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Details

Stereochemistry RACEMIC
Molecular Formula C18H14F4N2O4S
Molecular Weight 430.373
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BICALUTAMIDE

SMILES

CC(O)(CS(=O)(=O)C1=CC=C(F)C=C1)C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F

InChI

InChIKey=LKJPYSCBVHEWIU-UHFFFAOYSA-N
InChI=1S/C18H14F4N2O4S/c1-17(26,10-29(27,28)14-6-3-12(19)4-7-14)16(25)24-13-5-2-11(9-23)15(8-13)18(20,21)22/h2-8,26H,10H2,1H3,(H,24,25)

HIDE SMILES / InChI
Bicalutamide (brand name Casodex) is an oral non-steroidal anti-androgen for prostate cancer. It is indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog for the treatment of Stage D2 metastatic carcinoma of the prostate. Bicalutamide competitively inhibits the action of androgens by binding to cytosol androgen receptors in the target tissue. Prostatic carcinoma is known to be androgen sensitive and responds to treatment that counteracts the effect of androgen and/or removes the source of androgen. When CASODEX is combined with luteinizing hormone releasing hormone (LHRH) analog therapy, the suppression of serum testosterone induced by the LHRH analog is not affected. Bicalutamide is well-absorbed following oral administration, although the absolute bioavailability is unknown. Bicalutamide undergoes stereospecific metabolism. The S (inactive) isomer is metabolized primarily by glucuronidation. The R (active) isomer also undergoes glucuronidation but is predominantly oxidized to an inactive metabolite followed by glucuronidation. Both the parent and metabolite glucuronides are eliminated in the urine and feces. The S-enantiomer is rapidly cleared relative to the R-enantiomer, with the R-enantiomer accounting for about 99% of total steady-state plasma levels.

CNS Activity

Curator's Comment: The peripheral selectivity of bicalutamide has been shown to be due to poor penetration across the blood-brain barrier: tissue distribution studies with [3H]bicalutamide show that although it is concentrated in the organs of metabolism and secretion as well as in the prostate, the pituitary glands, and the seminal vesicles, levels in the hypothalamus and the central nervous system (CNS) are much lower than in blood.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
CASODEX

Approved Use

Bicalutamide 50 mg daily is indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog for the treatment of Stage D2 metastatic carcinoma of the prostate. Bicalutamide 150 mg daily is not approved for use alone or with other treatments [see Clinical Studies (14.2)

Launch Date

1995
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
810.7 μg/L
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BICALUTAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
202.5 μg × h/mL
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BICALUTAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
5.8 day
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered: GONADORELIN
BICALUTAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
146.4 h
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BICALUTAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
4%
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered: GONADORELIN
BICALUTAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Other AEs: Gynaecomastia, Breast pain...
Other AEs:
Gynaecomastia (45.2%)
Breast pain (57.1%)
Hot flushes (16.7%)
Constipation (31%)
Dry skin (2.4%)
Insomnia (9.5%)
Rash (11.9%)
Back pain (14.3%)
Asthenia (19%)
Diarrhoea (19%)
Urinary tract infection (16.7%)
Arthralgia (11.9%)
Pharyngitis (14.3%)
Pain (23.8%)
Sources:
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Other AEs: Back pain, Constipation...
Other AEs:
Back pain (6.9%)
Constipation (10.3%)
Libido decreased (50%)
Impotence (57%)
Dyspepsia (6.9%)
Dysuria (6.9%)
Haematuria (6.9%)
Pain (17.2%)
Pelvic pain (6.9%)
Somnolence (6.9%)
Urinary incontinence (6.9%)
Urinary urgency (6.9%)
Weight gain (10.3%)
Gynaecomastia (79%)
Breast tenderness (79%)
Hot flushes (41%)
Sources:
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Other AEs: General body pain, Back pain...
Other AEs:
General body pain (35%)
Back pain (25%)
Asthenia (22%)
Pelvic pain (21%)
Infection (18%)
Abdominal pain (11%)
Chest pain (8%)
Headache (7%)
Flu syndrome (7%)
Hot flashes (53%)
Hypertension (8%)
Constipation (22%)
Nausea (15%)
Diarrhea (12%)
Liver function test increased (7%)
Dyspepsia (7%)
Flatulence (6%)
Anorexia (6%)
Vomiting (6%)
Anemia (11%)
Peripheral edema (13%)
Weight loss (7%)
Hyperglycemia (6%)
Alkaline phosphatase increased (5%)
Weight gain (5%)
Bone pain (9%)
Myasthenia (7%)
Arthritis (5%)
Fracture pathological (4%)
Dizziness (10%)
Paresthesia (8%)
Insomnia (7%)
Anxiety (5%)
Depression (4%)
Dyspnea (13%)
Cough increased (8%)
Pharyngitis (8%)
Bronchitis (6%)
Pneumonia (4%)
Rhinitis (4%)
Rash (9%)
Sweating (6%)
Nocturia (12%)
Hematuria (12%)
Urinary tract infection (9%)
Gynecomastia (9%)
Impotence (7%)
Breast pain (6%)
Urinary frequency (6%)
Urinary retention (5%)
Urination impaired (5%)
Urinary incontinence (4%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Arthralgia 11.9%
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Rash 11.9%
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Back pain 14.3%
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Pharyngitis 14.3%
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Hot flushes 16.7%
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Urinary tract infection 16.7%
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Asthenia 19%
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Diarrhoea 19%
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Dry skin 2.4%
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Pain 23.8%
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Constipation 31%
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Gynaecomastia 45.2%
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Breast pain 57.1%
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Insomnia 9.5%
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 72.1 years (range: 56-84 years)
Health Status: unhealthy
Age Group: 72.1 years (range: 56-84 years)
Sex: M
Sources:
Constipation 10.3%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Weight gain 10.3%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Pain 17.2%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Hot flushes 41%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Libido decreased 50%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Impotence 57%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Back pain 6.9%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Dyspepsia 6.9%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Dysuria 6.9%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Haematuria 6.9%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Pelvic pain 6.9%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Somnolence 6.9%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Urinary incontinence 6.9%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Urinary urgency 6.9%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Breast tenderness 79%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Gynaecomastia 79%
200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Dizziness 10%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Abdominal pain 11%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Anemia 11%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Diarrhea 12%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Hematuria 12%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Nocturia 12%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Dyspnea 13%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Peripheral edema 13%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Nausea 15%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Infection 18%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Pelvic pain 21%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Asthenia 22%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Constipation 22%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Back pain 25%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
General body pain 35%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Depression 4%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Fracture pathological 4%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Pneumonia 4%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Rhinitis 4%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Urinary incontinence 4%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Alkaline phosphatase increased 5%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Anxiety 5%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Arthritis 5%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Urinary retention 5%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Urination impaired 5%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Weight gain 5%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Hot flashes 53%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Anorexia 6%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Breast pain 6%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Bronchitis 6%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Flatulence 6%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Hyperglycemia 6%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Sweating 6%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Urinary frequency 6%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Vomiting 6%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Dyspepsia 7%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Flu syndrome 7%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Headache 7%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Impotence 7%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Insomnia 7%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Liver function test increased 7%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Myasthenia 7%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Weight loss 7%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Chest pain 8%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Cough increased 8%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Hypertension 8%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Paresthesia 8%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Pharyngitis 8%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Bone pain 9%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Gynecomastia 9%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Rash 9%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Urinary tract infection 9%
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M
Sources:
Overview

Overview

Drug as perpetrator​

Drug as perpetrator​

Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
likely
unlikely (co-administration study)
Comment: this isoenzyme is also responsible for the metabolism of (R)-bicalutamide; (S)-Bicalutamide is metabolised in vitro by CYP3A4
Page: 2.0
low
low
major
minor
minor
no
no
no
no
no
no
no
no
no
no
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Regulation of GCDFP-15 expression in human mammary cancer cells.
1999 Aug
Bicalutamide functions as an androgen receptor antagonist by assembly of a transcriptionally inactive receptor.
2002 Jul 19
Partial agonist/antagonist properties of androstenedione and 4-androsten-3beta,17beta-diol.
2004 Aug
Coregulator recruitment and histone modifications in transcriptional regulation by the androgen receptor.
2004 Nov
The androgen receptor co-activator CBP is up-regulated following androgen withdrawal and is highly expressed in advanced prostate cancer.
2004 Oct
Evaluation of tamoxifen and anastrozole in the prevention of gynecomastia and breast pain induced by bicalutamide monotherapy of prostate cancer.
2005 Feb 1
Androgen receptor signaling and vitamin D receptor action in prostate cancer cells.
2005 Sep 1
GREB1 is a novel androgen-regulated gene required for prostate cancer growth.
2006 Jun 1
Marked sexual dimorphism of lacrimal gland peroxidase in hamster: repression by androgens and estrogens.
2006 Mar 24
Therapeutic potential of CDK inhibitor NU2058 in androgen-independent prostate cancer.
2007 Dec 6
Androgen regulation of aldehyde dehydrogenase 1A3 (ALDH1A3) in the androgen-responsive human prostate cancer cell line LNCaP.
2007 Jun
Labeling and identification of LNCaP cell surface proteins: a pilot study.
2007 Jun 15
Hormonal regulation of beta2-adrenergic receptor level in prostate cancer.
2008 Jul 1
Prohibitin and the SWI/SNF ATPase subunit BRG1 are required for effective androgen antagonist-mediated transcriptional repression of androgen receptor-regulated genes.
2008 Sep
Differential mechanisms of bicalutamide-induced apoptosis in prostate cell lines.
2009
Genome-wide impact of androgen receptor trapped clone-27 loss on androgen-regulated transcription in prostate cancer cells.
2009 Apr 1
Interactions of methoxyacetic acid with androgen receptor.
2009 Jul 15
Development of a second-generation antiandrogen for treatment of advanced prostate cancer.
2009 May 8
REDD1 is a major target of testosterone action in preventing dexamethasone-induced muscle loss.
2010 Mar
Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer.
2014 Jun 12
Patents

Sample Use Guides

one 50 mg tablet once daily (morning or evening), with or without food
Route of Administration: Oral
Primary tumor cultures and PCa cell lines were treated with bicalutamide (0.1-10 uM) in the presence of dehydrotestosterone (10(-12) M) for 4 days. After bicalutamide treatment, no significant differences in the concentration that inhibits 50% were found among the different tumor cell lines (P = .081).
Name Type Language
BICALUTAMIDE
EP   HSDB   INN   JAN   MART.   MI   ORANGE BOOK   USAN   USP   USP-RS   VANDF   WHO-DD  
USAN   INN  
Official Name English
CASODEX
Preferred Name English
BICALUTAMIDE [HSDB]
Common Name English
ICI176,334-1
Code English
BICALUTAMIDE [ORANGE BOOK]
Common Name English
BICALUTAMIDE [USP-RS]
Common Name English
BICALUTAMIDE [USAN]
Common Name English
ICI-176334
Code English
BICALUTAMIDE [EP MONOGRAPH]
Common Name English
PROPANAMIDE, N-(4-CYANO-3-(TRIFLUOROMETHYL)PHENYL)-3-((4-FLUOROPHENYL)SULFONYL)-2-HYDROXY-2-METHYL-, (±)-
Systematic Name English
(±)-4'-CYANO-.ALPHA.,.ALPHA.,.ALPHA.-TRIFLUORO-3-((P-FLUOROPHENYL)SULFONYL)-2-METHYL-M-LACTOTOLUIDIDE
Common Name English
BICALUTAMIDE [USP IMPURITY]
Common Name English
BICALUTAMIDE [USP MONOGRAPH]
Common Name English
BICALUTAMIDE [JAN]
Common Name English
bicalutamide [INN]
Common Name English
Bicalutamide [WHO-DD]
Common Name English
ICI 176,334
Code English
BICALUTAMIDE [MART.]
Common Name English
BICALUTAMIDE [VANDF]
Common Name English
NSC-759816
Code English
BICALUTAMIDE [MI]
Common Name English
Classification Tree Code System Code
WHO-VATC QL02BB03
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
NDF-RT N0000000243
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
WHO-ATC L02AE51
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
NCI_THESAURUS C146993
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
WHO-ATC L02BB03
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
NDF-RT N0000175560
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
LIVERTOX NBK547970
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
Code System Code Type Description
FDA UNII
A0Z3NAU9DP
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
WIKIPEDIA
BICALUTAMIDE
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
DRUG CENTRAL
367
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
EVMPD
SUB05817MIG
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
PUBCHEM
2375
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
EPA CompTox
DTXSID2022678
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
IUPHAR
2863
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
MESH
C053541
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
INN
7021
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
NCI_THESAURUS
C1599
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
USAN
GG-51
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
RXCUI
83008
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY RxNorm
RS_ITEM_NUM
1071202
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
CAS
90357-06-5
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
ChEMBL
CHEMBL409
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
NSC
759816
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
HSDB
7655
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
MERCK INDEX
m2474
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY Merck Index
SMS_ID
100000085878
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
DAILYMED
A0Z3NAU9DP
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
DRUG BANK
DB01128
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY
CHEBI
3090
Created by admin on Mon Mar 31 19:15:55 GMT 2025 , Edited by admin on Mon Mar 31 19:15:55 GMT 2025
PRIMARY