#最小單位貼紙

Use in combination with prednisone for the treatment of patients with metastatic castration-resistant prostate cancer who have received prior chemotherapy containing docetaxel
#仿單變更2021

Antineoplastic Agent, Antiandrogen
Selectively and irreversibly inhibits CYP17 (17 alpha-hydroxylase/C17,20-lyase), an enzyme required for androgen biosynthesis which is expressed in testicular, adrenal, and prostatic tumor tissues. Inhibits the formation of the testosterone precursors dehydroepiandrosterone (DHEA) and androstenedione.

Absorption
1. Effects of food: Cmax 7- to 17-fold increase
2. AUC: 5- to 10-fold increase
Distribution
Protein binding: >99%
Metabolism
1. Hydrolyzed to the active metabolite abiraterone
2. Further metabolized to inactive metabolites abiraterone sulphate and N-oxide abiraterone sulphate via CYP3A4 and SULT2A1
Elimination Half Life
12 +/- 5 hours, prolonged in hepatic impairment

1. Pregnancy and women of childbearing potential (may cause fetal harm or loss of pregnancy, use effective contraception during treatment and for at least 1 week following discontinuation)
2. Preexisting severe hepatic impairment (Child-Pugh class C)

X

Avoided

Common:
Joint swelling or discomfort, hypokalemia, edema, muscle discomfort, hot flush, diarrhea, urinary tract infection, cough, hypertension, arrhythmia, urinary frequency, nocturia, dyspepsia, fractures, upper respiratory tract infection
Warnings:
1. Adrenocortical insufficiency: Concurrent infection, stress, or interruption of daily corticosteroids is associated with reports of adrenocortical insufficiency. Monitor closely for signs and symptoms.
2. Hepatotoxicity: Severe hepatotoxicity (eg, fulminant hepatitis, acute liver failure, and death) and significant increases in liver enzymes (ALT, AST, and bilirubin should be monitored prior to treatment, every 2 weeks for 3 months and monthly thereafter) has been reported. Do not use in patients with preexisting severe hepatic impairment (Child-Pugh class C).
3. Mineralocorticoid excess: Increased mineralocorticoids due to CYP17 inhibition may result in hypertension, hypokalemia, and fluid retention.
4. Cardiovascular disease: May cause hypertension, hypokalemia, and fluid retention.
5. Diabetes: Severe hypoglycemia has been reported, particularly in patients receiving concomitant therapy with thiazolidinediones (eg, pioglitazone) or repaglinide.<20211129>

Dosage:
ZYTIGA 1,000 mg (4 tablets) administered orally once daily in combination with prednisone 5 mg administered orally twice daily.
Administration:
1. ZYTIGA must be taken on an empty stomach. Administer on an empty stomach, at least 1 hour before and 2 hours after food. Concomitant administration with food may increase drug exposure and lead to adverse drug reactions.<20230130>
2. The tablets should be swallowed whole with water. Do not crush or chew!