Abiraterone

DEA Class; Rx

Common Brand Names; Zytiga, Yonsa

• Antineoplastics, Antiandrogen

Indicated for the treatment of metastatic prostate cancer.

Indicated in combination with prednisone for patients with metastatic castration-resistant prostate cancer (CRPC)

Indicated in combination with methylprednisolone for the treatment of patients with metastatic CRPC

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Adverse drug reactions are for abiraterone with prednisone

• Hypertriglyceridemia (63%)
• Hyperglycemia, nonfasting (57%)
• Increased ALT (11-46%)
• Fatigue (39%)
• Lymphopenia (20-38%)
• Increased AST (15-37%)
• Hypertension (8.5-37%)
• Hypernatremia (33%)
• Joint swelling/discomfort (30%)
• Hypokalemia (17-30%)
• Edema (25-27%)
• Muscle discomfort (26%)
• Hypophosphatemia (24%)
• Constipation (23%)
• Hot flush (15-22%)
• Diarrhea (18-22%)
• Hot flush (19%)
• Cough (6.5-17%)
• Increased total bilirubin (6.6-16%)
• Insomnia (14%)
• Contusion (13%)
• Upper respiratory tract infection (5.4-13%)
• Urinary tract infection (7-12%)
• Dyspnea (12%)
• Nasopharyngitis (11%)
• Dyspepsia (6.1-11%)

Caution in patients with a history of cardiovascular disease; safety in patients with LVEF <50% or NYHA Class III or IV heart failure is not established

Hypertension, hypokalemia, and fluid retention may result from increased mineralocorticoid due to CYP17 inhibition; control hypertension and correct hypokalemia before treatment; monitor blood pressure, serum potassium, and symptoms of fluid retention at least monthly

Closely monitor patients with medical conditions that might be compromised by increased blood pressure, hypokalemia, or fluid retention (eg, heart failure, recent MI, cardiovascular disease, ventricular arrhythmia)

QT prolongation and Torsades de Pointes observed in patients who develop hypokalemia during postmarketing surveillance and additional clinical trials

Adrenocortical insufficiency reported in patients receiving abiraterone in combination with prednisone, following interruption of daily steroids and/or with concurrent infection or stress; monitor for symptoms and signs of adrenocortical insufficiency; increased corticosteroid dosage may be indicated before, during, and after stressful situations; concurrent infection or interruption of daily corticosteroids associated with adrenocortical insufficiency

In postmarketing experience, severe hepatic toxicity, including fulminant hepatitis, acute liver failure and deaths occurred

Drug plus prednisone/prednisolone not recommended for use in combination with radium 223 dichloride outside clinical trials; increased incidences of fractures (and deaths observed in patients who received drug plus prednisone/prednisolone in combination with radium Ra 223 dichloride compared to placebo in combination with drug plus prednisone/prednisolone

Based on animal studies and mechanism of action, may cause fetal harm and loss of pregnancy

Based on findings from animal studies and mechanism of action, abiraterone is contraindicated for use in pregnant women because drug can cause fetal harm and potential loss of pregnancy

Not indicated for use in females

Not indicated for women

No information available on the presence of abiraterone acetate in human milk, or on the effects on the breastfed child or milk production

Abiraterone acetate

tablet (Zytiga)

• 250mg
• 500mg

ultramicronized tablet (Yonsa)

• 125mg