Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C24H31NO |
| Molecular Weight | 349.5099 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 6 / 6 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@]12CC[C@@]([H])(CC2=CC[C@@]3([H])[C@]4([H])CC=C(c5cccnc5)[C@@]4(C)CC[C@@]31[H])O
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
| Molecular Formula | C24H31NO |
| Molecular Weight | 349.5099 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 6 / 6 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionCurator'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
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.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3522 |
110.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | ZYTIGA Approved UseIndicated in combination with prednisone for the treatment of patients with metastatic castration-resistant prostate cancer. Launch Date1.30394882E12 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
226 ng/mL |
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1173 ng × h/mL |
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Dose | Population | Adverse 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
Disc. AE: Cardiac failure, AST high... Other AEs: Lymphopenia, Lymphopenia... AEs leading to discontinuation/dose reduction: Cardiac failure (5 patients) Other AEs:AST high (1%) ALT high (1%) Lymphopenia (grade 1-2, 29.3%) Sources: 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) |
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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
Other AEs: Fatigue, Fatigue... Other AEs: Fatigue (grade 1-2, 39%) Sources: 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%) |
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: Page: p. 27 |
unhealthy Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Sex: M Sources: Page: p. 27 |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 542 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 542 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
| 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: |
unhealthy, 70 years n = 546 Health Status: unhealthy Condition: metastatic castrationresistant prostate cancer Age Group: 70 years Sex: M Population Size: 546 Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202379Orig1s000ClinPharmR.pdf#page=8 Page: 8.0 |
|||
| strong [Ki 0.32 uM] | ||||
| yes [IC50 10.8 uM] | ||||
| yes [Ki 0.12 uM] | ||||
| yes [Ki 0.39 uM] | ||||
| yes [Ki 0.44 uM] | ||||
| yes [Ki 11.4 uM] | ||||
| yes [Ki 17.6 uM] | ||||
| yes [Ki 29.8 uM] | ||||
| yes [Ki 31.8 uM] | ||||
| yes [Ki 46.3 uM] | ||||
| yes [Ki 8.01 uM] |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| major | ||||
| minor | ||||
| no | ||||
| no | ||||
| yes | ||||
| yes |
PubMed
| Title | Date | PubMed |
|---|---|---|
| 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 |
Sample Use Guides
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
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
Edited
Fri Jun 25 21:48:56 UTC 2021
by
admin
on
Fri Jun 25 21:48:56 UTC 2021
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| Record UNII |
G819A456D0
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| Record Status |
Validated (UNII)
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| Record Version |
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Common Name | English | ||
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Code | English | ||
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Systematic Name | English | ||
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Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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LIVERTOX |
4
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NDF-RT |
N0000182633
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WHO-VATC |
QL02BX03
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NCI_THESAURUS |
C147923
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WHO-ATC |
L02BX03
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| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
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DB05812
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PRIMARY | |||
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C089740
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PRIMARY | |||
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1100072
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PRIMARY | RxNorm | ||
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SUB07361MIG
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PRIMARY | |||
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7375
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PRIMARY | |||
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154229-19-3
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PRIMARY | |||
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6745
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PRIMARY | |||
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G819A456D0
Created by
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PRIMARY | |||
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CHEMBL254328
Created by
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PRIMARY | |||
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ABIRATERONE
Created by
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PRIMARY | |||
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M1279
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PRIMARY | Merck Index | ||
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N0000187062
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PRIMARY | Cytochrome P450 2C8 Inhibitors [MoA] | ||
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C77333
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PRIMARY | |||
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132971
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PRIMARY | |||
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N0000182632
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PRIMARY | Cytochrome P450 17A1 Inhibitors [MoA] | ||
|
N0000182137
Created by
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PRIMARY | Cytochrome P450 2D6 Inhibitors [MoA] |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
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.
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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.
|
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|
EXCRETED UNCHANGED |
FECAL
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|
METABOLIC ENZYME -> SUBSTRATE | |||
|
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.
|
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|
METABOLIC ENZYME -> SUBSTRATE | |||
|
TRANSPORTER -> INHIBITOR |
WEAK
|
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|
BINDER->LIGAND |
BINDING
|
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
METABOLITE INACTIVE -> PARENT |
The conversion is likely through esterase activity (the esterases have not been identified) and is not CYP mediated.
MAJOR
PLASMA
|
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|
|
PRODRUG -> METABOLITE ACTIVE | |||
|
METABOLITE INACTIVE -> PARENT |
MAJOR
PLASMA; URINE
|
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
ACTIVE MOIETY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Volume of Distribution | PHARMACOKINETIC |
|
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| Biological Half-life | PHARMACOKINETIC |
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| Tmax | PHARMACOKINETIC |
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