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BRD4 is a reader protein that docks on acetylated DNA packaging and pulls in the machinery that switches growth genes such as MYC on. BET inhibitors such as pelabresib and ZEN-3694 block that docking; in NUT carcinoma the cancer's own driver is a BRD4 fusion. This dossier gathers the 3 products (1 approved), 7 trials, 0 pathways and 0 resistance routes in the corpus that involve it, with external identifiers so it can be joined to UniProt, ChEMBL, Open Targets and the rest of biology.
The ZEN-3694 record describes BET inhibitors as blocking the bromodomain proteins that switch on growth genes such as MYC, with objective but short-lived responses in early NUT carcinoma trials of molibresib and birabresib; the epigenetic-reprogramming pathway record lists BET proteins among the chromatin readers hijacked in cancer.
| Modality | Approved | Phase 3 | Phase 2 |
|---|---|---|---|
| Small molecule 3 |
| Trial | Setting | Result | Products | ||
|---|---|---|---|---|---|
MANIFEST-2 NCT04603495 | 3 | Mixed | JAK inhibitor-naive myelofibrosis: ruxolitinib with the BET inhibitor pelabresib or placebo | Pelabresib plus ruxolitinib roughly doubled the week-24 spleen volume response over ruxolitinib alone; the symptom endpoint did not reach significance. | |
| 3 | Recruiting | An Open-Label, Multicenter, Extension Study for Patients Previously Enrolled in Studies With Pelabresib | - | ||
| 2 | Recruiting | Phase 2 Trial of ZEN003694 in Squamous Cell Lung Cancer Patients Harboring NSD3 Amplification | - | ||
| 2 | Recruiting | A Randomized Phase 2b Study of ZEN003694 in Combination With Enzalutamide Versus Enzalutamide Monotherapy in Patients With Metastatic Castration-Resistant Prostate Cancer | - | ||
| 1/2 | Active | A Phase 1b/2 Study of BMS-986158 Monotherapy and in Combination With Either Ruxolitinib or Fedratinib in Participants With DIPSS-Intermediate or High Risk Myelofibrosis | - | ||
| 1/2 | Recruiting | Advanced, metastatic or unresectable NUT carcinoma: the BET bromodomain inhibitor ZEN003694 added to platinum-based chemotherapy; started July 2022, 36 planned | - | ||
| 1 | Recruiting | NUT carcinoma, advanced breast cancer and other solid tumours: BET inhibitor ZEN003694 with the CDK4/6 inhibitor abemaciclib; started August 2023, 45 planned | - |
No recorded escape route names this target.
No pathway diagram carries this target as a node.
No companion diagnostic in the registry measures this target.
No model entry for this target yet; check the cancer entries on the models page.
No open questions recorded for this target yet. Suggest one.
Query for this target: (TITLE:"BRD4" OR ABSTRACT:"BRD4" OR TITLE:"BET" OR ABSTRACT:"BET" OR TITLE:"BET bromodomain proteins BRD2, BRD3, BRD4, BRDT" OR ABSTRACT:"BET bromodomain proteins BRD2, BRD3, BRD4, BRDT" OR TITLE:"bromodomain containing 4" OR ABSTRACT:"bromodomain containing 4" OR TITLE:"MCAP" OR ABSTRACT:"MCAP" OR TITLE:"HUNK1" OR ABSTRACT:"HUNK1") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about BRD4, not a curated reading list.
The dossier as machine-readable JSON, at /api/v1/dossiers/brd4.json: identifiers from HGNC, Ensembl, UniProt and ChEMBL, products with status, trials, pathways, hotspots, open questions and assays. The full entity record is in the open API at /api/v1/entities/brd4.json. Licence CC BY-NC 4.0.