Prostaxen 60

• Metastatic castration-sensitive prostate cancer (mCSPC)
• Non-metastatic castration-resistant prostate cancer (NM-CRPC)

Apalutamide is an orally administered, selective Androgen Receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR. Apalutamide prevents AR nuclear translocation, inhibits DNA binding, impedes AR-mediated transcription, and lacks androgen receptor agonist activity.

Apalutamide treatment decreases tumor cell proliferation and increases apoptosis, leading to potent antitumor activity in mouse xenograft models of prostate cancer.

Recommended Dose: 240 mg (four 60 mg tablets) orally once daily.

Concurrent Treatment: Patients should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had a bilateral orchiectomy.

Important: Swallow tablets whole. Do not crush or split the tablets.

Common (>10%):

• Hypercholesterolemia (76%)
• Anemia (70%)
• Hyperglycemia (70%)
• Hypertriglyceridemia (67%)
• Leukopenia (47%)
• Lymphopenia (41%)
• Fatigue (39%)
• Hyperkalemia (32%)
• Hypertension (25%)
• Rash (24%)
• Diarrhea (20%)
• Nausea (18%)
• Arthralgia (16%)
• Fall (16%)
• Weight decreased (16%)
• Hot flush (14%)
• Fracture (12%)
• Decreased appetite (12%)
• Peripheral edema (11%)

Grades 3-4 (>10%): Hypertension (14%)

1-10%: Hypothyroidism (8%), Pruritus (6.2%), Ischemic heart disease (3.7%), Heart failure (2.2%)

Grades 3-4 (1-10%): Rash (5%), Fracture (3%), Fall (2%), Hypertriglyceridemia (2%), Lymphopenia (2%), Hyperkalemia (2%), Hyperglycemia (2%)

Contraindicated during pregnancy: Based on its mechanism of action, the drug can cause fetal harm and potential loss of pregnancy. No available data regarding use in pregnant women. Not indicated for use in females.

Contraception: Male patients with female partners of reproductive potential should use effective contraception during treatment and for 3 months after the last dose.

Serious Precautions:

• Not recommended in patients with history of seizures or predisposing factors (brain injury, stroke, brain tumors) - permanently discontinue if seizure occurs during treatment
• Falls and fractures risk - evaluate patient for risk; consider bone-targeted agents
• Ischemic heart disease - most patients had cardiac risk factors; monitor for signs and symptoms
• Safety not established in patients with clinically significant cardiovascular disease in the past 6 months
• Androgen deprivation therapy may prolong QT interval
• Contraindicated during pregnancy - may cause fetal harm
• Not indicated for use in females

There is no known specific antidote for apalutamide overdose. In the event of an overdose, stop apalutamide, undertake general supportive measures until clinical toxicity has been diminished or resolved.

Store below 30°C. Protect from moisture and light. Keep out of reach of children.