Details
Stereochemistry | ACHIRAL |
Molecular Formula | C15H14N2O4S |
Molecular Weight | 318.348 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
ONC(=O)\C=C\C1=CC(=CC=C1)S(=O)(=O)NC2=CC=CC=C2
InChI
InChIKey=NCNRHFGMJRPRSK-MDZDMXLPSA-N
InChI=1S/C15H14N2O4S/c18-15(16-19)10-9-12-5-4-8-14(11-12)22(20,21)17-13-6-2-1-3-7-13/h1-11,17,19H,(H,16,18)/b10-9+
Molecular Formula | C15H14N2O4S |
Molecular Weight | 318.348 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/?term=16928830; http://www.ncbi.nlm.nih.gov/pubmed/?term=24800886; http://www.ncbi.nlm.nih.gov/pubmed/?term=23382909
Curator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/?term=16928830; http://www.ncbi.nlm.nih.gov/pubmed/?term=24800886; http://www.ncbi.nlm.nih.gov/pubmed/?term=23382909
Belinostat is a hydroxamate-type histone deacetylase inhibitor indicated for the treatment of relapsed or refractory peripheal T-cell lymphoma. The compound received orphan drug designation for the treatment of malignant thymomas. Acting on a histone deacetylase Belinostat causes the accumulation of acetylated histones and other proteins, inducing cell cycle arrest and/or apoptosis of some transformed cells. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apoptosis, promoting cellular differentiation, and inhibiting angiogenesis. This agent may sensitize drug-resistant tumor cells to other antineoplastic agents, possibly through a mechanism involving the down-regulation of thymidylate synthase. PXD101 has been shown in preclinical studies to have the potential to treat a wide range of solid and hematologic malignancies either as a monotherapy or in combination with other active agents, and both an oral and intravenous formulation of the drug are being evaluated in clinical trials.
CNS Activity
Sources: http://www.ncbi.nlm.nih.gov/pubmed/17960383
Curator's Comment: Limited penetration demonstrated on non-human primates
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: O15379 Gene ID: 8841.0 Gene Symbol: HDAC3 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=18789133 |
41.0 nM [EC50] | ||
Target ID: Q13547 Gene ID: 3065.0 Gene Symbol: HDAC1 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=18789133 |
30.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | BELEODAQ Approved UseIndicated for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma (PTCL). This indication is approved under accelerated approval based on tumor response rate and duration of response. Launch Date2014 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
681 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/20706839 |
1000 mg/m² 1 times / day multiple, oral dose: 1000 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: |
BELINOSTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1.68 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
BELINOSTAT ACID plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
21.9 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
BELINOSTAT plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
1.26 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
BELINOSTAT AMIDE plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
2.1 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
METHYL BELINOSTAT plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
2.56 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
3-(PHENYLSULFAMOYL)BENZOIC ACID plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
80.8 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
BELINOSTAT GLUCURONIDE plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
8.7 μM × h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/20706839 |
1000 mg/m² 1 times / day multiple, oral dose: 1000 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: |
BELINOSTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
361 ug*min/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
BELINOSTAT ACID plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
719 ug*min/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
BELINOSTAT plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
647 ug*min/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
BELINOSTAT AMIDE plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
354 ug*min/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
METHYL BELINOSTAT plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
1009 ug*min/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
3-(PHENYLSULFAMOYL)BENZOIC ACID plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
15.1 mg*min/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
BELINOSTAT GLUCURONIDE plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.5 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/20706839 |
1000 mg/m² 1 times / day multiple, oral dose: 1000 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: |
BELINOSTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
131 min Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
BELINOSTAT ACID plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
118 min Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
BELINOSTAT plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
305 min Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
BELINOSTAT AMIDE plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
79.6 min Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
METHYL BELINOSTAT plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
264 min Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
3-(PHENYLSULFAMOYL)BENZOIC ACID plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
|
280 min Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01273155 |
400 mg/m^2 single, intravenous dose: 400 mg/m^2 route of administration: intravenous experiment type: single co-administered: |
BELINOSTAT GLUCURONIDE plasma | Homo sapiens population: unhealthy age: adults sex: food status: |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5.65% |
BELINOSTAT plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
1200 mg/m2 1 times / day steady, intravenous Highest studied dose Dose: 1200 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1200 mg/m2, 1 times / day Sources: |
unhealthy, 58.5 years (range: 25-74 years) n = 5 Health Status: unhealthy Condition: advanced malignancy refractory Age Group: 58.5 years (range: 25-74 years) Sex: M+F Population Size: 5 Sources: |
DLT: Atrial fibrillation, Diarrhea... Other AEs: Nausea, Vomiting... Dose limiting toxicities: Atrial fibrillation (1 patient) Other AEs:Diarrhea (1 patient) Fatigue (grade 3, 2 patients) Nausea (grade 2, 1 patient) Sources: Vomiting (grade 2, 1 patient) Lethargy (grade 3, 1 patient) Diarrhea (grade 3, 1 patient) |
1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 58.5 years (range: 25-74 years) n = 18 Health Status: unhealthy Condition: advanced malignancy refractory Age Group: 58.5 years (range: 25-74 years) Sex: M+F Population Size: 18 Sources: |
DLT: Atrial fibrillation, Vomiting... Dose limiting toxicities: Atrial fibrillation (1 patient) Sources: Vomiting (1 patient) Nausea (1 patient) |
600 mg/m2 1 times / day steady, intravenous Dose: 600 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 600 mg/m2, 1 times / day Sources: |
unhealthy, 58.5 years (range: 25-74 years) n = 6 Health Status: unhealthy Condition: advanced malignancy refractory Age Group: 58.5 years (range: 25-74 years) Sex: M+F Population Size: 6 Sources: |
DLT: Fatigue... |
1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Disc. AE: Fatigue, Anemia... Other AEs: Nausea, Nausea... AEs leading to discontinuation/dose reduction: Fatigue (grade 3-4, 5%) Other AEs:Anemia (grade 3-4, 11%) Febrile neutropenia Nausea (grade 1-2, 41%) Sources: Nausea (grade 3-4, 1%) Fatigue (grade 1-2, 32%) Pyrexia (grade 1-2, 33%) Pyrexia (grade 3-4, 2%) Anemia (grade 1-2, 21%) Vomiting (grade 1-2, 28%) Vomiting (grade 3-4, 1%) Constipation (grade 1-2, 22%) Constipation (grade 3-4, 1%) Diarrhea (grade 1-2, 21%) Diarrhea (grade 3-4, 2%) Dyspnea (grade 1-2, 16%) Dyspnea (grade 3-4, 6%) Rash (grade 1-2, 19%) Rash (grade 3-4, 1%) Peripheral edema (grade 1-2, 20%) Cough (grade 1-2, 19%) Thrombocytopenia (grade 1-2, 9%) Thrombocytopenia (grade 3-4, 7%) Pruritus (grade 1-2, 13%) Pruritus (grade 3-4, 3%) Chills (grade 1-2, 15%) Chills (grade 3-4, 1%) Blood lactate dehydrogenase increased (grade 1-2, 14%) Blood lactate dehydrogenase increased (grade 3-4, 2%) Decreased appetite (grade 1-2, 13%) Decreased appetite (grade 3-4, 2%) Headache (grade 1-2, 15%) Infusion site pain (grade 1-2, 14%) Hypokalemia (grade 1-2, 8%) Hypokalemia (grade 3-4, 4%) QT prolonged (grade 1-2, 7%) QT prolonged (grade 3-4, 4%) Abdominal pain (grade 1-2, 10%) Abdominal pain (grade 3-4, 1%) Hypotension (grade 1-2, 7%) Hypotension (grade 3-4, 3%) Phlebitis (grade 1-2, 9%) Phlebitis (grade 3-4, 1%) Dizziness (grade 1-2, 10%) Tumor lysis syndrome (grade 4, 1 patient) Pneumonia (serious|grade 5, > 2) Sepsis (serious|grade 5, > 2) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Atrial fibrillation | 1 patient DLT |
1200 mg/m2 1 times / day steady, intravenous Highest studied dose Dose: 1200 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1200 mg/m2, 1 times / day Sources: |
unhealthy, 58.5 years (range: 25-74 years) n = 5 Health Status: unhealthy Condition: advanced malignancy refractory Age Group: 58.5 years (range: 25-74 years) Sex: M+F Population Size: 5 Sources: |
Diarrhea | 1 patient DLT |
1200 mg/m2 1 times / day steady, intravenous Highest studied dose Dose: 1200 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1200 mg/m2, 1 times / day Sources: |
unhealthy, 58.5 years (range: 25-74 years) n = 5 Health Status: unhealthy Condition: advanced malignancy refractory Age Group: 58.5 years (range: 25-74 years) Sex: M+F Population Size: 5 Sources: |
Nausea | grade 2, 1 patient | 1200 mg/m2 1 times / day steady, intravenous Highest studied dose Dose: 1200 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1200 mg/m2, 1 times / day Sources: |
unhealthy, 58.5 years (range: 25-74 years) n = 5 Health Status: unhealthy Condition: advanced malignancy refractory Age Group: 58.5 years (range: 25-74 years) Sex: M+F Population Size: 5 Sources: |
Vomiting | grade 2, 1 patient | 1200 mg/m2 1 times / day steady, intravenous Highest studied dose Dose: 1200 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1200 mg/m2, 1 times / day Sources: |
unhealthy, 58.5 years (range: 25-74 years) n = 5 Health Status: unhealthy Condition: advanced malignancy refractory Age Group: 58.5 years (range: 25-74 years) Sex: M+F Population Size: 5 Sources: |
Diarrhea | grade 3, 1 patient | 1200 mg/m2 1 times / day steady, intravenous Highest studied dose Dose: 1200 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1200 mg/m2, 1 times / day Sources: |
unhealthy, 58.5 years (range: 25-74 years) n = 5 Health Status: unhealthy Condition: advanced malignancy refractory Age Group: 58.5 years (range: 25-74 years) Sex: M+F Population Size: 5 Sources: |
Lethargy | grade 3, 1 patient | 1200 mg/m2 1 times / day steady, intravenous Highest studied dose Dose: 1200 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1200 mg/m2, 1 times / day Sources: |
unhealthy, 58.5 years (range: 25-74 years) n = 5 Health Status: unhealthy Condition: advanced malignancy refractory Age Group: 58.5 years (range: 25-74 years) Sex: M+F Population Size: 5 Sources: |
Fatigue | grade 3, 2 patients DLT |
1200 mg/m2 1 times / day steady, intravenous Highest studied dose Dose: 1200 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1200 mg/m2, 1 times / day Sources: |
unhealthy, 58.5 years (range: 25-74 years) n = 5 Health Status: unhealthy Condition: advanced malignancy refractory Age Group: 58.5 years (range: 25-74 years) Sex: M+F Population Size: 5 Sources: |
Atrial fibrillation | 1 patient DLT |
1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 58.5 years (range: 25-74 years) n = 18 Health Status: unhealthy Condition: advanced malignancy refractory Age Group: 58.5 years (range: 25-74 years) Sex: M+F Population Size: 18 Sources: |
Nausea | 1 patient DLT |
1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 58.5 years (range: 25-74 years) n = 18 Health Status: unhealthy Condition: advanced malignancy refractory Age Group: 58.5 years (range: 25-74 years) Sex: M+F Population Size: 18 Sources: |
Vomiting | 1 patient DLT |
1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 58.5 years (range: 25-74 years) n = 18 Health Status: unhealthy Condition: advanced malignancy refractory Age Group: 58.5 years (range: 25-74 years) Sex: M+F Population Size: 18 Sources: |
Fatigue | grade 3 DLT |
600 mg/m2 1 times / day steady, intravenous Dose: 600 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 600 mg/m2, 1 times / day Sources: |
unhealthy, 58.5 years (range: 25-74 years) n = 6 Health Status: unhealthy Condition: advanced malignancy refractory Age Group: 58.5 years (range: 25-74 years) Sex: M+F Population Size: 6 Sources: |
Febrile neutropenia | Disc. AE | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Abdominal pain | grade 1-2, 10% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Dizziness | grade 1-2, 10% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Decreased appetite | grade 1-2, 13% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Pruritus | grade 1-2, 13% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Blood lactate dehydrogenase increased | grade 1-2, 14% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Infusion site pain | grade 1-2, 14% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Chills | grade 1-2, 15% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Headache | grade 1-2, 15% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Dyspnea | grade 1-2, 16% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Cough | grade 1-2, 19% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Rash | grade 1-2, 19% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Peripheral edema | grade 1-2, 20% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Anemia | grade 1-2, 21% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Diarrhea | grade 1-2, 21% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Constipation | grade 1-2, 22% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Vomiting | grade 1-2, 28% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Fatigue | grade 1-2, 32% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Pyrexia | grade 1-2, 33% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Nausea | grade 1-2, 41% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Hypotension | grade 1-2, 7% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
QT prolonged | grade 1-2, 7% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Hypokalemia | grade 1-2, 8% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Phlebitis | grade 1-2, 9% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Thrombocytopenia | grade 1-2, 9% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Abdominal pain | grade 3-4, 1% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Chills | grade 3-4, 1% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Constipation | grade 3-4, 1% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Nausea | grade 3-4, 1% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Phlebitis | grade 3-4, 1% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Rash | grade 3-4, 1% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Vomiting | grade 3-4, 1% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Anemia | grade 3-4, 11% Disc. AE |
1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Blood lactate dehydrogenase increased | grade 3-4, 2% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Decreased appetite | grade 3-4, 2% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Diarrhea | grade 3-4, 2% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Pyrexia | grade 3-4, 2% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Hypotension | grade 3-4, 3% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Pruritus | grade 3-4, 3% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Hypokalemia | grade 3-4, 4% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
QT prolonged | grade 3-4, 4% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Fatigue | grade 3-4, 5% Disc. AE |
1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Dyspnea | grade 3-4, 6% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Thrombocytopenia | grade 3-4, 7% | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Tumor lysis syndrome | grade 4, 1 patient | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Pneumonia | serious|grade 5, > 2 | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Sepsis | serious|grade 5, > 2 | 1000 mg/m2 1 times / day steady, intravenous Recommended|MTD Dose: 1000 mg/m2, 1 times / day Route: intravenous Route: steady Dose: 1000 mg/m2, 1 times / day Sources: |
unhealthy, 64.0 years (range: 29-81 years) n = 129 Health Status: unhealthy Condition: relapsed or refractory peripheral T-cell lymphoma Age Group: 64.0 years (range: 29-81 years) Sex: M+F Population Size: 129 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes | ||||
yes | ||||
yes | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206256Orig1s000ClinPharmR.pdf#page=24 Page: 24.0 |
yes | |||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206256Orig1s000PharmR.pdf#page=12 Page: 12.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101. | 2003 Aug |
|
Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies. | 2006 Aug |
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The histone deacetylase inhibitor belinostat (PXD101) suppresses bladder cancer cell growth in vitro and in vivo. | 2007 Oct 12 |
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Interactions between bortezomib and romidepsin and belinostat in chronic lymphocytic leukemia cells. | 2008 Jan 15 |
|
Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. | 2008 Jan 15 |
|
Integrative analysis of epigenetic modulation in melanoma cell response to decitabine: clinical implications. | 2009 |
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Combined inhibition of DNA methylation and histone acetylation enhances gene re-expression and drug sensitivity in vivo. | 2009 Mar 10 |
|
Gene expression-signature of belinostat in cell lines is specific for histone deacetylase inhibitor treatment, with a corresponding signature in xenografts. | 2009 Sep |
|
Chemical phylogenetics of histone deacetylases. | 2010 Mar |
|
Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors. | 2011 Jul 14 |
|
Histone acetylation-mediated regulation of the Hippo pathway. | 2013 |
|
Glucuronidation by UGT1A1 is the dominant pathway of the metabolic disposition of belinostat in liver cancer patients. | 2013 |
|
Epigenetic and molecular mechanisms underlying the antileukemic activity of the histone deacetylase inhibitor belinostat in human acute promyelocytic leukemia cells. | 2014 Sep |
|
A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. | 2015 Sep |
Sample Use Guides
Recommended dosage of Beleodaq is 1,000 mg/m^2 administered over 30 minutes by intravenous infusion once daily on days 1-5 of a 21-day cycle. Cycles can be repeated until disease progression or unacceptable toxicity. Treatment discontinuation or interruption with or without dosage reductions by 25% may be needed to manage adverse reactions.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=17935615
The in vitro treatment of carcinoma cell lines at 1–5 uM belinostat for 48 h caused a dose-dependent inhibition of proliferation, with the most potent inhibitory effect occurring on 5637 cells.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:35:41 GMT 2023
by
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on
Fri Dec 15 15:35:41 GMT 2023
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Record UNII |
F4H96P17NZ
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Record Status |
Validated (UNII)
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Classification Tree | Code System | Code | ||
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NDF-RT |
N0000175588
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WHO-ATC |
L01XX49
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FDA ORPHAN DRUG |
289309
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NCI_THESAURUS |
C1946
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EU-Orphan Drug |
EU/3/13/1151
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CHEMBL408513
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C48812
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DTXSID60194378
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m2295
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7496
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726630
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1543543
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61076
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8823
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100000144569
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866323-14-0
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6918638
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BELINOSTAT
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414864-00-9
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NON-SPECIFIC STEREOCHEMISTRY | |||
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SUB121262
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DB05015
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Related Record | Type | Details | ||
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TARGET->LIGAND | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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BINDER->LIGAND |
BINDING
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METABOLIC ENZYME -> SUBSTRATE |
Related Record | Type | Details | ||
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METABOLITE INACTIVE -> PARENT |
MEDIATOR: UGT1A1
MAJOR
PLASMA; URINE
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METABOLITE -> PARENT |
The enzymes responsible for the formation of 3-(anilinosulfonyl)-benzenecarboxylic acid, (3-ASBA) are not known.
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METABOLITE -> PARENT |
PLASMA; URINE
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METABOLITE -> PARENT |
Belinostat also undergoes hepatic metabolism by CYP2A6, CYP2C9, and CYP3A4 enzymes to form belinostat amide and belinostat acid.
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
Belinostat also undergoes hepatic metabolism by CYP2A6, CYP2C9, and CYP3A4 enzymes to form belinostat amide and belinostat acid.
MAJOR
PLASMA; URINE
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METABOLITE -> PARENT |
MAJOR
PLASMA; URINE
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METABOLITE INACTIVE -> PARENT |
Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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