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Details

Stereochemistry ACHIRAL
Molecular Formula C21H16F4N4O2S
Molecular Weight 464.4378
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ENZALUTAMIDE

SMILES

CC1(C)C(=O)N(c2ccc(C#N)c(c2)C(F)(F)F)C(=S)N1c3ccc(c(c3)F)C(=NC)O

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
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
Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.
2011 Nov 10
Inhibitors of androgen receptor activation function-2 (AF2) site identified through virtual screening.
2011 Sep 22
Androgen receptor promotes ligand-independent prostate cancer progression through c-Myc upregulation.
2013
NF-κB2/p52 induces resistance to enzalutamide in prostate cancer: role of androgen receptor and its variants.
2013 Aug
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

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.
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
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 [WHO-DD]
Common Name English
ENZALUTAMIDE [ORANGE BOOK]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C146993
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
NDF-RT N0000175560
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
LIVERTOX 354
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
WHO-ATC L02BB04
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
Code System Code Type Description
IUPHAR
6812
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY
PUBCHEM
15951529
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY
FDA UNII
93T0T9GKNU
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY
NDF-RT
N0000185507
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY Cytochrome P450 2C9 Inducers [MoA]
ChEMBL
CHEMBL1082407
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY
DRUG BANK
DB08899
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY
INN
9621
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY
DRUG CENTRAL
4628
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY
MESH
C540278
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY
EVMPD
SUB77412
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY
CAS
915087-33-1
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY
RXCUI
1307298
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY RxNorm
NDF-RT
N0000185607
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY Cytochrome P450 2C19 Inducers [MoA]
NDF-RT
N0000185506
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY Cytochrome P450 3A4 Inducers [MoA]
NCI_THESAURUS
C71744
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY
MERCK INDEX
M11683
Created by admin on Fri Jun 25 20:32:43 UTC 2021 , Edited by admin on Fri Jun 25 20:32:43 UTC 2021
PRIMARY