All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

tucidinostat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
histone deacetylase inhibitors	4973	743420-02-2

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: tucidinostat chidamide epidaza C5055 HBI-8000 CS-055 hiyasta CS055

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. Molecular weight: 390.42 Formula: C22H19FN4O2 CLOGP: 1.86 LIPINSKI: 0 HAC: 6 HDO: 3 TPSA: 97.11 ALOGS: -5.22 ROTB: 6

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2B,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK1,GRK2,GRK3,ITK,JAK2,KIT,MAP2K6,MAP3K21,MAP3K7,MAPK12,MAPK7,MARK4,MELK,MET,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK	43
kinase-selectivity-class	AXL,DYRK1B,GRK2,PDK4,TTK	5
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

Date	Agency	Company	Orphan
June 23, 2021	PMDA	HUYA JAPAN G.K.
Dec. 23, 2014	China Food and Drug Administration (CFDA)

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Myelosuppression	224.27	104.81	51	367	53540	90574489

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Myelosuppression	225.03	67.82	56	365	40405	42580509

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Myelosuppression	338.94	80.50	90	861	94250	110494098
Hypokalaemia	91.90	80.50	40	911	182408	110405940
Thrombocytopenia	89.17	80.50	48	903	348837	110239511

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01XH06	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Histone deacetylase (HDAC) inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agent
CHEBI has role	CHEBI:64946	anti-HIV agent

Related Drugs by ATC class:

L01XH Histone deacetylase (HDAC) inhibitors 4 drugs

belinostatpanobinostatromidepsinvorinostat

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Peripheral T-cell lymphoma	indication	109977009
Relapsed or refractory T-cell leukemia-lymphoma	indication	110007008	DOID:5603

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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 2	Enzyme	Q92769	HDAC2_HUMAN	INHIBITOR	IC50	6.80		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Histone deacetylase 1	Enzyme	Q13547	HDAC1_HUMAN	INHIBITOR	IC50	7.02		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Histone deacetylase 3	Enzyme	O15379	HDAC3_HUMAN	INHIBITOR	IC50	7.17		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Histone deacetylase 10	Enzyme	Q969S8	HDA10_HUMAN	INHIBITOR	IC50	7.11		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Histone deacetylase 8	Enzyme	Q9BY41	HDAC8_HUMAN	INHIBITOR	IC50	6.14		SCIENTIFIC LITERATURE
Histone deacetylase 11	Enzyme	Q96DB2	HDA11_HUMAN	INHIBITOR	IC50	6.37		SCIENTIFIC LITERATURE
Nicotinamide phosphoribosyltransferase	Enzyme	P43490	NAMPT_HUMAN		IC50	5.68		CHEMBL

External reference:

ID	Source
87CIC980Y0	UNII
C2932486	UMLSCUI
CHEBI:135918	CHEBI
CHEMBL3621988	ChEMBL_ID
12136798	PUBCHEM_CID
DB06334	DRUGBANK_ID
10318	INN_ID
8305	IUPHAR_LIGAND_ID
D10993	KEGG_DRUG
019181	NDDF
1616493-44-7	SECONDARY_CAS_RN
C000613826	MESH_SUPPLEMENTAL_RECORD_UI
87CIC980Y0	INXIGHT DRUGS

Pharmaceutical products:

None