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

Details

Stereochemistry ABSOLUTE
Molecular Formula C25H31NO6
Molecular Weight 441.5167
Optical Activity UNSPECIFIED
Defined Stereocenters 8 / 8
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of Deflazacort

SMILES

CC(=O)OCC(=O)[C@@]12N=C(C)O[C@@H]1C[C@H]3[C@@H]4CCC5=CC(=O)C=C[C@]5(C)[C@H]4[C@@H](O)C[C@]23C

InChI

InChIKey=FBHSPRKOSMHSIF-GRMWVWQJSA-N
InChI=1S/C25H31NO6/c1-13-26-25(20(30)12-31-14(2)27)21(32-13)10-18-17-6-5-15-9-16(28)7-8-23(15,3)22(17)19(29)11-24(18,25)4/h7-9,17-19,21-22,29H,5-6,10-12H2,1-4H3/t17-,18-,19-,21+,22+,23-,24-,25+/m0/s1

HIDE SMILES / InChI
Molecular Formula C25H31NO6
Molecular Weight 441.5167
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 8 / 8
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including, http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2763756/

Deflazacort is a glucocorticoid developed for the treatment of different inflammatory and immune conditions. The drug is rapidly metabolized to an active metabolite, 21-hydroxy-deflazaxort that may cross the blood brain barrier. Deflazacort acts by suppressing inflammatory response.

CNS Activity

CNS Penetrant
2588
Sources: www.ncbi.nlm.nih.gov/pubmed/10229911
Curator's Comment: Deflazacort active metabolite, 21-hydroxy-deflazacort crosses the blood-brain barrier in very low concentrations.

Approval Year

2017
411
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
CALCORT

Approved Use

Treat inflammation including asthma, arthritis and allergies; treat problems with skin, kidney, heart, digestive system, eyes or blood, treat problems where body has growths (tumours), suppress the immune system in transplant operations.
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
206 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
0.9 mg/kg single, oral
dose: 0.9 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
21-DESACETYLDEFLAZACORT plasma
Homo sapiens
population: UNHEALTHY
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
381 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
0.9 mg/kg single, oral
dose: 0.9 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
21-DESACETYLDEFLAZACORT plasma
Homo sapiens
population: UNHEALTHY
age: ADOLESCENT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
400 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
0.9 mg/kg single, oral
dose: 0.9 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
21-DESACETYLDEFLAZACORT plasma
Homo sapiens
population: UNHEALTHY
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
655 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
0.9 mg/kg single, oral
dose: 0.9 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
21-DESACETYLDEFLAZACORT plasma
Homo sapiens
population: UNHEALTHY
age: ADOLESCENT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
2 h
OTHER GOV'T
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208684,208685Orig1s000ClinPharmR.pdf#page=15
36 mg single, oral
dose: 36 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
21-DESACETYLDEFLAZACORT plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
60%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
0.9 mg/kg single, oral
dose: 0.9 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
21-DESACETYLDEFLAZACORT plasma
Homo sapiens
population: UNHEALTHY
age: ADOLESCENT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
1.2 mg/kg 1 times / day multiple, oral
Higher than recommended
Dose: 1.2 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 1.2 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Other AEs: Cushingoid, Erythema...
Other AEs:
Cushingoid (69%)
Erythema (49%)
Hirsutism (37%)
Headache (34%)
Weight increased (32%)
Constipation (15%)
Abdominal pain upper (14%)
Skin striae (11%)
Acne (11%)
Abdominal discomfort (8%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Other AEs: Cushingoid, Weight increased...
Other AEs:
Cushingoid (33%)
Weight increased (20%)
Increased appetite (14%)
Upper respiratory tract infection (12%)
Cough (12%)
Pollakiuria (12%)
Nasopharyngitis (10%)
Hirsutism (10%)
Central obesity (10%)
Erythema (8%)
Irritability (8%)
Rhinorrhea (8%)
Abdominal discomfort (6%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Other AEs: Cushingoid, Hirsutism...
Other AEs:
Cushingoid (60%)
Hirsutism (35%)
Weight increased (28%)
Erythema (28%)
Central obesity (25%)
Abdominal pain (18%)
Pollakiuria (15%)
Constipation (10%)
Irritability (10%)
Abnormal behavior (9%)
Pyrexia (9%)
Back pain (7%)
Rash (7%)
Contusion (6%)
Nausea (6%)
Psychomotor hyperactivity (6%)
Epistaxis (6%)
Skin striae (6%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Acne 11%
1.2 mg/kg 1 times / day multiple, oral
Higher than recommended
Dose: 1.2 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 1.2 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Skin striae 11%
1.2 mg/kg 1 times / day multiple, oral
Higher than recommended
Dose: 1.2 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 1.2 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Abdominal pain upper 14%
1.2 mg/kg 1 times / day multiple, oral
Higher than recommended
Dose: 1.2 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 1.2 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Constipation 15%
1.2 mg/kg 1 times / day multiple, oral
Higher than recommended
Dose: 1.2 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 1.2 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Weight increased 32%
1.2 mg/kg 1 times / day multiple, oral
Higher than recommended
Dose: 1.2 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 1.2 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Headache 34%
1.2 mg/kg 1 times / day multiple, oral
Higher than recommended
Dose: 1.2 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 1.2 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Hirsutism 37%
1.2 mg/kg 1 times / day multiple, oral
Higher than recommended
Dose: 1.2 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 1.2 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Erythema 49%
1.2 mg/kg 1 times / day multiple, oral
Higher than recommended
Dose: 1.2 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 1.2 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Cushingoid 69%
1.2 mg/kg 1 times / day multiple, oral
Higher than recommended
Dose: 1.2 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 1.2 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Abdominal discomfort 8%
1.2 mg/kg 1 times / day multiple, oral
Higher than recommended
Dose: 1.2 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 1.2 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Central obesity 10%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Hirsutism 10%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Nasopharyngitis 10%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Cough 12%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Pollakiuria 12%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Upper respiratory tract infection 12%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Increased appetite 14%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Weight increased 20%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Cushingoid 33%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Abdominal discomfort 6%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Erythema 8%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Irritability 8%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Rhinorrhea 8%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Constipation 10%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Irritability 10%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Pollakiuria 15%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Abdominal pain 18%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Central obesity 25%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Erythema 28%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Weight increased 28%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Hirsutism 35%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Contusion 6%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Epistaxis 6%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Nausea 6%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Psychomotor hyperactivity 6%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Skin striae 6%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Cushingoid 60%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Back pain 7%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Rash 7%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Abnormal behavior 9%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Pyrexia 9%
0.9 mg/kg 1 times / day multiple, oral
Recommended
Dose: 0.9 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 0.9 mg/kg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
unhealthy, 5 - 15 years
Health Status: unhealthy
Age Group: 5 - 15 years
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208684s000,208685s000lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946

inhibitor
2252

inducer
1087
inhibitor
2438
inhibitor
2507
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
2153

CYP2C19
2057

UGT1A1
246

UGT1A4
98

UGT1A6
136

UGT1A9
148

UGT2B7
197

CYP2B6
926

CYP2C8
1057

UGT1A3
89

UGT2B15
84

P-gp
1741

BCRP
910

OATP1B1
1079

OATP1B3
961

OAT1
725

OAT3
747

OCT2
779
esterase
74

P-gp
2052

BCRP
697

OATP1B1
503

OATP1B3
435
CYP1A2
832

CYP2B6
669
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BCRP
985
 no
21-DESACETYLDEFLAZACORT
2
CYP1A2
2333
 no
21-DESACETYLDEFLAZACORT
2
CYP1A2
2333
 no
21-DESACETYLDEFLAZACORT
2
CYP2B6
1160
 no
21-DESACETYLDEFLAZACORT
2
CYP2C19
2141
 no
21-DESACETYLDEFLAZACORT
2
CYP2C9
2497
 no
21-DESACETYLDEFLAZACORT
2
CYP3A4
2633
 no
21-DESACETYLDEFLAZACORT
2
OAT1
730
 no
21-DESACETYLDEFLAZACORT
2
OAT3
749
 no
21-DESACETYLDEFLAZACORT
2
OATP1B1
1095
 no
21-DESACETYLDEFLAZACORT
2
OATP1B3
970
 no
21-DESACETYLDEFLAZACORT
2
OCT2
782
 no
21-DESACETYLDEFLAZACORT
2
P-gp
1932
 no
21-DESACETYLDEFLAZACORT
2
UGT1A1
303
 no
21-DESACETYLDEFLAZACORT
2
UGT1A4
100
 no
21-DESACETYLDEFLAZACORT
2
UGT1A6
171
 no
21-DESACETYLDEFLAZACORT
2
UGT1A9
155
 no
21-DESACETYLDEFLAZACORT
2
UGT2B7
210
 no
21-DESACETYLDEFLAZACORT
2
CYP2B6
1160
 weak
21-DESACETYLDEFLAZACORT
2
CYP2C8
1117
 weak
21-DESACETYLDEFLAZACORT
2
CYP2D6
2546
 weak
21-DESACETYLDEFLAZACORT
2
CYP3A4
2633
 weak
21-DESACETYLDEFLAZACORT
2
UGT1A3
99
 weak
21-DESACETYLDEFLAZACORT
2
UGT2B15
84
 weak
21-DESACETYLDEFLAZACORT
2
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BCRP
697
 no
21-DESACETYLDEFLAZACORT
2
OATP1B1
503
 no
21-DESACETYLDEFLAZACORT
2
OATP1B3
435
 no
21-DESACETYLDEFLAZACORT
2
P-gp
2052
 yes
21-DESACETYLDEFLAZACORT
2
esterase
74
 yes
CYP3A4
1946
 yes
21-DESACETYLDEFLAZACORT
2
yes (co-administration study)
Comment: In a dedicated drug-drug interaction (DDI) study with multiple doses of clarithromycin, a strong CYP3A4 inhibitor, a 2 to 3 fold increase in Cmax, and AUCinf values of 21-des-DFZ was observed.
Page: 3.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
2263
21-DESACETYLDEFLAZACORT
2
PubMed

PubMed

TitleDatePubMed
Transactivation via the human glucocorticoid and mineralocorticoid receptor by therapeutically used steroids in CV-1 cells: a comparison of their glucocorticoid and mineralocorticoid properties.
2004-09
Effectiveness of nifedipine and deflazacort in the management of distal ureter stones.
2000-10-01
Prednisone versus deflazacort in the treatment of autoimmune thrombocytopenic purpura: evaluation of clinical response and immunological modifications.
1991-07-01
Patents

Patents

JP2005519852A
45

Sample Use Guides

In Vivo Use Guide
The usual dose for most conditions, including rheumatoid arthritis is half to three tablets each day, the dose for severe asthma may be up to 8 or 12 tablets each day.
Route of Administration: Oral
In Vitro Use Guide
Phytohaemagglutinin stimulated peripheral blood lymphocytes, NK and K cells were incubated with different concentrations of the drug (0, 1.2, 6.0, 24, 60, 240, and 600 x 10(-7) M) and the immunosuppressive effect was measured. Deflazacort suppressed the cells in a dose dependent way.
Substance Class Chemical
Created
by admin
on Mon Mar 31 17:56:44 GMT 2025
Edited
by admin
on Mon Mar 31 17:56:44 GMT 2025
Record UNII
KR5YZ6AE4B
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
EMFLAZA
Preferred Name English
Deflazacort
INN   MART.   MI   USAN   USP-RS   WHO-DD  
USAN   INN  
Official Name English
2-((6aR,6bS,8aS,8bS,11aR,12aS,12bS)-7-hydroxy-6a,8a-dimethyl-10-methylene-4-oxo-1,2,4,6a,6b,7,8,8a,9,10,11a,12,12a,12b-tetradecahydro-8bH-naphtho[2',1':4,5]indeno[1,2-d]oxazol-8b-yl)-2-oxoethyl acetate
Systematic Name English
Deflazacort [USP-RS]
Common Name English
11 ?, 21-dihydroxy-2'-methyl-5' ?-H-pregna-1,4-dieno[17,16d]oxazole-3,20-dione-21-acetate
Common Name English
Deflazacort [MI]
Common Name English
2-[(1S,2S,4R,8S,9S,11S,12S,13R)-11-hydroxy-6,9,13-trimethyl-16-oxo-5-oxa-7-azapentacyclo[10.8.0.0{2,9}.0{4,8}.0{13,18}]icosa-6,14,17-trien-8-yl]-2-oxoethyl acetate
Systematic Name English
Deflazacort [WHO-DD]
Common Name English
DL-458IT
Code English
Azacortinol
Common Name English
MDL-458
Code English
Deflazacort [USAN]
Common Name English
Deflazacort [ORANGE BOOK]
Common Name English
MDL458
Code English
L-5458
Code English
Deflazacort [INN]
Common Name English
5?H-Pregna-1,4-dieno[17,16-d]oxazole-3,20-dione, 21-(acetyloxy)-11-hydroxy-2?-methyl-, (11?,16?)-
Common Name English
Deflazacort [MART.]
Common Name English
(11?,16?)-21-(Acetyloxy)-11-hydroxy-2?-methyl-5?H-pregna-1,4-dieno[17,16-d]oxazole-3,20-dione
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C521
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
FDA ORPHAN DRUG 491715
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
FDA ORPHAN DRUG 315110
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
WHO-VATC QH02AB13
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
FDA ORPHAN DRUG 403413
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
WHO-ATC H02AB13
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
NDF-RT N0000175576
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
Code System Code Type Description
LACTMED
Deflazacort
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
MERCK INDEX
m4135
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY Merck Index
EPA CompTox
DTXSID9020378
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
RS_ITEM_NUM
1166116
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
ECHA (EC/EINECS)
238-483-7
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
DAILYMED
KR5YZ6AE4B
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
DRUG BANK
DB11921
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
WIKIPEDIA
Deflazacort
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
FDA UNII
KR5YZ6AE4B
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
ChEMBL
CHEMBL1201891
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
INN
4323
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
CAS
14484-47-0
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
RXCUI
22396
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY RxNorm
NCI_THESAURUS
C87230
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
DRUG CENTRAL
793
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
PUBCHEM
189821
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
SMS_ID
100000092093
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
USAN
X-95
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
EVMPD
SUB06943MIG
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
MESH
C021988
Created by admin on Mon Mar 31 17:56:44 GMT 2025 , Edited by admin on Mon Mar 31 17:56:44 GMT 2025
PRIMARY
Related Record Type Details
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> SUBSTRATE
GLUCOCORTICOID RECEPTOR
TARGET -> INHIBITOR
CYTOCHROME P450 3A4
METABOLIC ENZYME -> INHIBITOR
- Co-administration of deflazacort with clarithromycin, a strong CYP3A4 inhibitor, increased total exposure to 21-desDFZ by about 3-fold. - Co-administration of deflazacort with rifampin, a strong CYP3A4 inducer, significantly decreased the exposure of 21-desDFZ.
Related Record Type Details
Structure of 21-Desacetyldeflazacort
METABOLITE ACTIVE -> PRODRUG
Structure of 6BETA-HYDROXY-21-DESACETYL DEFLAZACORT
METABOLITE INACTIVE -> PARENT
Related Record Type Details
Structure of 21-Desacetyldeflazacort
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

Biological Half-life PHARMACOKINETIC
NIH
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