Systemic Therapy Program
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Date



Disease Group



Cancer Type

Document Type

Drug Monographs
Treatment Regimens
Scientific Name:
CYPROTERONE
Brand Name(s):
Androcur Depot®, Androcur®

Drug Monograph

Pharmacology

Mechanism of Action

Steroid which clinically demonstrates 2 distinct properties:
Antiandrogenic: Cyproterone blocks the binding of dihydrotestosterone (active metabolite of testosterone) to the specific receptors in the prostatic carcinoma cells).
Progesteronic/antigonadotrophic: Cyproterone exerts a negative feed-back on the hypothalamo-pituitary axis, by inhibiting the secretion of LH leading to diminished production of testicular testosterone.

Pharmacokinetics

Oral Absorption:
oral absorption complete at 50 mg dose
Distribution:
tissue distribution is one of the major causes of the rapid fall of plasma levels
cross blood brain barrier? no information
Vd: no information 
PPB: no information
Metabolism:
the principle metabolite is 15 B-hydroxy-cyproterone acetate
metabolite(s) active- no information
  inactive- yes
Excretion:
drug is excreted unchanged in urine and feces
urine 33%  feces 60%
t½ 38 ± 5 hours (oral route); 38 ± 14 hours (IM route) 
Cl: no information

Side Effects

IMMEDIATE ONSET (hours to days)

• nausea and vomiting

EARLY ONSET (days to weeks)

• breast swelling or soreness (gynecomastia)
• discharge from the nipple (galactorrhea)
impotence or decreased sex drive (decreased libido)
• blood clots (thrombophlebitis)
• swelling of hands, feet or lower legs (edema)
• elevated liver function tests
• bowel changes (diarrhea or constipation)
• fatigue, lethargy, weakness
• increased serum calcium levels (hypercalcemia)
• loss of diabetic control
• hypochromic anemia (rare)

DELAYED/LATE ONSET (weeks to years)

• elevated liver function tests
• depression
• low sperm counts
• benign breast lumps (benign nodular hyperplasia of the breast)
• dry skin

Therapeutics

Approved Indications

Prostate cancer

Routes

Intramuscular
Oral

Dosing

Oral:
• bid: 50 mg taken after meals with diethylstilbestrol (DES) 0.1 mg daily
• bid: 100 mg as single agent or post orchidectomy

Intramuscular:
• q1-2w: 300 mg
Pediatric: No pediatric indications

Contraindications

• Severe liver or kidney dysfunction • Known hypersensitivity to cyproterone

Monitoring

Clinical Monitoring

RECOMMENDED CRITERIA
• Baseline & periodic liver function tests [serum alkaline phosphatase, GGT, ALT, AST & Bilirubin levels (serum proteins may be added if indicated)]

SUGGESTED CRITERIA
NO ADDITIONAL TOXICITY RATINGS

Extravasation Hazard

None

Significant Interactions

Ethinyl estradiol

Product Information

Commercial Product Description

• Androcur® White tablets with 50mg Cyproterone • Androcur Depot® Ampuls with 100mg Cyproterone in castor oil

Pharmaceutical Considerations

Depot injection:
100 mg/mL (3 mL ampul) cyproterone acetate in castor oil solution. Store at room temperature.

Tablets:
50 mg cyproterone acetate; store at room temperature. Contain corn starch and lactose. Tartrazine- and gluten-free.

Note

HANDLING RISK LEVEL:

HAZARD RISK LEVEL 2
FDA Pregnancy Risk Factor - Unknown
• This drug must be handled using precautions outlined in CCNS Policies for Preparing Cancer Chemotherapy and Administering Cancer Chemotherapy and the CCNS Standard for Oral Systemic Therapy for Cancer
• Go to "Additional Information" tab (above) for links to CCNS Policies

Availability & Funding

Administrative Information (Nova Scotia)

• CCNS Provincial Formulary Status- Community Level • Take Home Prescription • Pharmacare Formulary Status- Formulary Go to "Additional Information" tab (above) for links to Provincial Formulary of Cancer Drugs.