panobinostat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
histone deacetylase inhibitors 4682 404950-80-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • farydak
  • panobinostat lactate
  • panobinostat lactate anhydrous
  • panobinostat
  • LBH-589
  • LBH589
An indole and hydroxamic acid derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used as an antineoplastic agent in combination with BORTEZOMIB and DEXAMETHASONE for the treatment of MULTIPLE MYELOMA.
  • Molecular weight: 349.43
  • Formula: C21H23N3O2
  • CLOGP: 2.42
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 4
  • TPSA: 77.15
  • ALOGS: -5.25
  • ROTB: 7

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
CL (Clearance) 10.20 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.10 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 13.10 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Aug. 28, 2015 EMA
Feb. 23, 2015 FDA NOVARTIS PHARMS CORP

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Malignant neoplasm progression 90.03 34.67 42 1443 82079 63405458
Diarrhoea 88.83 34.67 95 1390 715271 62772266
Platelet count decreased 81.84 34.67 44 1441 116078 63371459
Death 61.24 34.67 58 1427 374323 63113214
Thrombocytopenia 61.03 34.67 40 1445 151117 63336420
Plasma cell myeloma 47.58 34.67 21 1464 35884 63451653
Plasmacytoma 46.37 34.67 11 1474 2568 63484969

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Diarrhoea 102.38 34.11 118 1899 389794 34565120
Platelet count decreased 93.04 34.11 67 1950 119650 34835264
Malignant neoplasm progression 84.13 34.11 56 1961 87990 34866924
Morganella infection 48.11 34.11 10 2007 512 34954402
Bronchial haemorrhage 45.06 34.11 10 2007 699 34954215
Thrombocytopenia 39.98 34.11 47 1970 156200 34798714

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Platelet count decreased 158.61 32.97 97 3027 194567 79546697
Malignant neoplasm progression 137.52 32.97 78 3046 135912 79605352
Diarrhoea 124.16 32.97 161 2963 880328 78860936
Thrombocytopenia 74.49 32.97 70 3054 265189 79476075
Plasma cell myeloma 63.14 32.97 34 3090 53225 79688039
Death 51.98 32.97 85 3039 566429 79174835
Plasmacytoma 47.75 32.97 14 3110 4389 79736875
Morganella infection 44.29 32.97 10 3114 1117 79740147
Bronchial haemorrhage 42.71 32.97 10 3114 1310 79739954
White blood cell count decreased 40.39 32.97 43 3081 188245 79553019
Pneumonia 35.53 32.97 79 3045 660167 79081097

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XH03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Histone deacetylase (HDAC) inhibitors
FDA MoA N0000175071 Histone Deacetylase Inhibitors
FDA EPC N0000175588 Histone Deacetylase Inhibitor
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D056572 Histone Deacetylase Inhibitors
FDA MoA N0000182137 Cytochrome P450 2D6 Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:61115 histone deacetylase inhibitors

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

DiseaseRelationSNOMED_IDDOID
Multiple myeloma indication 109989006 DOID:9538
Primary cutaneous T-cell lymphoma indication 400122007




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.83 acidic
pKa2 13.3 acidic
pKa3 9.33 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 10MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 DISCN CAPSULE ORAL 8883842 June 13, 2028 TREATMENT OF MULTIPLE MYELOMA, IN COMBINATION WITH BORTEZOMIB AND DEXAMETHASONE
EQ 15MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 DISCN CAPSULE ORAL 8883842 June 13, 2028 TREATMENT OF MULTIPLE MYELOMA, IN COMBINATION WITH BORTEZOMIB AND DEXAMETHASONE
EQ 20MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 DISCN CAPSULE ORAL 8883842 June 13, 2028 TREATMENT OF MULTIPLE MYELOMA, IN COMBINATION WITH BORTEZOMIB AND DEXAMETHASONE

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histone deacetylase 11 Enzyme INHIBITOR Ki 8.46 CHEMBL DRUG LABEL
Histone deacetylase 7 Enzyme INHIBITOR Ki 8.64 CHEMBL DRUG LABEL
Histone deacetylase 8 Enzyme INHIBITOR Ki 7.66 CHEMBL DRUG LABEL
Histone deacetylase 4 Enzyme INHIBITOR Ki 9.22 CHEMBL DRUG LABEL
Histone deacetylase 9 Enzyme INHIBITOR Ki 8.92 CHEMBL DRUG LABEL
Histone deacetylase 10 Enzyme INHIBITOR Ki 7.51 CHEMBL DRUG LABEL
Histone deacetylase 5 Enzyme INHIBITOR Ki 9.15 CHEMBL DRUG LABEL
Histone deacetylase 2 Enzyme INHIBITOR Ki 9.19 CHEMBL DRUG LABEL
Histone deacetylase 1 Enzyme INHIBITOR Ki 9 CHEMBL DRUG LABEL
Histone deacetylase 3 Enzyme INHIBITOR Ki 8.96 CHEMBL DRUG LABEL
Histone deacetylase 6 Enzyme INHIBITOR Ki 9.15 CHEMBL DRUG LABEL
Bromodomain-containing protein 4 Unclassified IC50 8.30 CHEMBL
Histone deacetylase Enzyme IC50 8 IUPHAR
Histone deacetylase 8 Unclassified IC50 6.35 CHEMBL
Protein Tat Unclassified EC50 6.89 CHEMBL
Histone deacetylase Enzyme IC50 8.74 CHEMBL

External reference:

IDSource
D10019 KEGG_DRUG
960055-56-5 SECONDARY_CAS_RN
4034263 VANDF
CHEBI:85990 CHEBI
LBH PDB_CHEM_ID
CHEMBL483254 ChEMBL_ID
CHEMBL3545368 ChEMBL_ID
7489 IUPHAR_LIGAND_ID
8805 INN_ID
DB06603 DRUGBANK_ID
9647FM7Y3Z UNII
1603349 RXNORM
232927 MMSL
30903 MMSL
d08348 MMSL
015928 NDDF
015929 NDDF
429068009 SNOMEDCT_US
429398005 SNOMEDCT_US
734519004 SNOMEDCT_US
C1998098 UMLSCUI
D000077767 MESH_DESCRIPTOR_UI
6918837 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
FARYDAK HUMAN PRESCRIPTION DRUG LABEL 1 0078-0650 CAPSULE 10 mg ORAL NDA 30 sections
FARYDAK HUMAN PRESCRIPTION DRUG LABEL 1 0078-0651 CAPSULE 15 mg ORAL NDA 30 sections
FARYDAK HUMAN PRESCRIPTION DRUG LABEL 1 0078-0652 CAPSULE 20 mg ORAL NDA 30 sections
FARYDAK HUMAN PRESCRIPTION DRUG LABEL 1 73116-100 CAPSULE 10 mg ORAL NDA 34 sections
FARYDAK HUMAN PRESCRIPTION DRUG LABEL 1 73116-101 CAPSULE 15 mg ORAL NDA 34 sections
FARYDAK HUMAN PRESCRIPTION DRUG LABEL 1 73116-102 CAPSULE 20 mg ORAL NDA 34 sections