chidamide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 4973 | 743420-02-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An orally bioavailable benzamide-type inhibitor of histone deacetylase (HDAC) isoenzymes 1, 2, 3 and 10, with potential antineoplastic activity. Chidamide binds to and inhibits HDACs, leading to an increase of acetylation levels of histone proteins. This agent also inhibits the expression of kinases in the PI3K/Akt and MAPK/Ras signaling pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis. This may inhibit tumor cell proliferation in susceptible tumor cells. HDACs, a class of enzymes that deacetylate chromatin histone proteins, are upregulated in many tumor types and play key roles in gene expression. Compared to some other benzamide-type HDAC inhibitors, chidamide is more stable, more resistant to degradation and has a longer half-life.
|
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 23, 2014 | China Food and Drug Administration (CFDA) |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
Pharmacologic Action:
None
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Peripheral T-cell lymphoma | indication | 109977009 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.63 | acidic |
| pKa2 | 11.87 | acidic |
| pKa3 | 4.26 | Basic |
| pKa4 | 3.32 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Histone deacetylase 3 | Enzyme | INHIBITOR | IC50 | 7.17 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Histone deacetylase 1 | Enzyme | INHIBITOR | IC50 | 7.02 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Histone deacetylase 2 | Enzyme | INHIBITOR | IC50 | 6.80 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Histone deacetylase 10 | Enzyme | INHIBITOR | IC50 | 7.11 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Histone deacetylase 8 | Enzyme | INHIBITOR | IC50 | 6.13 | SCIENTIFIC LITERATURE | ||||
| Histone deacetylase 11 | Enzyme | INHIBITOR | IC50 | 6.36 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| C2932486 | UMLSCUI |
| CHEBI:135918 | CHEBI |
| CHEMBL3621988 | ChEMBL_ID |
| DB06334 | DRUGBANK_ID |
| C000613826 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9800555 | PUBCHEM_CID |
| 10318 | INN_ID |
| 87CIC980Y0 | UNII |
Pharmaceutical products:
None