U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C21H23N3O2
Molecular Weight 349.4262
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of PANOBINOSTAT

SMILES

CC1=C(CCNCC2=CC=C(\C=C\C(=O)NO)C=C2)C3=C(N1)C=CC=C3

InChI

InChIKey=FPOHNWQLNRZRFC-ZHACJKMWSA-N
InChI=1S/C21H23N3O2/c1-15-18(19-4-2-3-5-20(19)23-15)12-13-22-14-17-8-6-16(7-9-17)10-11-21(25)24-26/h2-11,22-23,26H,12-14H2,1H3,(H,24,25)/b11-10+

HIDE SMILES / InChI

Molecular Formula C21H23N3O2
Molecular Weight 349.4262
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 1
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including https://www.drugbank.ca/drugs/DB06603

Panobinostat is an oral deacetylace (DAC) inhibitor approved on February 23, 2015 by the FDA for the treatment of multiple myeloma. The approval was accelerated based on progression-free survival, therefore confirmatory trials by the sponsor to demonstrate clinical efficacy in multiple myeloma treatment are in progress of being conducted. Panobinostat is marketed by Novartis under the brand name Farydak. Panobinostat is a deacetylase (DAC) inhibitor. DACs, also known as histone DACs (HDAC), are responsible for regulating the acetylation of about 1750 proteins in the body; their functions are involved in many biological processes including DNA replication and repair, chromatin remodelling, transcription of genes, progression of the cell-cycle, protein degradation and cytoskeletal reorganization. In multiple myeloma, there is an overexpression of DAC proteins. Panobinostat inhibits class I (HDACs 1, 2, 3, 8), class II (HDACs 4, 5, 6, 7, 9, 10) and class IV (HDAC 11) proteins. Panobinostat's antitumor activity is believed to be attributed to epigenetic modulation of gene expression and inhibition of protein metabolism. Panobinostat also exhibits cytotoxic synergy with bortezomib, a proteasome inhibitor concurrently used in treatment of multiple myeloma.

Originator

Curator's Comment: # Novartis

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
280.0 nM [IC50]
11.0 nM [IC50]
2.1 nM [IC50]
13.0 nM [IC50]
2.5 nM [IC50]
200.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
FARYDAK

Approved Use

FARYDAK, a histone deacetylase inhibitor, in combination with bortezomib and dexamethasone, is indicated for the treatment of patients with multiple myeloma who have received at least 2 prior regimens, including bortezomib and an immunomodulatory agent

Launch Date

2015
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
15.3 ng/mL
20 mg 1 times / day multiple, oral
dose: 20 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: BORTEZOMIB
PANOBINOSTAT plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
95.2 ng × h/mL
20 mg 1 times / day multiple, oral
dose: 20 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: BORTEZOMIB
PANOBINOSTAT plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
16.7 h
20 mg 1 times / day multiple, oral
dose: 20 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: BORTEZOMIB
PANOBINOSTAT plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
10%
PANOBINOSTAT plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
34 mg/m2 3 times / week multiple, oral
Highest studied dose|RP2D
Dose: 34 mg/m2, 3 times / week
Route: oral
Route: multiple
Dose: 34 mg/m2, 3 times / week
Sources:
unhealthy, 1-21 years
n = 11
Health Status: unhealthy
Condition: relapsed and refractory hematologic malignancies
Age Group: 1-21 years
Sex: M+F
Population Size: 11
Sources:
DLT: Hypertriglyceridemia...
Dose limiting toxicities:
Hypertriglyceridemia (grade 4, 1 patient)
Sources:
15 mg/m2 1 times / week multiple, intravenous (starting)
Dose: 15 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 15 mg/m2, 1 times / week
Sources:
unhealthy, 3-17 years
n = 9
Health Status: unhealthy
Condition: refractory solid tumors
Age Group: 3-17 years
Sex: M+F
Population Size: 9
Sources:
DLT: Electrocardiogram T wave abnormal...
Dose limiting toxicities:
Electrocardiogram T wave abnormal (2 patients)
Sources:
20 mg 3 times / week multiple, oral
Recommended|MTD
Dose: 20 mg, 3 times / week
Route: oral
Route: multiple
Dose: 20 mg, 3 times / week
Co-administed with::
bortezomib(1.3 mg/m2)
dexamethasone
Sources: Page: p. 36, 45
unhealthy, 60 years (range: 28-79 years)
n = 386
Health Status: unhealthy
Age Group: 60 years (range: 28-79 years)
Sex: M+F
Population Size: 386
Sources: Page: p. 36, 45
Disc. AE: Diarrhea, Thrombocytopenia...
AEs leading to
discontinuation/dose reduction:
Diarrhea (17 patients)
Thrombocytopenia (6 patients)
Fatigue (11 patient)
Asthenia (11 patient)
Peripheral neuropathy (14 patients)
Thrombocytopenia (28%)
Sources: Page: p. 36, 45
20 mg/m2 1 times / week multiple, intravenous
Highest studied dose
Dose: 20 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / week
Sources:
unhealthy, 63.0 years (range: 43–75 years)
n = 8
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 63.0 years (range: 43–75 years)
Sex: M+F
Population Size: 8
Sources:
DLT: Gamma glutamyl transpeptidase increased...
Other AEs: Thrombocytopenia, Leukopenia...
Dose limiting toxicities:
Gamma glutamyl transpeptidase increased (grade 3, 1 patient)
Other AEs:
Thrombocytopenia (grade 3-4, 2 patients)
Leukopenia (grade 3-4, 2 patients)
Neutropenia (grade 3-4, 5 patients)
Nausea (grade 1-2, 4 patients)
Stomatitis (grade 1-2, 3 patients)
Vomiting (grade 1-2, 3 patients)
Fatigue (grade 3-4, 1 patient)
Fever (grade 1-2, 4 patients)
Decreased appetite (grade 1-2, 5 patients)
Hypoalbuminemia (grade 1-2, 2 patients)
Rash (grade 1-2, 3 patients)
Sources:
20 mg 3 times / week multiple, oral
Recommended|MTD
Dose: 20 mg, 3 times / week
Route: oral
Route: multiple
Dose: 20 mg, 3 times / week
Sources:
unhealthy
Other AEs: Diarrhea, Arrhythmia...
Other AEs:
Diarrhea (severe|grade 5, 25%)
Arrhythmia (severe)
Sources:
AEs

AEs

AESignificanceDosePopulation
Hypertriglyceridemia grade 4, 1 patient
DLT
34 mg/m2 3 times / week multiple, oral
Highest studied dose|RP2D
Dose: 34 mg/m2, 3 times / week
Route: oral
Route: multiple
Dose: 34 mg/m2, 3 times / week
Sources:
unhealthy, 1-21 years
n = 11
Health Status: unhealthy
Condition: relapsed and refractory hematologic malignancies
Age Group: 1-21 years
Sex: M+F
Population Size: 11
Sources:
Electrocardiogram T wave abnormal 2 patients
DLT
15 mg/m2 1 times / week multiple, intravenous (starting)
Dose: 15 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 15 mg/m2, 1 times / week
Sources:
unhealthy, 3-17 years
n = 9
Health Status: unhealthy
Condition: refractory solid tumors
Age Group: 3-17 years
Sex: M+F
Population Size: 9
Sources:
Asthenia 11 patient
Disc. AE
20 mg 3 times / week multiple, oral
Recommended|MTD
Dose: 20 mg, 3 times / week
Route: oral
Route: multiple
Dose: 20 mg, 3 times / week
Co-administed with::
bortezomib(1.3 mg/m2)
dexamethasone
Sources: Page: p. 36, 45
unhealthy, 60 years (range: 28-79 years)
n = 386
Health Status: unhealthy
Age Group: 60 years (range: 28-79 years)
Sex: M+F
Population Size: 386
Sources: Page: p. 36, 45
Fatigue 11 patient
Disc. AE
20 mg 3 times / week multiple, oral
Recommended|MTD
Dose: 20 mg, 3 times / week
Route: oral
Route: multiple
Dose: 20 mg, 3 times / week
Co-administed with::
bortezomib(1.3 mg/m2)
dexamethasone
Sources: Page: p. 36, 45
unhealthy, 60 years (range: 28-79 years)
n = 386
Health Status: unhealthy
Age Group: 60 years (range: 28-79 years)
Sex: M+F
Population Size: 386
Sources: Page: p. 36, 45
Peripheral neuropathy 14 patients
Disc. AE
20 mg 3 times / week multiple, oral
Recommended|MTD
Dose: 20 mg, 3 times / week
Route: oral
Route: multiple
Dose: 20 mg, 3 times / week
Co-administed with::
bortezomib(1.3 mg/m2)
dexamethasone
Sources: Page: p. 36, 45
unhealthy, 60 years (range: 28-79 years)
n = 386
Health Status: unhealthy
Age Group: 60 years (range: 28-79 years)
Sex: M+F
Population Size: 386
Sources: Page: p. 36, 45
Diarrhea 17 patients
Disc. AE
20 mg 3 times / week multiple, oral
Recommended|MTD
Dose: 20 mg, 3 times / week
Route: oral
Route: multiple
Dose: 20 mg, 3 times / week
Co-administed with::
bortezomib(1.3 mg/m2)
dexamethasone
Sources: Page: p. 36, 45
unhealthy, 60 years (range: 28-79 years)
n = 386
Health Status: unhealthy
Age Group: 60 years (range: 28-79 years)
Sex: M+F
Population Size: 386
Sources: Page: p. 36, 45
Thrombocytopenia 28%
Disc. AE
20 mg 3 times / week multiple, oral
Recommended|MTD
Dose: 20 mg, 3 times / week
Route: oral
Route: multiple
Dose: 20 mg, 3 times / week
Co-administed with::
bortezomib(1.3 mg/m2)
dexamethasone
Sources: Page: p. 36, 45
unhealthy, 60 years (range: 28-79 years)
n = 386
Health Status: unhealthy
Age Group: 60 years (range: 28-79 years)
Sex: M+F
Population Size: 386
Sources: Page: p. 36, 45
Thrombocytopenia 6 patients
Disc. AE
20 mg 3 times / week multiple, oral
Recommended|MTD
Dose: 20 mg, 3 times / week
Route: oral
Route: multiple
Dose: 20 mg, 3 times / week
Co-administed with::
bortezomib(1.3 mg/m2)
dexamethasone
Sources: Page: p. 36, 45
unhealthy, 60 years (range: 28-79 years)
n = 386
Health Status: unhealthy
Age Group: 60 years (range: 28-79 years)
Sex: M+F
Population Size: 386
Sources: Page: p. 36, 45
Hypoalbuminemia grade 1-2, 2 patients
20 mg/m2 1 times / week multiple, intravenous
Highest studied dose
Dose: 20 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / week
Sources:
unhealthy, 63.0 years (range: 43–75 years)
n = 8
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 63.0 years (range: 43–75 years)
Sex: M+F
Population Size: 8
Sources:
Rash grade 1-2, 3 patients
20 mg/m2 1 times / week multiple, intravenous
Highest studied dose
Dose: 20 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / week
Sources:
unhealthy, 63.0 years (range: 43–75 years)
n = 8
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 63.0 years (range: 43–75 years)
Sex: M+F
Population Size: 8
Sources:
Stomatitis grade 1-2, 3 patients
20 mg/m2 1 times / week multiple, intravenous
Highest studied dose
Dose: 20 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / week
Sources:
unhealthy, 63.0 years (range: 43–75 years)
n = 8
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 63.0 years (range: 43–75 years)
Sex: M+F
Population Size: 8
Sources:
Vomiting grade 1-2, 3 patients
20 mg/m2 1 times / week multiple, intravenous
Highest studied dose
Dose: 20 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / week
Sources:
unhealthy, 63.0 years (range: 43–75 years)
n = 8
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 63.0 years (range: 43–75 years)
Sex: M+F
Population Size: 8
Sources:
Fever grade 1-2, 4 patients
20 mg/m2 1 times / week multiple, intravenous
Highest studied dose
Dose: 20 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / week
Sources:
unhealthy, 63.0 years (range: 43–75 years)
n = 8
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 63.0 years (range: 43–75 years)
Sex: M+F
Population Size: 8
Sources:
Nausea grade 1-2, 4 patients
20 mg/m2 1 times / week multiple, intravenous
Highest studied dose
Dose: 20 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / week
Sources:
unhealthy, 63.0 years (range: 43–75 years)
n = 8
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 63.0 years (range: 43–75 years)
Sex: M+F
Population Size: 8
Sources:
Decreased appetite grade 1-2, 5 patients
20 mg/m2 1 times / week multiple, intravenous
Highest studied dose
Dose: 20 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / week
Sources:
unhealthy, 63.0 years (range: 43–75 years)
n = 8
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 63.0 years (range: 43–75 years)
Sex: M+F
Population Size: 8
Sources:
Gamma glutamyl transpeptidase increased grade 3, 1 patient
DLT
20 mg/m2 1 times / week multiple, intravenous
Highest studied dose
Dose: 20 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / week
Sources:
unhealthy, 63.0 years (range: 43–75 years)
n = 8
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 63.0 years (range: 43–75 years)
Sex: M+F
Population Size: 8
Sources:
Fatigue grade 3-4, 1 patient
20 mg/m2 1 times / week multiple, intravenous
Highest studied dose
Dose: 20 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / week
Sources:
unhealthy, 63.0 years (range: 43–75 years)
n = 8
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 63.0 years (range: 43–75 years)
Sex: M+F
Population Size: 8
Sources:
Leukopenia grade 3-4, 2 patients
20 mg/m2 1 times / week multiple, intravenous
Highest studied dose
Dose: 20 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / week
Sources:
unhealthy, 63.0 years (range: 43–75 years)
n = 8
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 63.0 years (range: 43–75 years)
Sex: M+F
Population Size: 8
Sources:
Thrombocytopenia grade 3-4, 2 patients
20 mg/m2 1 times / week multiple, intravenous
Highest studied dose
Dose: 20 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / week
Sources:
unhealthy, 63.0 years (range: 43–75 years)
n = 8
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 63.0 years (range: 43–75 years)
Sex: M+F
Population Size: 8
Sources:
Neutropenia grade 3-4, 5 patients
20 mg/m2 1 times / week multiple, intravenous
Highest studied dose
Dose: 20 mg/m2, 1 times / week
Route: intravenous
Route: multiple
Dose: 20 mg/m2, 1 times / week
Sources:
unhealthy, 63.0 years (range: 43–75 years)
n = 8
Health Status: unhealthy
Condition: advanced solid tumors
Age Group: 63.0 years (range: 43–75 years)
Sex: M+F
Population Size: 8
Sources:
Arrhythmia severe
20 mg 3 times / week multiple, oral
Recommended|MTD
Dose: 20 mg, 3 times / week
Route: oral
Route: multiple
Dose: 20 mg, 3 times / week
Sources:
unhealthy
Diarrhea severe|grade 5, 25%
20 mg 3 times / week multiple, oral
Recommended|MTD
Dose: 20 mg, 3 times / week
Route: oral
Route: multiple
Dose: 20 mg, 3 times / week
Sources:
unhealthy
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no
no
no
no
no
no
no
no
no
no
unlikely
unlikely
unlikely
weak
weak
weak
yes [IC50 2 uM]
yes (co-administration study)
Comment: The coadministration of a single 60 mg dextromethorphan (DM) dose with FARYDAK (20 mg once per day, on Days 3, 5, and 8) increased the Cmax and AUC0-¥ of DM by 20% to 200% (interquartile range)and 20% to 130% (interquartile range), respectively
Page: 28.0
yes
yes
yes
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: In an in vivo evaluation, coadministration of a single 20 mg FARYDAK dose with the strong CYP3A4 inhibitor ketoconazole (200 mg twice daily for 14 days) increased the Cmax and AUC0-48 of PAN by 67% and 73% respectively
Page: 27.0
no
no
yes [Km >100 uM]
yes
yes
yes
yes
yes
yes
yes
yes
Tox targets
PubMed

PubMed

TitleDatePubMed
Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.
2008 Jan 15
A systematic assessment of radiation dose enhancement by 5-Aza-2'-deoxycytidine and histone deacetylase inhibitors in head-and-neck squamous cell carcinoma.
2009 Mar 1
SIRT1 activation enhances HDAC inhibition-mediated upregulation of GADD45G by repressing the binding of NF-κB/STAT3 complex to its promoter in malignant lymphoid cells.
2013 May 16
A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors.
2015 Sep
Patents

Sample Use Guides

20 mg, taken orally once every other day for 3 doses per week (on Days 1, 3, 5, 8, 10, and 12) of Weeks 1 and 2 of each 21-day cycle for 8 cycles
Route of Administration: Oral
Besides, Panobinostat inhibits growth of non small cell lung cancer cell lines (such as human H1299, L55 and A549 with IC50 of 5 nM, 11 nM and 30 nM, respectively), mesothelioma (such as human OK-6 and Ok-5 with IC50 of 5 nM and 7 nM, respectively) and small cell lung cancer cell lines (such as human RG-1 and LD-T with IC50 of 4 nM and 5 nM, respectively).
Substance Class Chemical
Created
by admin
on Fri Dec 15 18:02:01 GMT 2023
Edited
by admin
on Fri Dec 15 18:02:01 GMT 2023
Record UNII
9647FM7Y3Z
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PANOBINOSTAT
DASH   INN   MART.   MI   USAN   WHO-DD  
INN   USAN  
Official Name English
PANOBINOSTAT [MART.]
Common Name English
2-PROPENAMIDE, N-HYDROXY-3-(4-(((2-(2-METHYL-1H-INDOL-3-YL)ETHYL)AMINO)METHYL)PHENYL)-, (2E)-
Systematic Name English
PANOBINOSTAT [USAN]
Common Name English
(2E)-N-Hydroxy-3-[4-({[2-(2-methyl-1H-indol-3-yl)ethyl]amino}methyl)phenyl]prop-2-enamide
Systematic Name English
Panobinostat [WHO-DD]
Common Name English
PANOBINOSTAT [MI]
Common Name English
panobinostat [INN]
Common Name English
Classification Tree Code System Code
NDF-RT N0000175588
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
FDA ORPHAN DRUG 291509
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
FDA ORPHAN DRUG 244407
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
WHO-VATC QL01XX42
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
FDA ORPHAN DRUG 705919
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
FDA ORPHAN DRUG 376212
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
WHO-ATC L01XX42
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
EU-Orphan Drug EU/3/09/721
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
NCI_THESAURUS C1946
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
Code System Code Type Description
MESH
C496932
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
EPA CompTox
DTXSID40193506
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
DRUG BANK
DB06603
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
CAS
404950-80-7
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
ChEMBL
CHEMBL483254
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
WIKIPEDIA
PANOBINOSTAT
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
USAN
YY-135
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
CHEBI
85990
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
NDF-RT
N0000182137
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY Cytochrome P450 2D6 Inhibitors [MoA]
DRUG CENTRAL
4682
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
PUBCHEM
6918837
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
DAILYMED
9647FM7Y3Z
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
EVMPD
SUB31049
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
MERCK INDEX
m8383
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY Merck Index
SMS_ID
100000115952
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
NCI_THESAURUS
C66948
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
FDA UNII
9647FM7Y3Z
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
INN
8805
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
IUPHAR
7489
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY
RXCUI
1603350
Created by admin on Fri Dec 15 18:02:01 GMT 2023 , Edited by admin on Fri Dec 15 18:02:01 GMT 2023
PRIMARY RxNorm
Related Record Type Details
TARGET->WEAK INHIBITOR
IC50
METABOLIC ENZYME -> INHIBITOR
TRANSPORTER -> INHIBITOR
SALT/SOLVATE -> PARENT
TARGET -> INHIBITOR
IC50
EXCRETED UNCHANGED
URINE
METABOLIC ENZYME -> SUBSTRATE
IN VITRO
TARGET -> INHIBITOR
IC50
TRANSPORTER -> INHIBITOR
TARGET -> INHIBITOR
IC50
METABOLIC ENZYME -> SUBSTRATE
MINOR
TARGET -> INHIBITOR
IC50
METABOLIC ENZYME -> SUBSTRATE
IN VITRO
TRANSPORTER -> INHIBITOR
TARGET -> INHIBITOR
IC50
METABOLIC ENZYME -> SUBSTRATE
IN VITRO
TRANSPORTER -> SUBSTRATE
TARGET->WEAK INHIBITOR
IC50
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
IN VITRO
TARGET->WEAK INHIBITOR
IC50
BINDER->LIGAND
Panobinostat is approximately 90% bound to human plasma proteins in vitro and is independent of concentration.
BINDING
METABOLIC ENZYME -> SUBSTRATE
MINOR
METABOLIC ENZYME -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
IN VITRO
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
IN VITRO
TARGET -> INHIBITOR
A PAN HDAC INHIBITOR.
IC50
METABOLIC ENZYME -> INHIBITOR
TIME-DEPENDENT INHIBITION
TARGET -> INHIBITOR
IC50
SOLVATE->ANHYDROUS
EXCRETED UNCHANGED
FECAL
TARGET -> INHIBITOR
IC50
METABOLIC ENZYME -> SUBSTRATE
The fraction metabolized through CYP3A accounts for approximately 40% of the total hepatic panobinostat elimination.
Related Record Type Details
METABOLITE -> PARENT
FECAL; PLASMA; URINE
METABOLITE -> PARENT
FECAL; PLASMA; URINE
METABOLITE -> PARENT
FECAL
METABOLITE INACTIVE -> PARENT
FECAL; PLASMA; URINE
METABOLITE -> PARENT
FECAL; PLASMA; URINE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
ORAL BIOAVAILABILITY PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC Elimination
PHARMACOKINETIC
Tmax PHARMACOKINETIC IN PATIENTS WITH ADVANCED CANCER

ORAL ADMINISTRATION