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
Diarrhoea 89.38 34.73 94 1305 588382 50015343
Malignant neoplasm progression 87.74 34.73 41 1358 68083 50535642
Platelet count decreased 80.84 34.73 44 1355 100682 50503043
Thrombocytopenia 58.68 34.73 39 1360 127634 50476091
Death 54.35 34.73 55 1344 325324 50278401
Plasmacytoma 45.40 34.73 11 1388 2374 50601351
Plasma cell myeloma 40.66 34.73 19 1380 31303 50572422

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 106.41 36.12 118 1803 332580 29240026
Platelet count decreased 94.05 36.12 67 1854 104605 29468001
Malignant neoplasm progression 87.09 36.12 56 1865 73803 29498803
Morganella infection 47.95 36.12 10 1911 461 29572145
Bronchial haemorrhage 44.25 36.12 10 1911 673 29571933
Thrombocytopenia 41.11 36.12 47 1874 134776 29437830

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 157.21 32.40 97 2884 167614 64328137
Malignant neoplasm progression 136.37 32.40 77 2904 112794 64382957
Diarrhoea 126.81 32.40 160 2821 722544 63773207
Thrombocytopenia 72.87 32.40 69 2912 223732 64272019
Plasmacytoma 47.25 32.40 14 2967 3856 64491895
Death 45.04 32.40 80 2901 482625 64013126
Morganella infection 43.77 32.40 10 2971 996 64494755
Bronchial haemorrhage 41.84 32.40 10 2971 1212 64494539
White blood cell count decreased 40.79 32.40 43 2938 157794 64337957
Plasma cell myeloma 38.79 32.40 25 2956 46050 64449701
Pneumonia 34.43 32.40 78 2903 559498 63936253
Neutrophil count decreased 33.36 32.40 28 2953 77168 64418583

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 DISCN CAPSULE ORAL Feb. 23, 2022 TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST 2 PRIOR REGIMENS, INCLUDING BORTEZOMIB AND AN IMMUNOMODULATORY AGENT
EQ 15MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 DISCN CAPSULE ORAL Feb. 23, 2022 TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST 2 PRIOR REGIMENS, INCLUDING BORTEZOMIB AND AN IMMUNOMODULATORY AGENT
EQ 20MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 DISCN CAPSULE ORAL Feb. 23, 2022 TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST 2 PRIOR REGIMENS, INCLUDING BORTEZOMIB AND AN IMMUNOMODULATORY AGENT

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
6918837 PUBCHEM_CID
1603349 RXNORM
232927 MMSL
30903 MMSL
d08348 MMSL
015928 NDDF
015929 NDDF
429068009 SNOMEDCT_US
429398005 SNOMEDCT_US
734519004 SNOMEDCT_US
D000077767 MESH_DESCRIPTOR_UI
C1998098 UMLSCUI

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