Drug Information
| Drug General Information | Top | |||
|---|---|---|---|---|
| Drug ID |
D02YNI
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| Former ID |
DIB004417
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| Drug Name |
OTX-015
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| Synonyms |
MK 8628
Click to Show/Hide
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| Drug Type |
Small molecular drug
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| Indication | Acute myeloid leukaemia [ICD-11: 2A60; ICD-9: 205] | Phase 1/2 | [1] | |
| Myelodysplastic syndrome [ICD-11: 2A37; ICD-9: 238.7] | Phase 1 | [2], [3], [4] | ||
| Solid tumour/cancer [ICD-11: 2A00-2F9Z; ICD-10: C76-C80; ICD-9: 140-229] | Phase 1 | [5] | ||
| Company |
Constellation pharmaceuticals
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| Structure |
 |
Download2D MOL |
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| Formula |
C25H22ClN5O2S
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| Canonical SMILES |
CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NC4=CC=C(C=C4)O)C5=CC=C(C=C5)Cl)C
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| InChI |
1S/C25H22ClN5O2S/c1-13-14(2)34-25-22(13)23(16-4-6-17(26)7-5-16)28-20(24-30-29-15(3)31(24)25)12-21(33)27-18-8-10-19(32)11-9-18/h4-11,20,32H,12H2,1-3H3,(H,27,33)/t20-/m0/s1
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| InChIKey |
GNMUEVRJHCWKTO-FQEVSTJZSA-N
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| CAS Number |
CAS 202590-98-5
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| PubChem Compound ID | ||||
| Target and Pathway | Top | |||
|---|---|---|---|---|
| Target(s) | Bromodomain and extraterminal domain protein (BET) | Target Info | Inhibitor | [6] |
| Bromodomain-containing protein 2 (BRD2) | Target Info | Modulator | [7], [8], [9] | |
| Bromodomain-containing protein 4 (BRD4) | Target Info | Modulator | [7], [8], [9] | |
| KEGG Pathway | SNARE interactions in vesicular transport | |||
| NetPath Pathway | TGF_beta_Receptor Signaling Pathway | |||
| Pathway Interaction Database | Regulation of retinoblastoma protein | |||
| Reactome | COPII (Coat Protein 2) Mediated Vesicle Transport | |||
| WikiPathways | Chemical Compounds to monitor Proteins | |||
| miR-targeted genes in squamous cell - TarBase | ||||
| miR-targeted genes in muscle cell - TarBase | ||||
| miR-targeted genes in lymphocytes - TarBase | ||||
| References | Top | |||
|---|---|---|---|---|
| REF 1 | ClinicalTrials.gov (NCT02303782) A Study Assessing tOTX015 in Combination With Azacitidine (AZA) or AZA Single Agent in Patients With Newly-diagnosed Acute Myeloid Leukemia (AML) Not Candidate for Standard Intensive Induction Therapy (SIIT). U.S. National Institutes of Health. | |||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8359). | |||
| REF 3 | Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. | |||
| REF 4 | Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468(7327):1119-23. | |||
| REF 5 | Small molecules, big targets: drug discovery faces the protein-protein interaction challenge.Nat Rev Drug Discov. 2016 Aug;15(8):533-50. | |||
| REF 6 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||
| REF 7 | Targeting bromodomains: epigenetic readers of lysine acetylation.Nat Rev Drug Discov.2014 May;13(5):337-56. | |||
| REF 8 | BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells. Oncotarget. 2015 Jul 10;6(19):17698-712. | |||
| REF 9 | The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs.Clin Cancer Res.2015 Apr 1;21(7):1628-38. | |||
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