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
Diarrhoea 226.12 52.46 81 342 83483 2274179
Plasma cell myeloma 223.41 52.46 49 374 8084 2349578
Platelet count decreased 161.71 52.46 43 380 15770 2341892
Malignant neoplasm progression 148.02 52.46 38 385 12090 2345572
Thrombocytopenia 113.18 52.46 34 389 19097 2338565
Death 83.31 52.46 40 383 81428 2276234
Vomiting 78.74 52.46 37 386 71565 2286097
Nausea 76.78 52.46 42 381 112147 2245515
Febrile neutropenia 66.90 52.46 20 403 10862 2346800
Pneumonia 58.66 52.46 27 396 49269 2308393
Fatigue 55.58 52.46 31 392 84842 2272820
Hypokalaemia 54.44 52.46 17 406 10637 2347025
White blood cell count decreased 52.96 52.46 19 404 18189 2339473

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 288.15 49.05 102 386 53750 1692543
Plasma cell myeloma 200.58 49.05 53 435 9961 1736332
Platelet count decreased 196.23 49.05 58 430 16465 1729828
Malignant neoplasm progression 195.95 49.05 56 432 14102 1732191
Pneumonia 121.08 49.05 53 435 46129 1700164
Thrombocytopenia 95.21 49.05 36 452 21213 1725080
Pyrexia 76.94 49.05 39 449 46361 1699932
Nausea 64.86 49.05 36 452 51160 1695133
Fatigue 56.93 49.05 33 455 50748 1695545
Vomiting 56.92 49.05 30 458 38285 1708008
White blood cell count decreased 54.01 49.05 21 467 13128 1733165

Pharmacologic Action:

SourceCodeDescription
ATC L01XX42 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Other antineoplastic agents
FDA EPC N0000175588 Histone Deacetylase Inhibitor
FDA MoA N0000182137 Cytochrome P450 2D6 Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D056572 Histone Deacetylase Inhibitors
CHEBI has role CHEBI:50926 angiogenesis modulating agent
CHEBI has role CHEBI:35610 antineoplastic agent

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 10MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 RX CAPSULE ORAL 7067551 Aug. 31, 2021 TREATMENT OF MULTIPLE MYELOMA, IN COMBINATION WITH BORTEZOMIB AND DEXAMETHASONE
EQ 15MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 RX CAPSULE ORAL 7067551 Aug. 31, 2021 TREATMENT OF MULTIPLE MYELOMA, IN COMBINATION WITH BORTEZOMIB AND DEXAMETHASONE
EQ 20MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 RX CAPSULE ORAL 7067551 Aug. 31, 2021 TREATMENT OF MULTIPLE MYELOMA, IN COMBINATION WITH BORTEZOMIB AND DEXAMETHASONE
EQ 10MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 RX CAPSULE ORAL 6833384 Sept. 30, 2021 TREATMENT OF MULTIPLE MYELOMA, IN COMBINATION WITH BORTEZOMIB AND DEXAMETHASONE
EQ 15MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 RX CAPSULE ORAL 6833384 Sept. 30, 2021 TREATMENT OF MULTIPLE MYELOMA, IN COMBINATION WITH BORTEZOMIB AND DEXAMETHASONE
EQ 20MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 RX CAPSULE ORAL 6833384 Sept. 30, 2021 TREATMENT OF MULTIPLE MYELOMA, IN COMBINATION WITH BORTEZOMIB AND DEXAMETHASONE
EQ 10MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 RX 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 RX 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 RX 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 RX CAPSULE ORAL Feb. 23, 2020 NEW CHEMICAL ENTITY
EQ 15MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 RX CAPSULE ORAL Feb. 23, 2020 NEW CHEMICAL ENTITY
EQ 20MG BASE FARYDAK SECURA N205353 Feb. 23, 2015 RX CAPSULE ORAL Feb. 23, 2020 NEW CHEMICAL ENTITY
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
D000077767 MESH_DESCRIPTOR_UI
D10019 KEGG_DRUG
C3892978 UMLSCUI
9647FM7Y3Z UNII
8805 INN_ID
CHEMBL483254 ChEMBL_ID
960055-56-5 SECONDARY_CAS_RN
LBH PDB_CHEM_ID
DB06603 DRUGBANK_ID
CHEBI:85990 CHEBI
CHEMBL3545368 ChEMBL_ID
6918837 PUBCHEM_CID
7489 IUPHAR_LIGAND_ID
429398005 SNOMEDCT_US
429068009 SNOMEDCT_US
1603350 RXNORM
015928 NDDF
d08348 MMSL
4034263 VANDF

Pharmaceutical products:

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