5153 | BRD4 | Clinical phase 1 |
| Birabresib (OTX015) | BRD2, BRD3, BRD4 | Clinical phase 1 |
| CPI-203 | BRD4 | Preclinical |
| GSK1324726A (I-BET726( | BRD2, BRD3, BRD4 | Preclinical |
| Bromosporine | BRD2, BRD4 | Preclinical |
| BI 894999 | BRD4 | Preclinical |
| JQ1 | BRD2, BRD3, BRD4, BRDT | Preclinical |
| I-BET151 (GSK1210151A) | BRD2, BRD3, BRD4 | Preclinical |
| PFI-1 (PF-640S761) | BRD2, BRD4 | Preclinical |