birabresib
Small moleculeexperimental
Birabresib is an experimental small molecule inhibitor of BRD2, BRD3, and BRD4 under investigation for the treatment of cancer. It is in development by Merck & Co. It is currently in clinical trials for leukemia and glioblastoma. — Wikipedia
Clinical trial activity
6 trials · 2 clinical orgs · 0 marketing orgs
Phase 1
6
Phase 2
2
Phase 3
0
Phase 4
0
Earliest trial started Dec 1, 2012 (NCT01713582)
Timeline
2010s
- Jan 1, 2012
Earliest Phase 1 Sponsor(trial)
Indications
Studied for
- Breast Neoplasms · Phase 1
- Carcinoma · Phase 1
- Carcinoma, Non-Small-Cell Lung · Phase 1
- Glioblastoma · Phase 1/Phase 2
- Leukemia, Myeloid, Acute · Phase 1/Phase 2
- Lymphoma, Large B-Cell, Diffuse · Phase 1
- Lymphoma, Large-Cell, Immunoblastic · Phase 1
- Multiple Myeloma · Phase 1
- Pancreatic Neoplasms · Phase 1
- Precursor Cell Lymphoblastic Leukemia-Lymphoma · Phase 1
- Prostatic Neoplasms, Castration-Resistant · Phase 1
- Triple Negative Breast Neoplasms · Phase 1
Mechanism of action
- Bromodomain-containing protein 2INHIBITOR
BRD2 inhibitor
- Bromodomain-containing protein 3INHIBITOR
BRD3 inhibitor
- BRD4/HDAC1INHIBITOR
BRD4/HDAC1 inhibitor
Bromodomain and extra-terminal motif (BET) inhibitor
Chemistry & pharmacology
Loading structure…
SMILES
Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=N[C@@H](CC(=O)Nc1ccc(O)cc1)c1nnc(C)n1-2- Mol. weight
- 492 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaBirabresib ↗
- ChEMBLCHEMBL3581647 ↗
Also known as
- birabresib
- birabresib
- mk-8628
- mk-8628
- mk-8628
- otx015
- otx015
- otx-015
- otx-015
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02698189 | Phase 1 | May 19, 2016 | Merck |
| NCT02698176 | Phase 1 | May 4, 2016 | Merck |
| NCT02303782 | Phase 1/Phase 2 (Phase 2) | Jan 1, 2015 | OncoEthix |
| NCT02259114 | Phase 1 | Oct 23, 2014 | Merck, OncoEthix |
| NCT02296476 | Phase 1/Phase 2 (Phase 2) | Oct 1, 2014 | OncoEthix |
| NCT01713582 | Phase 1 | Dec 1, 2012 | Merck, OncoEthix |
Showing 6 of 6 trials
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