Stem definition | Drug id | CAS RN |
---|---|---|
histone deacetylase inhibitors | 4682 | 404950-80-7 |
None
Property | Value | Reference |
---|---|---|
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 |
Date | Agency | Company | Orphan |
---|---|---|---|
Aug. 28, 2015 | EMA | ||
Feb. 23, 2015 | FDA | NOVARTIS PHARMS CORP |
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 |
---|---|---|---|---|---|---|
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 |
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 |
---|---|---|---|---|---|---|
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 |
Source | Code | Description |
---|---|---|
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 |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Multiple myeloma | indication | 109989006 | DOID:9538 |
Primary cutaneous T-cell lymphoma | indication | 400122007 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 9.83 | acidic |
pKa2 | 13.3 | acidic |
pKa3 | 9.33 | Basic |
None
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
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 |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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 |
ID | Source |
---|---|
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 |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
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 |