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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

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

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

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

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
21.4 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
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
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
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
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%
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:
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:
DLT: Rash...
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:
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:
DLT: Seizure...
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:
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:
Other AEs: Convulsions...
Other AEs:
Convulsions (grade 3-4, 33%)
Sources:
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:
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:
Disc. AE: Fatigue...
Other AEs: Fatigue...
AEs leading to
discontinuation/dose reduction:
Fatigue (3%)
Other AEs:
Fatigue (grade 3-4, 17%)
Sources:
240 mg 2 times / day multiple, oral
Dose: 240 mg, 2 times / day
Route: oral
Route: multiple
Dose: 240 mg, 2 times / day
Sources:
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:
DLT: Seizure...
360 mg 1 times / day multiple, oral
Dose: 360 mg, 1 times / day
Route: oral
Route: multiple
Dose: 360 mg, 1 times / day
Sources:
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:
DLT: Seizure...
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:
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:
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:
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: 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: 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: 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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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: 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: 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: 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: 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: 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: 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: 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: 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: 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: Page: p. 79
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
moderate
moderate
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: -
yes [IC50 1.67 uM]
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
yes [IC50 23 uM]
yes [IC50 42 uM]
yes [IC50 50 uM]
yes [IC50 56 uM]
yes
yes
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
no
no
no
no
no
no
no
no
no
no
yes
yes
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
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
PubMed

PubMed

TitleDatePubMed
Inhibitors of androgen receptor activation function-2 (AF2) site identified through virtual screening.
2011 Sep 22
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

Sample Use Guides

160 mg (four 40 mg capsules) administered orally once daily
Route of Administration: Oral
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
METABOLIC ENZYME -> INDUCER
Therefore, co-administration of enzalutamide with CYP3A4, 2C9, and 2C19 substrates with a narrow therapeutic index should be avoided.
MODERATE
TARGET -> INHIBITOR RESISTANT
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> INHIBITOR
LABELED -> NON-LABELED
METABOLIC ENZYME -> INHIBITOR
TARGET -> AGONIST
BINDING
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.
METABOLIC ENZYME -> INHIBITOR
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> INHIBITOR
METABOLIC ENZYME -> INHIBITOR
METABOLIC ENZYME -> INHIBITOR
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.
METABOLIC ENZYME -> INHIBITOR
TIME-DEPENDENT INHIBITION
TARGET -> AGONIST
TARGET -> INHIBITOR
METABOLIC ENZYME -> INDUCER
Therefore, co-administration of enzalutamide with CYP3A4, 2C9, and 2C19 substrates with a narrow therapeutic index should be avoided.
MODERATE
METABOLIC ENZYME -> INDUCER
Therefore, co-administration of enzalutamide with CYP3A4, 2C9, and 2C19 substrates with a narrow therapeutic index should be avoided
STRONG
METABOLIC ENZYME -> INHIBITOR
Related Record Type Details
METABOLITE -> PARENT
MINOR
URINE
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
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
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
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
IMPURITY -> PARENT
IMPURITY -> PARENT
IMPURITY -> PARENT
Related Record Type Details
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