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Details

Stereochemistry ACHIRAL
Molecular Formula C21H16F4N4O2S
Molecular Weight 464.436
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ENZALUTAMIDE

SMILES

CNC(=O)C1=CC=C(C=C1F)N2C(=S)N(C(=O)C2(C)C)C3=CC(=C(C=C3)C#N)C(F)(F)F

InChI

InChIKey=WXCXUHSOUPDCQV-UHFFFAOYSA-N
InChI=1S/C21H16F4N4O2S/c1-20(2)18(31)28(12-5-4-11(10-26)15(8-12)21(23,24)25)19(32)29(20)13-6-7-14(16(22)9-13)17(30)27-3/h4-9H,1-3H3,(H,27,30)

HIDE SMILES / InChI
Molecular Formula C21H16F4N4O2S
Molecular Weight 464.436
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Enzalutamide (brand name Xtandi) is an orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. It was developed at UCLA and marketed by the pharmaceutical company Medivation for the treatment of metastatic castration-resistant prostate cancer. Through a mechanism that is reported to be different from other approved AR antagonists, enzalutamide inhibits the activity of prostate cancer cell ARs, which may result in a reduction in prostate cancer cell proliferation and, correspondingly, a reduction in the serum prostate specific antigen (PSA) level. AR over-expression in prostate cancer represents a key mechanism associated with prostate cancer hormone resistance.

CNS Activity

CNS Active
3913
Curator's Comment: Enzalutamide crosses the blood–brain barrier and apparently leads to sensitization to seizures in small numbers of patients. The ability to cross the blood–brain barrier may be a therapeutic advantage in patients with advanced epidural or meningeal disease but calls for caution.

Originator

University of California-Los Angeles
2
Curator's Comment: Medivation Inc., a San Francisco biotech company that sells a high-priced prostate cancer medication discovered by UCLA.

Approval Year

2012
595
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 21.4 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
XTANDI

Approved Use

Indicated for the treatment of patients with metastatic castration-resistant prostate cancer (CRPC).

Launch Date

1.34637119E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
3.4 μg/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/25917876
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ENZALUTAMIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: FED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
340 μg × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/25917876
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ENZALUTAMIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: FED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
6 day
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/25917876
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ENZALUTAMIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: FED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1.94%
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/25917876
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ENZALUTAMIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: FED
Doses

Doses

DosePopulationAdverse events​
300 mg 2 times / day multiple, oral
Highest studied dose
Dose: 300 mg, 2 times / day
Route: oral
Route: multiple
Dose: 300 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
unhealthy, 68 years (range: 44–93 years )
n = 3
Health Status: unhealthy
Condition: castration-resistant prostate cancer
Age Group: 68 years (range: 44–93 years )
Sex: M
Population Size: 3
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
DLT: Rash...
Dose limiting toxicities:
Rash (33%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
300 mg 2 times / day multiple, oral
Highest studied dose
Dose: 300 mg, 2 times / day
Route: oral
Route: multiple
Dose: 300 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
unhealthy, 68 years (range: 44–93 years )
n = 3
Health Status: unhealthy
Condition: castration-resistant prostate cancer
Age Group: 68 years (range: 44–93 years )
Sex: M
Population Size: 3
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
DLT: Seizure...
Dose limiting toxicities:
Seizure (33%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
300 mg 2 times / day multiple, oral
Highest studied dose
Dose: 300 mg, 2 times / day
Route: oral
Route: multiple
Dose: 300 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
unhealthy, 68 years (range: 44–93 years )
n = 3
Health Status: unhealthy
Condition: castration-resistant prostate cancer
Age Group: 68 years (range: 44–93 years )
Sex: M
Population Size: 3
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
Other AEs: Convulsions...
Other AEs:
Convulsions (grade 3-4, 33%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
240 mg 1 times / day multiple, oral
MTD
Dose: 240 mg, 1 times / day
Route: oral
Route: multiple
Dose: 240 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
unhealthy, 68 years (range: 44–93 years )
n = 29
Health Status: unhealthy
Condition: castration-resistant prostate cancer
Age Group: 68 years (range: 44–93 years )
Sex: M
Population Size: 29
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Disc. AE: Fatigue...
Other AEs: Fatigue...
AEs leading to
discontinuation/dose reduction:
Fatigue (3%)
Other AEs:
Fatigue (grade 3-4, 17%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
240 mg 2 times / day multiple, oral
Dose: 240 mg, 2 times / day
Route: oral
Route: multiple
Dose: 240 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
unhealthy, 68 years (range: 44–93 years )
n = 22
Health Status: unhealthy
Condition: castration-resistant prostate cancer
Age Group: 68 years (range: 44–93 years )
Sex: M
Population Size: 22
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
DLT: Seizure...
Dose limiting toxicities:
Seizure (5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
360 mg 1 times / day multiple, oral
Dose: 360 mg, 1 times / day
Route: oral
Route: multiple
Dose: 360 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
unhealthy, 68 years (range: 44–93 years )
n = 28
Health Status: unhealthy
Condition: castration-resistant prostate cancer
Age Group: 68 years (range: 44–93 years )
Sex: M
Population Size: 28
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
DLT: Seizure...
Dose limiting toxicities:
Seizure (4%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Disc. AE: Seizure, Infection...
Other AEs: Asthenia, Asthenia...
AEs leading to
discontinuation/dose reduction:
Seizure (0.9%)
Infection (grade 5, 1%)
Sepsis (grade 5, 1%)
Other AEs:
Asthenia (grade 1-4, 50.6%)
Asthenia (grade 3-4, 9%)
Fatigue (grade 1-4, 50.6%)
Fatigue (grade 3-4, 9%)
Peripheral edema (grade 1-4, 15.4%)
Peripheral edema (grade 3-4, 1%)
Back pain (grade 1-4, 26.4%)
Back pain (grade 3-4, 5.3%)
Arthralgia (grade 1-4, 20.5%)
Arthralgia (grade 3-4, 2.5%)
Musculoskeletal pain (grade 1-4, 15%)
Musculoskeletal pain (grade 3-4, 1.3%)
Muscular weakness (grade 1-4, 9.8%)
Muscular weakness (grade 3-4, 1.5%)
Musculoskeletal stiffness (grade 1-4, 2.6%)
Musculoskeletal stiffness (grade 3-4, 0.3%)
Diarrhea (grade 1-4, 21.8%)
Diarrhea (grade 3-4, 1.1%)
Hot flush (grade 1-4, 20.3%)
Hypertension (grade 1-4, 6.4%)
Hypertension (grade 3-4, 2.1%)
Headache (grade 1-4, 12.1%)
Headache (grade 3-4, 0.9%)
Dizziness (grade 1-4, 9.5%)
Dizziness (grade 3-4, 0.5%)
Vertigo (grade 1-4, 9.5%)
Vertigo (grade 3-4, 0.5%)
Cauda equina syndrome (grade 1-4, 7.4%)
Cauda equina syndrome (grade 3-4, 6.6%)
Paresthesia (grade 1-4, 6.6%)
Amnesia (grade 1-4, 4.3%)
Memory impairment (grade 1-4, 4.3%)
Cognitive disorder (grade 1-4, 4.3%)
Disturbance in attention (grade 1-4, 4.3%)
Amnesia (grade 3-4, 0.3%)
Memory impairment (grade 3-4, 0.3%)
Cognitive disorder (grade 3-4, 0.3%)
Disturbance in attention (grade 3-4, 0.3%)
Hypoesthesia (grade 1-4, 4%)
Hypoesthesia (grade 3-4, 0.3%)
Nasopharyngitis (grade 1-4, 10.9%)
Upper respiratory tract infection (grade 1-4, 10.9%)
Sinusitis (grade 1-4, 10.9%)
Rhinitis (grade 1-4, 10.9%)
Pharyngitis (grade 1-4, 10.9%)
Laryngitis (grade 1-4, 10.9%)
Pneumonia (grade 1-4, 8.5%)
Lower respiratory tract infection (grade 1-4, 8.5%)
Bronchitis (grade 1-4, 8.5%)
Lung infection (grade 1-4, 8.5%)
Pneumonia (grade 3-4, 2.4%)
Lower respiratory tract infection (grade 3-4, 2.4%)
Bronchitis (grade 3-4, 2.4%)
Lung infection (grade 3-4, 2.4%)
Insomnia (grade 1-4, 8.8%)
Anxiety (grade 1-4, 6.5%)
Anxiety (grade 3-4, 0.3%)
Hematuria (grade 1-4, 6.9%)
Hematuria (grade 3-4, 1.8%)
Pollakiuria (grade 1-4, 4.8%)
Fall (grade 1-4, 4.6%)
Fall (grade 3-4, 0.3%)
Pruritus (grade 1-4, 3.8%)
Dry skin (grade 1-4, 3.5%)
Epistaxis (grade 1-4, 3.3%)
Epistaxis (grade 3-4, 0.1%)
Neutropenia (grade 1-4, 15%)
Bilirubin increased (grade 1-4, 3%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Page: p. 79
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Page: p. 79
Disc. AE: Thrombocytopenia, Colonic obstruction...
AEs leading to
discontinuation/dose reduction:
Thrombocytopenia (0.2%)
Colonic obstruction (0.2%)
Diarrhea (0.2%)
Fatigue (0.6%)
Rash (0.2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Page: p. 79
AEs

AEs

AESignificanceDosePopulation
Rash 33%
DLT, Disc. AE
300 mg 2 times / day multiple, oral
Highest studied dose
Dose: 300 mg, 2 times / day
Route: oral
Route: multiple
Dose: 300 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
unhealthy, 68 years (range: 44–93 years )
n = 3
Health Status: unhealthy
Condition: castration-resistant prostate cancer
Age Group: 68 years (range: 44–93 years )
Sex: M
Population Size: 3
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Seizure 33%
DLT, Disc. AE
300 mg 2 times / day multiple, oral
Highest studied dose
Dose: 300 mg, 2 times / day
Route: oral
Route: multiple
Dose: 300 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
unhealthy, 68 years (range: 44–93 years )
n = 3
Health Status: unhealthy
Condition: castration-resistant prostate cancer
Age Group: 68 years (range: 44–93 years )
Sex: M
Population Size: 3
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Convulsions grade 3-4, 33%
300 mg 2 times / day multiple, oral
Highest studied dose
Dose: 300 mg, 2 times / day
Route: oral
Route: multiple
Dose: 300 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
unhealthy, 68 years (range: 44–93 years )
n = 3
Health Status: unhealthy
Condition: castration-resistant prostate cancer
Age Group: 68 years (range: 44–93 years )
Sex: M
Population Size: 3
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
Fatigue 3%
Disc. AE
240 mg 1 times / day multiple, oral
MTD
Dose: 240 mg, 1 times / day
Route: oral
Route: multiple
Dose: 240 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
unhealthy, 68 years (range: 44–93 years )
n = 29
Health Status: unhealthy
Condition: castration-resistant prostate cancer
Age Group: 68 years (range: 44–93 years )
Sex: M
Population Size: 29
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Fatigue grade 3-4, 17%
240 mg 1 times / day multiple, oral
MTD
Dose: 240 mg, 1 times / day
Route: oral
Route: multiple
Dose: 240 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
unhealthy, 68 years (range: 44–93 years )
n = 29
Health Status: unhealthy
Condition: castration-resistant prostate cancer
Age Group: 68 years (range: 44–93 years )
Sex: M
Population Size: 29
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Seizure 5%
DLT, Disc. AE
240 mg 2 times / day multiple, oral
Dose: 240 mg, 2 times / day
Route: oral
Route: multiple
Dose: 240 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
unhealthy, 68 years (range: 44–93 years )
n = 22
Health Status: unhealthy
Condition: castration-resistant prostate cancer
Age Group: 68 years (range: 44–93 years )
Sex: M
Population Size: 22
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Seizure 4%
DLT, Disc. AE
360 mg 1 times / day multiple, oral
Dose: 360 mg, 1 times / day
Route: oral
Route: multiple
Dose: 360 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
unhealthy, 68 years (range: 44–93 years )
n = 28
Health Status: unhealthy
Condition: castration-resistant prostate cancer
Age Group: 68 years (range: 44–93 years )
Sex: M
Population Size: 28
Sources:
https://pubmed.ncbi.nlm.nih.gov/20398925
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Seizure 0.9%
Disc. AE
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Laryngitis grade 1-4, 10.9%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Nasopharyngitis grade 1-4, 10.9%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Pharyngitis grade 1-4, 10.9%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Rhinitis grade 1-4, 10.9%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Sinusitis grade 1-4, 10.9%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Upper respiratory tract infection grade 1-4, 10.9%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Headache grade 1-4, 12.1%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Musculoskeletal pain grade 1-4, 15%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Neutropenia grade 1-4, 15%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Peripheral edema grade 1-4, 15.4%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Musculoskeletal stiffness grade 1-4, 2.6%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Hot flush grade 1-4, 20.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Arthralgia grade 1-4, 20.5%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Diarrhea grade 1-4, 21.8%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Back pain grade 1-4, 26.4%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Bilirubin increased grade 1-4, 3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Epistaxis grade 1-4, 3.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Dry skin grade 1-4, 3.5%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Pruritus grade 1-4, 3.8%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Hypoesthesia grade 1-4, 4%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Amnesia grade 1-4, 4.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Cognitive disorder grade 1-4, 4.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Disturbance in attention grade 1-4, 4.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Memory impairment grade 1-4, 4.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Fall grade 1-4, 4.6%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Pollakiuria grade 1-4, 4.8%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Asthenia grade 1-4, 50.6%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Fatigue grade 1-4, 50.6%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Hypertension grade 1-4, 6.4%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Anxiety grade 1-4, 6.5%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Paresthesia grade 1-4, 6.6%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Hematuria grade 1-4, 6.9%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Cauda equina syndrome grade 1-4, 7.4%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Bronchitis grade 1-4, 8.5%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Lower respiratory tract infection grade 1-4, 8.5%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Lung infection grade 1-4, 8.5%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Pneumonia grade 1-4, 8.5%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Insomnia grade 1-4, 8.8%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Dizziness grade 1-4, 9.5%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Vertigo grade 1-4, 9.5%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Muscular weakness grade 1-4, 9.8%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Epistaxis grade 3-4, 0.1%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Amnesia grade 3-4, 0.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Anxiety grade 3-4, 0.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Cognitive disorder grade 3-4, 0.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Disturbance in attention grade 3-4, 0.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Fall grade 3-4, 0.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Hypoesthesia grade 3-4, 0.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Memory impairment grade 3-4, 0.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Musculoskeletal stiffness grade 3-4, 0.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Dizziness grade 3-4, 0.5%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Vertigo grade 3-4, 0.5%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Headache grade 3-4, 0.9%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Peripheral edema grade 3-4, 1%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Diarrhea grade 3-4, 1.1%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Musculoskeletal pain grade 3-4, 1.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Muscular weakness grade 3-4, 1.5%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Hematuria grade 3-4, 1.8%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Hypertension grade 3-4, 2.1%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Bronchitis grade 3-4, 2.4%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Lower respiratory tract infection grade 3-4, 2.4%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Lung infection grade 3-4, 2.4%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Pneumonia grade 3-4, 2.4%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Arthralgia grade 3-4, 2.5%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Back pain grade 3-4, 5.3%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Cauda equina syndrome grade 3-4, 6.6%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Asthenia grade 3-4, 9%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Fatigue grade 3-4, 9%
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Infection grade 5, 1%
Disc. AE
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Sepsis grade 5, 1%
Disc. AE
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203415lbl.pdf
Colonic obstruction 0.2%
Disc. AE
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Page: p. 79
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Page: p. 79
Diarrhea 0.2%
Disc. AE
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Page: p. 79
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Page: p. 79
Rash 0.2%
Disc. AE
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Page: p. 79
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Page: p. 79
Thrombocytopenia 0.2%
Disc. AE
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Page: p. 79
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Page: p. 79
Fatigue 0.6%
Disc. AE
160 mg 1 times / day steady, oral
Recommended
Dose: 160 mg, 1 times / day
Route: oral
Route: steady
Dose: 160 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Page: p. 79
unhealthy, 69 years (range: 41-92 years)
n = 800
Health Status: unhealthy
Condition: metastatic castration-resistant prostate cancer
Age Group: 69 years (range: 41-92 years)
Sex: M
Population Size: 800
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203415Orig1s000MedR.pdf
Page: p. 79
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737

inducer
781
inhibitor
1767

inducer
389

substrate
1037
inhibitor
1852

substrate
1217
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2B6
810

CYP2C8
911

CYP2C19
1478

CYP3A4/5
278

CYP1A2
1524

P-gp
1461
CYP2C8
693

P-gp
1537

CYP3A5
395

CYP1A1
349

CYP1A2
1054

CYP2A6
543

CYP2B6
664

CYP2C18
138

CYP2C19
991

CYP2E1
667
CYP2C19
293

CYP2C8
168
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP2C19
1553
 moderate
CYP2C9
1819
 moderate
CYP3A4
1925
 strong
yes (co-administration study)
Comment: Co-administration of a strong CYP3A4 inhibitor (itraconazole) increased the composite AUC of enzalutamide plus Ndesmethyl enzalutamide by 1.3 fold in healthy volunteers
Page: -
P-gp
1650
 yes [IC50 1.67 uM]
CYP2C8
965
 yes [IC50 10 uM]
no (co-administration study)
Comment: Among these enzymes, the IC50 of CYP2C8 was the lowest. However, enzalutamide at steady state did not cause a clinically relevant change in the AUC of pioglitazone (CYP2C8 substrate) in vivo.
Page: 4.0
CYP2C19
1553
 yes [IC50 23 uM]
CYP2B6
1001
 yes [IC50 42 uM]
CYP2C9
1819
 yes [IC50 50 uM]
CYP1A2
1692
 yes [IC50 56 uM]
CYP2D6
1891
 yes
CYP3A4/5
335
 yes
CYP2C8
965
 yes
yes (co-administration study)
Comment: Co-administration of a strong CYP2C8 inhibitor (gemfibrozil) increased the composite area under the plasmaconcentration-time curve (AUC) of enzalutamide plus N-desmethyl enzalutamide in healthy volunteers.
Page: -
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP1A1
349
 no
CYP1A2
1054
 no
CYP2A6
543
 no
CYP2B6
664
 no
CYP2C18
138
 no
CYP2C19
991
 no
CYP2C9
1037
 no
CYP2D6
1217
 no
CYP2E1
667
 no
P-gp
1537
 no
CYP2C8
693
 yes
N-desmethyl enzalutamide
1
CYP3A5
395
 yes
CYP2C8
693
 yes
yes (co-administration study)
Comment: In vivo, the sum of enzalutamide and M2 exposure was increased by 2.2-fold and 1.3-fold when it was co-administered with gemfibrozil (strong CYP2C8 inhibitor) or itraconazole (strong CYP3A4 inhibitor), respectively.
Page: 3.0
CYP3A4
1737
 yes
yes (co-administration study)
Comment: In vivo, the sum of enzalutamide and M2 exposure was increased by 2.2-fold and 1.3-fold when it was co-administered with gemfibrozil (strong CYP2C8 inhibitor) or itraconazole (strong CYP3A4 inhibitor), respectively.
Page: 3.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:68534
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:68534
ChemicalBook
CB62500946
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB62500946
MolPort
MolPort-009-679-470
https://www.molport.com/shop/molecule-link/MolPort-009-679-470
Selleck Chemicals
MDV3100
http://www.selleckchem.com/products/MDV3100.html
ZINC
ZINC000034806477
http://zinc15.docking.org/substances/ZINC000034806477
eMolecules
32176540
https://www.emolecules.com/cgi-bin/more?vid=32176540
PubMed

PubMed

TitleDatePubMed
Development of a second-generation antiandrogen for treatment of advanced prostate cancer.
2009 May 8
Enzalutamide in metastatic prostate cancer before chemotherapy.
2014 Jul 31
Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer.
2014 Jun 12
Molecular alterations and emerging targets in castration resistant prostate cancer.
2014 Mar
Targeting chromatin binding regulation of constitutively active AR variants to overcome prostate cancer resistance to endocrine-based therapies.
2015 Jul 13
LncRNA HOTAIR Enhances the Androgen-Receptor-Mediated Transcriptional Program and Drives Castration-Resistant Prostate Cancer.
2015 Oct 6
Patents

Patents

08524755
2
20070004753
2
20070254933
1
20080139634
1
20100172975
1

Sample Use Guides

In Vivo Use Guide
160 mg (four 40 mg capsules) administered orally once daily
Route of Administration: Oral
In Vitro Use Guide
Resistant cells were maintained in vitro under constant exposure to 10 μM of enzalutamide.
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:30:25 UTC 2023
Edited
by admin
on Fri Dec 15 16:30:25 UTC 2023
Record UNII
93T0T9GKNU
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ENZALUTAMIDE
DASH   INN   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
ENZALUTAMIDE [USAN]
Common Name English
4-(3-(4-CYANO-3-(TRIFLUOROMETHYL)PHENYL)-5,5-DIMETHYL-4-OXO-2-THIOXOIMIDAZOLIDIN-1-YL)-2-FLUORO-N-METHYLBENZAMIDE
Systematic Name English
Enzalutamide [WHO-DD]
Common Name English
ENZALUTAMIDE [JAN]
Common Name English
XTANDI
Brand Name English
MDV 3100
Common Name English
MDV-3100
Code English
enzalutamide [INN]
Common Name English
MDV3100
Code English
ENZALUTAMIDE [VANDF]
Common Name English
ENZALUTAMIDE [MI]
Common Name English
BENZAMIDE, 4-(3-(4-CYANO-3-(TRIFLUOROMETHYL)PHENYL)-5,5-DIMETHYL-4-OXO-2-THIOXO-1-IMIDAZOLIDINYL)-2-FLUORO-N-METHYL-
Systematic Name English
ENZALUTAMIDE [ORANGE BOOK]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C146993
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
NDF-RT N0000175560
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
LIVERTOX NBK548070
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
WHO-ATC L02BB04
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
Code System Code Type Description
IUPHAR
6812
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
PUBCHEM
15951529
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
WIKIPEDIA
Enzalutamide
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
EPA CompTox
DTXSID10912307
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
FDA UNII
93T0T9GKNU
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
SMS_ID
100000138095
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
DAILYMED
93T0T9GKNU
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
NDF-RT
N0000185507
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY Cytochrome P450 2C9 Inducers [MoA]
ChEMBL
CHEMBL1082407
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
DRUG BANK
DB08899
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
INN
9621
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
USAN
WW-149
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
DRUG CENTRAL
4628
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
CHEBI
68534
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
MESH
C540278
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
EVMPD
SUB77412
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
CAS
915087-33-1
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
RXCUI
1307298
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY RxNorm
NDF-RT
N0000185607
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY Cytochrome P450 2C19 Inducers [MoA]
NDF-RT
N0000185506
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY Cytochrome P450 3A4 Inducers [MoA]
NCI_THESAURUS
C71744
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
MERCK INDEX
m11683
Created by admin on Fri Dec 15 16:30:25 UTC 2023 , Edited by admin on Fri Dec 15 16:30:25 UTC 2023
PRIMARY
Related Record Type Details
CYTOCHROME P450 2C19
METABOLIC ENZYME -> INDUCER
Therefore, co-administration of enzalutamide with CYP3A4, 2C9, and 2C19 substrates with a narrow therapeutic index should be avoided.
MODERATE
ANDROGEN RECEPTOR F876L
TARGET -> INHIBITOR RESISTANT
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> INHIBITOR
CYTOCHROME P450 3A4
METABOLIC ENZYME -> INHIBITOR
Structure of DEUTENZALUTAMIDE
LABELED -> NON-LABELED
CYTOCHROME P450 3A5
METABOLIC ENZYME -> INHIBITOR
ANDROGEN RECEPTOR
TARGET -> AGONIST
BINDING
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
In vivo, the sum of enzalutamide and M2 exposure was increased by 2.2-fold and 1.3-fold when it was co-administered with gemfibrozil (strong CYP2C8 inhibitor) or itraconazole (strong CYP3A4 inhibitor), respectively.
CYTOCHROME P450 2C19
METABOLIC ENZYME -> INHIBITOR
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
CYTOCHROME P450 2B6
METABOLIC ENZYME -> INHIBITOR
CYTOCHROME P450 2D6
METABOLIC ENZYME -> INHIBITOR
CYTOCHROME P450 2C9
METABOLIC ENZYME -> INHIBITOR
CYTOCHROME P450 2C8
METABOLIC ENZYME -> SUBSTRATE
In vivo, the sum of enzalutamide and M2 exposure was increased by 2.2-fold and 1.3-fold when it was co-administered with gemfibrozil (strong CYP2C8 inhibitor) or itraconazole (strong CYP3A4 inhibitor), respectively. If the co-administration of enzalutamide with a strong CYP2C8 inhibitor cannot be avoided, the daily enzalutamide dose should be reduced to 80 mg.
CYTOCHROME P450 1A2
METABOLIC ENZYME -> INHIBITOR
TIME-DEPENDENT INHIBITION
ANDROGEN RECEPTOR F876L
TARGET -> AGONIST
ANDROGEN RECEPTOR
TARGET -> INHIBITOR
CYTOCHROME P450 2C9
METABOLIC ENZYME -> INDUCER
Therefore, co-administration of enzalutamide with CYP3A4, 2C9, and 2C19 substrates with a narrow therapeutic index should be avoided.
MODERATE
CYTOCHROME P450 3A4
METABOLIC ENZYME -> INDUCER
Therefore, co-administration of enzalutamide with CYP3A4, 2C9, and 2C19 substrates with a narrow therapeutic index should be avoided
STRONG
CYTOCHROME P450 2C8
METABOLIC ENZYME -> INHIBITOR
Related Record Type Details
Structure of 4-(3-(4-CYANO-3-(TRIFLUOROMETHYL)PHENYL)-5,5-DIMETHYL-2,4-DIOXO-1-IMIDAZOLIDINYL)-2-FLUOROBENZOIC ACID
METABOLITE -> PARENT
MINOR
URINE
Structure of ENZALUTAMIDE CARBOXYLIC ACID
METABOLITE INACTIVE -> PARENT
In plasma, M1 accounted for 10% of the 14C-radioactivity. In urine, the most abundant 14C-component was M1 (62.7% of dose). In feces, the most abundant 14C-components were M1 and M10, which accounted for 3.34% and 4.26% of the radioactive dose, respectively.
FECAL; PLASMA; URINE
Structure of 4-(3-(4-CARBAMOYL-3-(TRIFLUOROMETHYL)PHENYL)-5,5-DIMETHYL-4-OXO-2-THIOXO-IMIDAZOLIDIN-1-YL)-2-FLUORO-BENZOIC ACID
METABOLITE -> PARENT
In urine, M10 was a minor metabolite, which accounted for 0.67% of the dose. In feces, M10 was one of the most abundant 14C-components, and it accounted for 4.26% of the radioactive dose.
FECAL; URINE
Structure of 4-(3-(4-(AMINOCARBONYL)-3-(TRIFLUOROMETHYL)PHENYL)-5,5-DIMETHYL-4-OXO-2-THIOXO-1-IMIDAZOLIDINYL)-2-FLUORO-N-METHYLBENZAMIDE
METABOLITE -> PARENT
Metabolite M7 was trace component in plasma; accounting for ≤ 2% of the radioactivity in the 6- and 24-hour postdose plasma samples and not detected at any other time point. In urine, M7 accounted for 9.45% of the radioactive dose. In feces, M7 accounted for 1.12% of the radioactive dose.
FECAL; PLASMA; URINE
Structure of BENZAMIDE, 4-(3-(4-CYANO-3-(TRIFLUOROMETHYL)PHENYL)-5,5-DIMETHYL-4-OXO-2-THIOXO-1-IMIDAZOLIDINYL)-2-FLUORO-N-(HYDROXYMETHYL)-
METABOLITE -> PARENT
Trace amount of M6 was observed in urine (≤ 0.42% of the dose) and plasma (≤ 2% of the radioactivity in the 6- and 24-hour postdose plasma samples and not detected at any other time point).
MINOR
PLASMA; URINE
Related Record Type Details
Structure of DEFLUORO ENZALUTAMIDE
IMPURITY -> PARENT
Structure of O-METHYL (4-CYANO-3-(TRIFLUOROMETHYL)PHENYL)CARBAMOTHIOATE
IMPURITY -> PARENT
Structure of 4-ISOTHIOCYANATO-2-(TRIFLUOROMETHYL)BENZONITRILE
IMPURITY -> PARENT
Related Record Type Details
Structure of ENZALUTAMIDE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC SINGLE ORAL DOSE

Tmax PHARMACOKINETIC DOSE

ORAL ADMINISTRATION

Volume of Distribution PHARMACOKINETIC
NIH
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