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

Details

Stereochemistry ACHIRAL
Molecular Formula C19H17F6N7O
Molecular Weight 473.375
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ENASIDENIB

SMILES

CC(C)(O)CNC1=NC(NC2=CC=NC(=C2)C(F)(F)F)=NC(=N1)C3=CC=CC(=N3)C(F)(F)F

InChI

InChIKey=DYLUUSLLRIQKOE-UHFFFAOYSA-N
InChI=1S/C19H17F6N7O/c1-17(2,33)9-27-15-30-14(11-4-3-5-12(29-11)18(20,21)22)31-16(32-15)28-10-6-7-26-13(8-10)19(23,24)25/h3-8,33H,9H2,1-2H3,(H2,26,27,28,30,31,32)

HIDE SMILES / InChI

Molecular Formula C19H17F6N7O
Molecular Weight 473.375
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including http://www.agios.com/patients-trials.php http://www.selleckchem.com/products/ag-221-enasidenib.html http://adisinsight.springer.com/drugs/800038591

Enasidenib, aslo known as AG-221 and CC-90007, is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2). The mutations of IDH2 present in certain cancer cells result in a new ability of the enzyme to catalyze the NAPH-dependent reduction of α-ketoglutarate to R(-)-2-hydroxyglutarate (2HG). The production of 2HG is believed to contribute to the formation and progression of cancer. The inhibition of mutant IDH2 and its neoactivity is therefore a potential therapeutic treatment for cancer. Enasidenib is an orally available, selective, potent inhibitor of the mutated IDH2 protein, making it a highly targeted investigational medicine for the potential treatment of patients with cancers that harbor an IDH2 mutation. Enasidenib has received orphan drug and fast track designations from the U.S. FDA. Enasidenib mesylate is in phase II clinical trials for Solid tumours and phase III clinical trials for the treatment of acute myeloid leukaemia.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
12.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
IDHIFA

Approved Use

IDHIFA is indicated for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) with an isocitrate dehydrogenase-2 (IDH2) mutation as detected by an FDA-approved test.

Launch Date

2017
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
822 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ENASIDENIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
13 μg/mL
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ENASIDENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
49500 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ENASIDENIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
25.5 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ENASIDENIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
137 h
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ENASIDENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1.5%
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ENASIDENIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
650 mg 1 times / day multiple, oral
Highest studied dose
Dose: 650 mg, 1 times / day
Route: oral
Route: multiple
Dose: 650 mg, 1 times / day
Sources:
unhealthy, adult
n = 5
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 5
Sources:
Other AEs: Abdominal distension, Diarrhea...
Other AEs:
Abdominal distension (1 patient)
Diarrhea (1 patient)
Fatigue (1 patient)
Hyperbilirubinemia (3 patients)
Rash (1 patient)
Sources:
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Disc. AE: Leukocytosis...
Other AEs: Nausea, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Leukocytosis (1%)
Other AEs:
Nausea (all grades, 50%)
Diarrhea (all grades, 43%)
Vomiting (all grades, 34%)
Decreased appetite (all grades, 34%)
Tumor lysis syndrome (all grades, 6%)
Differentiation syndrome (all grades, 14%)
Leukocytosis (all grades, 12%)
Dysgeusia (all grades, 12%)
Nausea (grade 3-4, 5%)
Diarrhea (grade 3-4, 8%)
Vomiting (grade 3-4, 2%)
Decreased appetite (grade 3-4, 4%)
Tumor lysis syndrome (grade 3-4, 6%)
Differentiation syndrome (grade 3-4, 7%)
Leukocytosis (grade 3-4, 6%)
Bilirubin total increased (all grades, 81%)
Calcium decreased (all grades, 74%)
Potassium decreased (all grades, 41%)
Blood phosphorus decreased (all grades, 27%)
Differentiation syndrome (4%)
Leukocytosis (3%)
Sources: Page: 5
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 6
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 6
Other AEs: Bilirubin total increased, Calcium decreased...
Other AEs:
Bilirubin total increased (grade 3-4, 15%)
Calcium decreased (grade 3-4, 8%)
Potassium decreased (grade 3-4, 15%)
Blood phosphorus decreased (grade 3-4, 8%)
Hyperbilirubinemia (3.7%)
Hyperbilirubinemia (1.4%)
Sources: Page: 6
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 45
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 45
Disc. AE: Death...
AEs leading to
discontinuation/dose reduction:
Death (grade 5, 4.2%)
Sources: Page: 45
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 45
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 45
Disc. AE: Death...
AEs leading to
discontinuation/dose reduction:
Death (grade 5, 11.7%)
Sources: Page: 45
AEs

AEs

AESignificanceDosePopulation
Abdominal distension 1 patient
650 mg 1 times / day multiple, oral
Highest studied dose
Dose: 650 mg, 1 times / day
Route: oral
Route: multiple
Dose: 650 mg, 1 times / day
Sources:
unhealthy, adult
n = 5
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 5
Sources:
Diarrhea 1 patient
650 mg 1 times / day multiple, oral
Highest studied dose
Dose: 650 mg, 1 times / day
Route: oral
Route: multiple
Dose: 650 mg, 1 times / day
Sources:
unhealthy, adult
n = 5
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 5
Sources:
Fatigue 1 patient
650 mg 1 times / day multiple, oral
Highest studied dose
Dose: 650 mg, 1 times / day
Route: oral
Route: multiple
Dose: 650 mg, 1 times / day
Sources:
unhealthy, adult
n = 5
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 5
Sources:
Rash 1 patient
650 mg 1 times / day multiple, oral
Highest studied dose
Dose: 650 mg, 1 times / day
Route: oral
Route: multiple
Dose: 650 mg, 1 times / day
Sources:
unhealthy, adult
n = 5
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 5
Sources:
Hyperbilirubinemia 3 patients
650 mg 1 times / day multiple, oral
Highest studied dose
Dose: 650 mg, 1 times / day
Route: oral
Route: multiple
Dose: 650 mg, 1 times / day
Sources:
unhealthy, adult
n = 5
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 5
Sources:
Leukocytosis 1%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Leukocytosis 3%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Differentiation syndrome 4%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Dysgeusia all grades, 12%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Leukocytosis all grades, 12%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Differentiation syndrome all grades, 14%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Blood phosphorus decreased all grades, 27%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Decreased appetite all grades, 34%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Vomiting all grades, 34%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Potassium decreased all grades, 41%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Diarrhea all grades, 43%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Nausea all grades, 50%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Tumor lysis syndrome all grades, 6%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Calcium decreased all grades, 74%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Bilirubin total increased all grades, 81%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Vomiting grade 3-4, 2%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Decreased appetite grade 3-4, 4%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Nausea grade 3-4, 5%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Leukocytosis grade 3-4, 6%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Tumor lysis syndrome grade 3-4, 6%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Differentiation syndrome grade 3-4, 7%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Diarrhea grade 3-4, 8%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 5
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 5
Hyperbilirubinemia 1.4%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 6
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 6
Hyperbilirubinemia 3.7%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 6
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 6
Bilirubin total increased grade 3-4, 15%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 6
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 6
Potassium decreased grade 3-4, 15%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 6
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 6
Blood phosphorus decreased grade 3-4, 8%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 6
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 6
Calcium decreased grade 3-4, 8%
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 6
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 6
Death grade 5, 4.2%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 45
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 45
Death grade 5, 11.7%
Disc. AE
100 mg 1 times / day multiple, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: 45
unhealthy, adult
n = 214
Health Status: unhealthy
Condition: myeloid leukemia
Age Group: adult
Sex: unknown
Population Size: 214
Sources: Page: 45
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
PubMed

PubMed

TitleDatePubMed
[Progress in molecularly targeted therapies for acute myeloid leukemia].
2015 Feb
IDH2 inhibition in AML: Finally progress?
2015 Jun-Sep
The Evolving Landscape in the Development of Isocitrate Dehydrogenase Mutant Inhibitors.
2016
Patents

Sample Use Guides

Continuous 28-day cycles of Enasidenib (AG 221) 100 mg orally (PO) once a day (QD) for 28 days, plus BSC.
Route of Administration: Oral
In Vitro Use Guide
Curator's Comment: Enasidenib has been demonstrated to reduce 2-HG levels by >90% and reverse histone and deoxyribonucleic acid (DNA) hypermethylation in vitro, and to induce differentiation in leukemia cell models
Unknown
Substance Class Chemical
Created
by admin
on Sat Dec 16 11:27:04 GMT 2023
Edited
by admin
on Sat Dec 16 11:27:04 GMT 2023
Record UNII
3T1SS4E7AG
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ENASIDENIB
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
ENASIDENIB [MI]
Common Name English
AG-221
Code English
2-METHYL-1-(4-(6-(TRIFLUOROMETHYL)PYRIDIN-2-YL)-6-(2-(TRIFLUOROMETHYL)PYRIDIN-4-YLAMINO)-1,3,5-TRIAZIN-2-YLAMINO)PROPAN-2-OL
Systematic Name English
ENASIDENIB [USAN]
Common Name English
Enasidenib [WHO-DD]
Common Name English
2-PROPANOL, 2-METHYL-1-((4-(6-(TRIFLUOROMETHYL)-2-PYRIDINYL)-6-((2-(TRIFLUOROMETHYL)-4-PYRIDINYL)AMINO)-1,3,5-TRIAZIN-2-YL)AMINO)-
Systematic Name English
enasidenib [INN]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 434514
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
NDF-RT N0000193615
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
NCI_THESAURUS C137826
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
WHO-ATC L01XX59
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
Code System Code Type Description
CAS
1446502-11-9
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
PUBCHEM
89683805
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
DRUG BANK
DB13874
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
NCI_THESAURUS
C111573
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
CHEBI
145374
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
USAN
DE-54
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
SMS_ID
100000175231
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
FDA UNII
3T1SS4E7AG
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
MERCK INDEX
m12047
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
CAS
1802003-09-3
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
NO STRUCTURE GIVEN
LACTMED
Enasidenib
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
INN
10162
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
WIKIPEDIA
Enasidenib
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
EPA CompTox
DTXSID801027942
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
RXCUI
1940332
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
DRUG CENTRAL
5251
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
DAILYMED
3T1SS4E7AG
Created by admin on Sat Dec 16 11:27:06 GMT 2023 , Edited by admin on Sat Dec 16 11:27:06 GMT 2023
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
EXCRETED UNCHANGED
URINE
METABOLIC ENZYME -> SUBSTRATE
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
CUMULATIVE EXCRETION
FECAL
EXCRETED UNCHANGED
FECAL
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
CUMULATIVE EXCRETION
URINE
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
TRANSPORTER -> NON-SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
TRANSPORTER -> NON-SUBSTRATE
Related Record Type Details
METABOLITE ACTIVE -> PARENT
METABOLITE ACTIVE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
PERMEABILITY CHEMICAL MEMBRANE TYPE

Tmax PHARMACOKINETIC