Table 1.
Antagonists of epigenetic reader domains in clinical trials
| Antagonist | Antagonist Class | Target | Disease State | Phase(s) | NCT Number(s) |
|---|---|---|---|---|---|
| ABBV-075 | Kac Reader | BET | Advanced Cancers | I | NCT02391480 |
| Myelofibrosis | I | NCT04480086 | |||
| ABBV-744 | Kac Reader | BET (BD2) | AML | I | NCT03360006 |
| Myelofibrosis | I | NCT04454658 | |||
| BMS-986158 | Kac Reader | BET | Pediatric Tumors Lymphomas | I | NCT03936465 |
| Advanced Cancers | I-II | NCT02419417 | |||
| FT-1101 | Kac Reader | BET | Hematologic Malignancies | I | NCT02543879 |
| GS-5829 | Kac Reader | BET | Solid Tumors Lymphomas | I | NCT02392611 |
| Breast Cancer | I-II | NCT02983604 | |||
| Castration-Resistant Prostate Cancer | I-II | NCT02607228 | |||
| GSK2820151 | Kac Reader | BET | Solid Tumors | I | NCT02630251 |
| GSK4027 | Kac Reader | PCAF/GCN5 | COPD Emphysema Chronic Bronchitis | IV | NCT00175565 |
| I-BET762 (GSK525762) | Kac Reader | BET | Hematologic Malignancies | I II |
NCT03925428
NCT01943851 |
| Castration-Resistant Prostate Cancer | I | NCT03150056 | |||
| Solid Tumors | I I II |
NCT02259114
NCT03925428 NCT03266159 |
|||
| Breast Cancer | II | NCT02964507 | |||
| Carcinoma | I I-II |
NCT01587703
NCT04116359 |
|||
| INCB054329 | Kac Reader | BET | Hematologic Malignancies Solid Tumors | I-II | NCT02431260 |
| INCB-057643 | Kac Reader | BET | Myelofibrosis | I | NCT04279847 |
| Solid Tumors | I-II | NCT02959437 | |||
| MAK683 | Kme Reader | EED | DLBCL | I-II | NCT02900651 |
| MK-8628 (OTX015) | Kac Reader | BET | Hematologic Malignancies | I | NCT01713582 |
| Advanced Cancers | I | NCT02259114 | |||
| GBM | II | NCT02296476 | |||
| PLX51107 | Kac Reader | BRD4 | AML Myelodysplastic Syndromes | I | NCT04022785 |
| Hematologic Malignancies Solid Tumors | I | NCT02683395 | |||
| RO6870810 | Kac Reader | BET | AML Myelodysplastic Syndromes | I | NCT02308761 |
| Multiple Myeloma | I | NCT03068351 | |||
| Solid Tumors | I | NCT01987362 | |||
| Ovarian Cancer TNBC | I | NCT03292172 | |||
| B-cell Lymphomas | I | NCT03255096 | |||
| RVX-208 | Kac Reader | BET | Diabetes | II III |
NCT01728467
NCT02586155 |
| Fabry Disease | I-II | NCT03228940 | |||
| Kidney Failure | I-II | NCT03160430 | |||
| Cardiovascular Diseases | II I-II II III II |
NCT01058018
NCT00768274 NCT01423188 NCT02586155 NCT01067820 |
|||
| SYHA1801 | Kac Reader | BRD4 | Solid Tumors | I | NCT04309968 |
| ZEN003694 | Kac Reader | BET | Castration-Resistant Prostate Cancer | I I-II I-II II |
NCT02705469
NCT04145375 NCT02711956 NCT04471974 |
| TNBC | II | NCT03901469 |