Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C23H29N3O5 |
| Molecular Weight | 427.4935 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
ONC(=O)CCCCCCC(=O)NC1=CC=C(CN[C@H](C(O)=O)C2=CC=CC=C2)C=C1
InChI
InChIKey=BKOTWGYGBLTPKM-QFIPXVFZSA-N
InChI=1S/C23H29N3O5/c27-20(10-6-1-2-7-11-21(28)26-31)25-19-14-12-17(13-15-19)16-24-22(23(29)30)18-8-4-3-5-9-18/h3-5,8-9,12-15,22,24,31H,1-2,6-7,10-11,16H2,(H,25,27)(H,26,28)(H,29,30)/t22-/m0/s1
| Molecular Formula | C23H29N3O5 |
| Molecular Weight | 427.4935 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Tefinostat (also known as CHR-2845) was developed as an innovative oral HDAC (histone deacetylase) inhibitor that selectively targets macrophages and monocytes – central cells of the innate immune system. Chroma Therapeutics develops tefinostat for the treatment of hematological and lymphoid malignancies. In addition, the drug is under investigation in clinical trial phase I/II for cancer-associated inflammation in hepatocellular carcinoma. The aim of this study is to find the best dose of the drug without causing side effects. Besides, Phase II of clinical trial ‘MONOCLE’ study for the treatment of chronic myelomonocytic leukemia (CMML) has been initiated and the first patient has been recruited.
Originator
Approval Year
Sample Use Guides
Up to 5 cohorts of 3-6 patients (number is dependent on DLT occurrence) will be treated for 28 days once or twice daily (360, 480mg once daily, then 240, 360, 480mg twice daily) to determine safety and tolerability of Tefinostat and to identify the recommended dose for Phase II.
Route of Administration:
Oral
| Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Apr 02 15:21:12 GMT 2025
by
admin
on
Wed Apr 02 15:21:12 GMT 2025
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| Record UNII |
35E75J4M7E
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| Record Status |
Validated (UNII)
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914604-57-2
Created by
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35E75J4M7E
Created by
admin on Wed Apr 02 15:21:12 GMT 2025 , Edited by admin on Wed Apr 02 15:21:12 GMT 2025
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15940950
Created by
admin on Wed Apr 02 15:21:12 GMT 2025 , Edited by admin on Wed Apr 02 15:21:12 GMT 2025
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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TARGET -> INHIBITOR |
Pan HDAC inhibitor
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TARGET -> INHIBITOR |
Pan HDAC inhibitor
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||
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TARGET -> INHIBITOR |
Pan HDAC inhibitor
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|
TARGET -> INHIBITOR |
Pan HDAC inhibitor
|
||
|
TARGET -> INHIBITOR |
Pan HDAC inhibitor
|
||
|
TARGET -> INHIBITOR |
Pan HDAC inhibitor
|
||
|
TARGET -> INHIBITOR |
Pan HDAC inhibitor
|
||
|
TARGET -> INHIBITOR |
Pan HDAC inhibitor
|
||
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TARGET -> INHIBITOR |
Pan HDAC inhibitor
|
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
PRODRUG -> METABOLITE ACTIVE |
cleaved to an active acid, CHR-2847, by the intracellular esterase human carboxylesterase-1 (hCE-1), the expression of which is limited to cells of monocytoid lineage and some hepatocytes, allowing selective accumulation of active drug within monocytoid cells.
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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ACTIVE MOIETY |
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