panobinostat 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: 2.64
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 4
  • TPSA: 77.15
  • ALOGS: -5.25
  • ROTB: 7

  • Status: ONP

  • 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
Plasma cell myeloma 206.13 38.50 70 1415 44408 46640169
Malignant neoplasm progression 87.13 38.50 42 1443 64884 46619693
Diarrhoea 82.24 38.50 94 1391 559508 46125069
Platelet count decreased 80.68 38.50 46 1439 99978 46584599
Thrombocytopenia 58.64 38.50 41 1444 126540 46558037
Death 46.52 38.50 55 1430 335493 46349084
Plasmacytoma 38.55 38.50 10 1475 2467 46682110

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
Plasma cell myeloma 211.33 34.90 91 1862 53371 29897154
Diarrhoea 100.40 34.90 115 1838 333988 29616537
Platelet count decreased 90.67 34.90 66 1887 106063 29844462
Malignant neoplasm progression 85.50 34.90 55 1898 72232 29878293
Morganella infection 49.92 34.90 10 1943 375 29950150
Bronchial haemorrhage 43.56 34.90 10 1943 719 29949806
Thrombocytopenia 37.02 34.90 45 1908 136999 29813526

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 cytostatic
CHEBI has role CHEBI:61115 hdac inhibitor

Drug Use (View source of the data)

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

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)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 RX 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 RX 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 RX 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 7 Enzyme INHIBITOR Ki 8.64 CHEMBL DRUG LABEL
Histone deacetylase 11 Enzyme INHIBITOR Ki 8.46 CHEMBL DRUG LABEL
Histone deacetylase 8 Enzyme INHIBITOR Ki 7.66 CHEMBL DRUG LABEL
Histone deacetylase 9 Enzyme INHIBITOR Ki 8.92 CHEMBL DRUG LABEL
Histone deacetylase 6 Enzyme INHIBITOR Ki 9.15 CHEMBL DRUG LABEL
Histone deacetylase 1 Enzyme INHIBITOR Ki 9 CHEMBL DRUG LABEL
Histone deacetylase 4 Enzyme INHIBITOR Ki 9.22 CHEMBL DRUG LABEL
Histone deacetylase 3 Enzyme INHIBITOR Ki 8.96 CHEMBL DRUG LABEL
Histone deacetylase 2 Enzyme INHIBITOR Ki 9.19 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 Enzyme IC50 8.74 CHEMBL

External reference:

IDSource
D10019 KEGG_DRUG
960055-56-5 SECONDARY_CAS_RN
4034263 VANDF
C3892978 UMLSCUI
CHEBI:85991 CHEBI
LBH PDB_CHEM_ID
CHEMBL483254 ChEMBL_ID
CHEMBL3545368 ChEMBL_ID
D000077767 MESH_DESCRIPTOR_UI
DB06603 DRUGBANK_ID
7489 IUPHAR_LIGAND_ID
8805 INN_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

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