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

Details

Stereochemistry ABSOLUTE
Molecular Formula C24H31NO
Molecular Weight 349.509
Optical Activity UNSPECIFIED
Defined Stereocenters 6 / 6
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ABIRATERONE

SMILES

[H][C@@]12CC=C(C3=CC=CN=C3)[C@@]1(C)CC[C@@]4([H])[C@@]2([H])CC=C5C[C@@H](O)CC[C@]45C

InChI

InChIKey=GZOSMCIZMLWJML-VJLLXTKPSA-N
InChI=1S/C24H31NO/c1-23-11-9-18(26)14-17(23)5-6-19-21-8-7-20(16-4-3-13-25-15-16)24(21,2)12-10-22(19)23/h3-5,7,13,15,18-19,21-22,26H,6,8-12,14H2,1-2H3/t18-,19-,21-,22-,23-,24+/m0/s1

HIDE SMILES / InChI
Molecular Formula C24H31NO
Molecular Weight 349.509
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 6 / 6
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002321/WC500112860.pdf

Abiraterone acetate (trade name Zytiga) is a prodrug to the abiraterone, steroidal compound with antiandrogen activity and a 17 α-hydroxylase/C17,20-lyase (CYP17) inhibitor. It is indicated in combination with prednisone for the treatment of patients with metastatic castration-resistant prostate cancer. Abiraterone acetate is converted in vivo to abiraterone which inhibits CYP17, enzyme expressed in testicular, adrenal, and prostatic tumor tissues and required for androgen biosynthesis. Administration of this agent may suppress testosterone production by both the testes and the adrenals to castrate-range levels. Androgen sensitive prostatic carcinoma responds to treatment that decreases androgen levels. Androgen deprivation therapies, such as treatment with GnRH agonists or orchiectomy, decrease androgen production in the testes but do not affect androgen production by the adrenals or in the tumor.

CNS Activity

CNS Penetrant
2554
Curator's Comment: Abiraterone was able to cross the blood brain barrier since 14C-abiraterone had been measured in the cerebellum, cerebrum, medulla and spinal cord.

Originator

Approval Year

2011
587
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 110.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
ZYTIGA

Approved Use

Indicated in combination with prednisone for the treatment of patients with metastatic castration-resistant prostate cancer.

Launch Date

2011
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
226 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202379s005lbl.pdf
1000 mg 1 times / day steady-state, oral
dose: 1000 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
297 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
12.5 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
125 mg single, oral
dose: 125 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
50.2 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
60.6 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
85.7 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
71.9 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
64.5 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
2000 mg single, oral
dose: 2000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1173 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202379s005lbl.pdf
1000 mg 1 times / day steady-state, oral
dose: 1000 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1562 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
177 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
125 mg single, oral
dose: 125 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
315 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
315 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
330 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
365 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
461 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
2000 mg single, oral
dose: 2000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
18.6 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
18.2 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
125 mg single, oral
dose: 125 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
18.2 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
18.2 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
13.1 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
17.7 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
1000 mg single, oral
dose: 1000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
15.4 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24374856/
2000 mg single, oral
dose: 2000 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ABIRATERONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Disc. AE: Cardiac failure, AST high...
Other AEs: Lymphopenia, Lymphopenia...
AEs leading to
discontinuation/dose reduction:
Cardiac failure (5 patients)
AST high (1%)
ALT high (1%)
Other AEs:
Lymphopenia (grade 1-2, 29.3%)
Lymphopenia (grade 3-4, 8.7%)
Hyperglycemia (grade 1-2, 50.5%)
Hyperglycemia (grade 3-4, 6.5%)
ALT high (grade 1-2, 35.9%)
ALT high (grade 3-4, 6.1%)
AST high (grade 1-2, 33.9%)
AST high (grade 3-4, 3.1%)
Hypernatremia (grade 1-2, 32.6%)
Hypernatremia (grade 3-4, 0.4%)
Hypokalemia (grade 1-2, 14.2%)
Hypokalemia (grade 3-4, 2.8%)
Cardiac failure (grade 3-4, 1.6%)
Cardiac failure (grade 5, 2 patients)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Other AEs: Fatigue, Fatigue...
Other AEs:
Fatigue (grade 1-2, 39%)
Fatigue (grade 3-4, 2.2%)
Edema peripheral (grade 1-2, 25%)
Pitting edema (grade 1-2, 25%)
Generalized edema (grade 1-2, 25%)
Pyrexia (grade 1-2, 8.7%)
Pyrexia (grade 3-4, 0.6%)
Arthritis (grade 1-2, 30%)
Arthralgia (grade 1-2, 30%)
Joint swelling (grade 1-2, 30%)
Joint stiffness (grade 1-2, 30%)
Groin pain (grade 1-2, 6.6%)
Constipation (grade 1-2, 23%)
Diarrhea (grade 1-2, 22%)
Dyspepsia (grade 1-2, 11%)
Hot flush (grade 1-2, 22%)
Hot flush (grade 3-4, 0.2%)
Hypertension (grade 1-2, 22%)
Hypertension (grade 3-4, 3.9%)
Cough (grade 1-2, 17%)
Dyspnea (grade 1-2, 12%)
Dyspnea (grade 3-4, 2.4%)
Insomnia (grade 1-2, 14%)
Insomnia (grade 3-4, 0.2%)
Contusion (grade 1-2, 13%)
Fall (grade 1-2, 5.9%)
Upper respiratory tract infection (grade 1-2, 13%)
Nasopharyngitis (grade 1-2, 8%)
Hematuria (grade 1-2, 10%)
Hematuria (grade 3-4, 1.3%)
Rash (grade 1-2, 8.1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
2000 mg 1 times / day multiple, oral
Highest studied dose
Dose: 2000 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2000 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202379Orig1s000MedR.pdf
Page: p. 27
unhealthy
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Sex: M
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202379Orig1s000MedR.pdf
Page: p. 27
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202379Orig1s000MedR.pdf
Page: p. 27
AEs

AEs

AESignificanceDosePopulation
ALT high 1%
Disc. AE
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
AST high 1%
Disc. AE
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Cardiac failure 5 patients
Disc. AE
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Hypokalemia grade 1-2, 14.2%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Lymphopenia grade 1-2, 29.3%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Hypernatremia grade 1-2, 32.6%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
AST high grade 1-2, 33.9%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
ALT high grade 1-2, 35.9%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Hyperglycemia grade 1-2, 50.5%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Hypernatremia grade 3-4, 0.4%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Cardiac failure grade 3-4, 1.6%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Hypokalemia grade 3-4, 2.8%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
AST high grade 3-4, 3.1%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
ALT high grade 3-4, 6.1%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Hyperglycemia grade 3-4, 6.5%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Lymphopenia grade 3-4, 8.7%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Cardiac failure grade 5, 2 patients
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 542
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 542
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Hematuria grade 1-2, 10%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Dyspepsia grade 1-2, 11%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Dyspnea grade 1-2, 12%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Contusion grade 1-2, 13%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Upper respiratory tract infection grade 1-2, 13%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Insomnia grade 1-2, 14%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Cough grade 1-2, 17%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Diarrhea grade 1-2, 22%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Hot flush grade 1-2, 22%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Hypertension grade 1-2, 22%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Constipation grade 1-2, 23%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Edema peripheral grade 1-2, 25%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Generalized edema grade 1-2, 25%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Pitting edema grade 1-2, 25%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Arthralgia grade 1-2, 30%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Arthritis grade 1-2, 30%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Joint stiffness grade 1-2, 30%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Joint swelling grade 1-2, 30%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Fatigue grade 1-2, 39%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Fall grade 1-2, 5.9%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Groin pain grade 1-2, 6.6%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Nasopharyngitis grade 1-2, 8%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Rash grade 1-2, 8.1%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Pyrexia grade 1-2, 8.7%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Hot flush grade 3-4, 0.2%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Insomnia grade 3-4, 0.2%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Pyrexia grade 3-4, 0.6%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Hematuria grade 3-4, 1.3%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Fatigue grade 3-4, 2.2%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Dyspnea grade 3-4, 2.4%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Hypertension grade 3-4, 3.9%
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Co-administed with::
Corticosteroid
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
unhealthy, 70 years
n = 546
Health Status: unhealthy
Condition: metastatic castrationresistant prostate cancer
Age Group: 70 years
Sex: M
Population Size: 546
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737
inhibitor
1767
inhibitor
1852

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2E1
882

CYP2C19
1478

CYP3A4/5
278

CYP2A6
707

P-gp
1461
SULT2A1
24

P-gp
1537

UGT1A4
347

UGT1A3
422
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP2A6
739
 no
CYP2A6
739
 no
ABIRATERONE
2
CYP2E1
970
 no
ABIRATERONE
2
P-gp
1650
 no
CYP2D6
1891
 strong [Ki 0.16 uM]
yes (co-administration study)
Comment: The systemic exposure of dextromethorphan (CYP2D6 substrate) as assessed by the ratios of the geometric mean for Cmax and AUC, were approximately 2.8- and 2.9-fold higher, respectively, when dextromethorphan was co-administered with abiraterone acetate
Page: 8.0
CYP1A2
1692
 strong [Ki 0.32 uM]
P-gp
1650
 yes [IC50 10.8 uM]
ABIRATERONE
2
CYP2C19
1553
 yes [Ki 0.12 uM]
CYP2D6
1891
 yes [Ki 0.39 uM]
ABIRATERONE
2
CYP1A2
1692
 yes [Ki 0.44 uM]
ABIRATERONE
2
CYP3A4/5
335
 yes [Ki 11.4 uM]
CYP2C9
1819
 yes [Ki 17.6 uM]
CYP2C9
1819
 yes [Ki 29.8 uM]
ABIRATERONE
2
CYP2E1
970
 yes [Ki 31.8 uM]
CYP2C19
1553
 yes [Ki 46.3 uM]
ABIRATERONE
2
CYP3A4/5
335
 yes [Ki 8.01 uM]
ABIRATERONE
2
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
UGT1A4
347
 major
UGT1A3
422
 minor
P-gp
1537
 no
P-gp
1537
 no
ABIRATERONE
2
CYP3A4
1737
 yes
SULT2A1
24
 yes
PubMed

PubMed

TitleDatePubMed
Efficacy of abiraterone acetate in post-docetaxel castration-resistant prostate cancer.
2010 Jul
Abiraterone acetate.
2011 Aug 1
[Abiraterone acetate: a novel therapeutic option in hormone-refractory prostate cancer].
2012 Feb
Open-label, phase I, pharmacokinetic studies of abiraterone acetate in healthy men.
2012 Jun
Differential response to abiraterone acetate and di-n-butyl phthalate in an androgen-sensitive human fetal testis xenograft bioassay.
2014 Mar
Patents

Patents

US2016052958
2
US2016068846
2
US2016083416
2
US5604213
2

Sample Use Guides

In Vivo Use Guide
1,000 mg (four 250 mg tablets) administered orally once daily in combination with prednisone 5 mg administered orally twice daily. Zytiga must be taken on an empty stomach. No food should be consumed for at least two hours before the dose of Zytiga is taken and for at least one hour after the dose of Zytiga is taken. For patients with baseline moderate hepatic impairment (Child-Pugh Class B), reduce the Zytiga starting dose to 250 mg once daily. For patients who develop hepatotoxicity during treatment, hold Zytiga until recovery. Retreatment may be initiated at a reduced dose. Zytiga should be discontinued if patients develop severe hepatotoxicity.
Route of Administration: Oral
In Vitro Use Guide
Abiraterone acetate (CB 7630) inhibits CYP17 with an IC50 of 110 nM in human testicular microsomes. In Caco-2 cell monolayers abiraterone acetate had a low apparent permeability and was not substrate of P-glycoprotein (P-gp). Abiraterone acetate inhibited P-gp significantly at high concentrations with a 50 % inhibitory concentration (IC50) of 10.8 uM however as abiraterone acetate is rapidly converted to abiraterone, no systemic inhibition of P-gp is expected.
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:08:43 GMT 2023
Edited
by admin
on Fri Dec 15 16:08:43 GMT 2023
Record UNII
G819A456D0
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ABIRATERONE
INN   MI   VANDF   WHO-DD  
INN  
Official Name English
NSC-741232
Code English
17-(3-PYRIDYL)ANDROSTA-5,16-DIEN-3.BETA.-OL
Systematic Name English
17-(PYRIDIN-3-YL)ANDROSTA-5,16-DIEN-3.BETA.-OL
Systematic Name English
Abiraterone [WHO-DD]
Common Name English
CB 7598
Code English
ABIRATERONE [VANDF]
Common Name English
ABIRATERONE [USP IMPURITY]
Common Name English
ABIRATERONE [MI]
Common Name English
CB-7598
Code English
ANDROSTA-5,16-DIEN-3-OL, 17-(3-PYRIDINYL)-(3.BETA.)-
Systematic Name English
abiraterone [INN]
Common Name English
Classification Tree Code System Code
LIVERTOX NBK548136
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
NDF-RT N0000182633
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
WHO-VATC QL02BX03
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
NCI_THESAURUS C147923
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
WHO-ATC L02BX03
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
Code System Code Type Description
DRUG BANK
DB05812
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
SMS_ID
100000093287
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
MESH
C089740
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
RXCUI
1100072
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY RxNorm
EVMPD
SUB07361MIG
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
INN
7375
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
CAS
154229-19-3
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
IUPHAR
6745
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
EPA CompTox
DTXSID80879993
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
FDA UNII
G819A456D0
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
ChEMBL
CHEMBL254328
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
WIKIPEDIA
ABIRATERONE
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
MERCK INDEX
m1279
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY Merck Index
NSC
741232
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
DAILYMED
G819A456D0
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
NDF-RT
N0000187062
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY Cytochrome P450 2C8 Inhibitors [MoA]
NCI_THESAURUS
C77333
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
CHEBI
68642
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
PUBCHEM
132971
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY
NDF-RT
N0000182632
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY Cytochrome P450 17A1 Inhibitors [MoA]
NDF-RT
N0000182137
Created by admin on Fri Dec 15 16:08:43 GMT 2023 , Edited by admin on Fri Dec 15 16:08:43 GMT 2023
PRIMARY Cytochrome P450 2D6 Inhibitors [MoA]
Related Record Type Details
CYTOCHROME P450 2C8
METABOLIC ENZYME -> INHIBITOR
In vitro studies with human hepatic microsomes showed that abiraterone has the potential to inhibit CYP1A2, CYP2D6, CYP2C8 and to a lesser extent CYP2C9, CYP2C19 and CYP3A4/5.
CYTOCHROME P450 2D6
METABOLIC ENZYME -> INHIBITOR
Abiraterone is an inhibitor of CYP2D6, in vivo. In vitro studies with human hepatic microsomes showed that abiraterone has the potential to inhibit CYP1A2, CYP2D6, CYP2C8 and to a lesser extent CYP2C9, CYP2C19 and CYP3A4/5.
Structure of ABIRATERONE
EXCRETED UNCHANGED
FECAL
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
CYTOCHROME P450 1A2
METABOLIC ENZYME -> INHIBITOR
In vitro studies with human hepatic microsomes showed that abiraterone has the potential to inhibit CYP1A2, CYP2D6, CYP2C8 and to a lesser extent CYP2C9, CYP2C19 and CYP3A4/5.
URIDINE DIPHOSPHATE GLUCURONOSYLTRANSFERASE 1A4
METABOLIC ENZYME -> SUBSTRATE
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> INHIBITOR
WEAK
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Related Record Type Details
Structure of ABIRATERONE DECANOATE
PRODRUG -> METABOLITE ACTIVE
Structure of ABIRATERONE SULFATE
METABOLITE INACTIVE -> PARENT
The conversion is likely through esterase activity (the esterases have not been identified) and is not CYP mediated.
MAJOR
PLASMA
Structure of (3S,8R,9S,10R,13S,14S)-10,13-DIMETHYL-17-(1-OXIDOPYRIDIN-1-IUM-3-YL)-2,3,4,7,8,9,11,12,14,15-DECAHYDRO-1H-CYCLOPENTA(A)PHENANTHREN-3-OL
METABOLITE -> PARENT
Structure of ABIRATERONE ACETATE
PRODRUG -> METABOLITE ACTIVE
Structure of (3.BETA.)-17-(3-PYRIDINYL)ANDROSTA-5,16-DIENE-3,19-DIOL
METABOLITE -> PARENT
Structure of N-OXIDE ABIRATERONE SULFATE
METABOLITE INACTIVE -> PARENT
MAJOR
PLASMA; URINE
Related Record Type Details
Structure of ABIRATERONE ACETATE
PARENT -> IMPURITY
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Related Record Type Details
Structure of ABIRATERONE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC
NIH
NCATS
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