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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   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
  RG-6146, JQ2     R/R: AML, MDS   1 Recruitment completed  
CPI-0610*   NA Benzoisoxazoloazepine 2-time potent for BRD4 than BRD2, 3, T R/R: MM   1 Recruitment completed Constellation Pharmaceuticals
     6-time potent for BDII than BDI R/R: DLBCL, follicular lymphoma   1 Preliminary analysis released  
      R/R: AML, MDS   1/2 Recruiting  
      Lymphoma   1 Active, not recruiting  
GSK525762 I-BET762 Molibresib Benzodiazepine Pan BET inhibitor R/R: AML, MDS, NHL None 1/2 Recruiting GlaxoSmithKline
INCB054329    Diazaacenaphthylen More potent to BRD2, 3, 4 than BRDT Advanced hematologic malignancies None 1/2 Recruitment completed Incyte Corporation
BMS-986158   NA Carboline based   Advanced hematologic malignancies Nivolumab 1/2a Recruiting Bristol-Myers Squibb
MK-8628* OTX-015 Birabresib Methyltriazolodiazepines Pan BET inhibitor Hematologic malignancies   1b Reported Merck Sharp & Dohme Corp
      De novo and sAML, DLBCL   1 Active, not recruiting  
ABBV-075   Mivebresib Ethanesulfonamide More potent to BRD2,4,T than BRD3 AML, MM, NHL Venetoclax 1 Recruiting AbbVie Inc
ABBV-744   NA   highly BDII-selective R/R: AML   1 Recruiting AbbVie Inc
AZD5153   NA Triazolopyridazine Bivalent inhibitor R/R: lymphoma   1 Recruiting AstraZeneca
  1. *trial results released. R/R: relapsed/refractory