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

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

Stem definition	Drug id	CAS RN
histone deacetylase inhibitors	4876	414864-00-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: belinostat beleodaq PXD101	a hydroxamate-type inhibitor of histone deacetylase Molecular weight: 318.35 Formula: C15H14N2O4S CLOGP: 0.96 LIPINSKI: 0 HAC: 6 HDO: 3 TPSA: 95.50 ALOGS: -4.05 ROTB: 4 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

None

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	0.80 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	23.60 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.06 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.60 hours	Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	1.857		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	1.294		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	39.537	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	20.417	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	13.870	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	21.130	%	High	1
herg	hERG pIC50	4.335	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	12.274	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	13.152	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	8.900	%	High	1
kinase-safety-class	ACVR2A,ACVR2B,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IKBKB,ITK,JAK1,JAK2,JAK3,KIT,MAP2K1,MAP2K6,MAP3K21,MAP3K7,MAPK1,MAPK10,MAPK12,MAPK7,MAPK8,MAPK9,MAPKAPK2,MAPKAPK5,MARK4,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIK3CG,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ZAP70	60
kinase-selectivity-class	AURKA,AXL,DDR1,DYRK1B,ERBB2,GRK2,MAP2K6,MAPK7,MTOR,PDK4,PIK3CB,PIK3CD,PIK3CG,SIK2,STK33,TEK	16
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	3.972		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	218.273		High	1
mppb	Mouse plasma protein binding (% unbound)	13.870		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	6.138		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pppb	Pig plasma protein binding (% unbound)	23.940	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	152.405	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	86.320	%	High	1
rppb	Rat plasma protein binding (% unbound)	12.500	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	632.412	uM	High	1

Approvals:

Date	Agency	Company	Orphan
July 3, 2014	FDA	SPECTRUM PHARMS

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
Disease progression	52.22	45.78	21	373	156594	90471459

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
Disease progression	68.96	35.56	34	496	143622	42477183

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
Disease progression	89.54	39.08	40	720	243994	110344545

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01XH04	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Histone deacetylase (HDAC) inhibitors
FDA MoA	N0000175071	Histone Deacetylase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D056572	Histone Deacetylase Inhibitors
FDA EPC	N0000175588	Histone Deacetylase Inhibitor
CHEBI has role	CHEBI:35610	antineoplastic agent
CHEBI has role	CHEBI:61115	EC 3.5.1.98 (histone deacetylase) inhibitor

Related Drugs by ATC class:

L01XH Histone deacetylase (HDAC) inhibitors 4 drugs

panobinostatromidepsintucidinostatvorinostat

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

Disease	Relation	SNOMED_ID	DOID
Peripheral T-cell lymphoma	indication	109977009

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.83	acidic
pKa2	9.83	acidic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
500MG/VIAL	BELEODAQ	ACROTECH BIOPHARMA	N206256	July 3, 2014	RX	POWDER	INTRAVENOUS	6888027	Aug. 10, 2026	TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY PERIPHERAL T-CELL LYMPHOMA (PTCL).

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 4	Enzyme	P56524	HDAC4_HUMAN	INHIBITOR	IC50	7.57		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Histone deacetylase 5	Enzyme	Q9UQL6	HDAC5_HUMAN	INHIBITOR	Ki	7.60		CHEMBL	CHEMBL
Histone deacetylase 2	Enzyme	Q92769	HDAC2_HUMAN	INHIBITOR	Ki	9.07		CHEMBL	CHEMBL
Histone deacetylase 1	Enzyme	Q13547	HDAC1_HUMAN	INHIBITOR	Ki	9.07		CHEMBL	CHEMBL
Histone deacetylase 3	Enzyme	O15379	HDAC3_HUMAN	INHIBITOR	Ki	8.82		CHEMBL	CHEMBL
Histone deacetylase 6	Enzyme	Q9UBN7	HDAC6_HUMAN	INHIBITOR	Ki	8.80		CHEMBL	CHEMBL
Histone deacetylase 7	Enzyme	Q8WUI4	HDAC7_HUMAN	INHIBITOR	Ki	7.29		CHEMBL	CHEMBL
Histone deacetylase 8	Enzyme	Q9BY41	HDAC8_HUMAN	INHIBITOR	Ki	7.66		CHEMBL	CHEMBL
Histone deacetylase 9	Enzyme	Q9UKV0	HDAC9_HUMAN	INHIBITOR	Ki	7.62		CHEMBL	CHEMBL
Histone deacetylase 10	Enzyme	Q969S8	HDA10_HUMAN	INHIBITOR	Ki	7.23		CHEMBL	CHEMBL
Histone deacetylase 11	Enzyme	Q96DB2	HDA11_HUMAN	INHIBITOR	Ki	7.57		CHEMBL	CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform	Kinase	P42336	PK3CA_HUMAN		IC50	8.54		CHEMBL
Aspartyl/asparaginyl beta-hydroxylase	Enzyme	Q12797	ASPH_HUMAN		IC50	5.51		CHEMBL
Bromodomain-containing protein 4	Nuclear other	O60885	BRD4_HUMAN		IC50	7.57		CHEMBL
Histone deacetylase	Enzyme		Q9XYC7_PLAFA		IC50	6.67		CHEMBL

External reference:

ID	Source
D08870	KEGG_DRUG
4033540	VUID
N0000190861	NUI
866323-14-0	SECONDARY_CAS_RN
4033540	VANDF
CHEBI:61076	CHEBI
5OG	PDB_CHEM_ID
CHEMBL408513	ChEMBL_ID
C487081	MESH_SUPPLEMENTAL_RECORD_UI
7496	IUPHAR_LIGAND_ID
DB05015	DRUGBANK_ID
1543543	RXNORM
222033	MMSL
30383	MMSL
d08271	MMSL
015607	NDDF
704194004	SNOMEDCT_US
704195003	SNOMEDCT_US
C1948068	UMLSCUI
8823	INN_ID
6918638	PUBCHEM_CID
F4H96P17NZ	UNII
F4H96P17NZ	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Beleodaq	Human Prescription Drug Label	1	72893-002	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	500 mg	INTRAVENOUS	NDA	29 sections