Table 1 The list of BET inhibitors in clinical trials in hematologic malignancies
From: Super-enhancers: critical roles and therapeutic targets in hematologic malignancies
Drug name | Other name | Trade name | Structure | Class (target) | Disease | Combination | Phase | Status | Company |
|---|---|---|---|---|---|---|---|---|---|
FT-1101 | Â | NA | Unrelated to JQ1 | Pan BET inhibitor | R/R: AML, MDS, NHL | Azacitidine | 1 | Recruiting | Forma Therapeutics |
RO6870810 | TEN-010 | NA | An analog of JQ1 | Pan BET inhibitor | R/R: MM | Daratumumab | 1b | Recruiting | Hoffmann-La Roche |
| Â | RG-6146, JQ2 | Â | Â | Â | R/R: AML, MDS | Â | 1 | Recruitment completed | Â |
CPI-0610* | Â | NA | Benzoisoxazoloazepine | 2-time potent for BRD4 than BRD2, 3, T | R/R: MM | Â | 1 | Recruitment completed | Constellation Pharmaceuticals |
| Â | Â | Â | Â | 6-time potent for BDII than BDI | R/R: DLBCL, follicular lymphoma | Â | 1 | Preliminary analysis released | Â |
| Â | Â | Â | Â | Â | R/R: AML, MDS | Â | 1/2 | Recruiting | Â |
| Â | Â | Â | Â | Â | Lymphoma | Â | 1 | Active, not recruiting | Â |
GSK525762 | I-BET762 | Molibresib | Benzodiazepine | Pan BET inhibitor | R/R: AML, MDS, NHL | None | 1/2 | Recruiting | GlaxoSmithKline |
INCB054329 | Â | Â | Diazaacenaphthylen | More potent to BRD2, 3, 4 than BRDT | Advanced hematologic malignancies | None | 1/2 | Recruitment completed | Incyte Corporation |
BMS-986158 | Â | NA | Carboline based | Â | Advanced hematologic malignancies | Nivolumab | 1/2a | Recruiting | Bristol-Myers Squibb |
MK-8628* | OTX-015 | Birabresib | Methyltriazolodiazepines | Pan BET inhibitor | Hematologic malignancies | Â | 1b | Reported | Merck Sharp & Dohme Corp |
| Â | Â | Â | Â | Â | De novo and sAML, DLBCL | Â | 1 | Active, not recruiting | Â |
ABBV-075 | Â | Mivebresib | Ethanesulfonamide | More potent to BRD2,4,T than BRD3 | AML, MM, NHL | Venetoclax | 1 | Recruiting | AbbVie Inc |
ABBV-744 | Â | NA | Â | highly BDII-selective | R/R: AML | Â | 1 | Recruiting | AbbVie Inc |
AZD5153 | Â | NA | Triazolopyridazine | Bivalent inhibitor | R/R: lymphoma | Â | 1 | Recruiting | AstraZeneca |