Prostate and other male cancers:

Indications for: XTANDI

Castration-resistant prostate cancer (CRPC). Metastatic castration-sensitive prostate cancer (mCSPC).

Adult Dosage:

Swallow whole. 160mg once daily. Give concurrent GnRH analog or patient should have had bilateral orchiectomy. Dose modifications: ≥Grade 3 toxicity or intolerable side effect: withhold dose for 1 week or until improvement to ≤Grade 2, then resume at same or reduced dose (120mg or 80mg), if warranted. Concomitant strong CYP2C8 inhibitors, if unavoidable: reduce to 80mg once daily. Concomitant strong CYP3A4 inducers, if unavoidable: increase to 240mg once daily. When CYP2C8 inhibitor or CYP3A4 inducer is discontinued, return enzalutamide dose to the dose used prior to initiation of the inhibitor or inducer.

Children Dosage:

Not established.

XTANDI Warnings/Precautions:

Risk of seizure; permanently discontinue if occurs. Discontinue if posterior reversible encephalopathy syndrome (PRES) develops. Monitor for ischemic heart disease; discontinue if Grade 3 or 4 develops. Manage CV risk factors (eg, hypertension, diabetes, dyslipidemia). Evaluate for fall and fracture risk; monitor and manage as per established guidelines. Severe renal impairment or ESRD: not studied. Embryo-fetal toxicity. Advise males (w. female partners of reproductive potential) to use effective contraception during and for 3 months after the last dose.

XTANDI Classification:

Androgen receptor inhibitor.

XTANDI Interactions:

Avoid concomitant strong CYP2C8 inhibitors (eg, gemfibrozil); if unavoidable, reduce dose (see Adult dose). Avoid concomitant strong CYP3A4 inducers (eg, rifampin); if unavoidable, increase dose (see Adult dose). Antagonizes midazolam (CYP3A4 substrate) and omeprazole (CYP2C19 substrate). May antagonize certain CYP3A4, CYP2C9, or CYP2C19 substrates; increase dose of these substrates, if unavoidable. Caution with concomitant drugs that may lower the seizure threshold.

Adverse Reactions:

Asthenia/fatigue, back pain, hot flush, constipation, arthralgia, decreased appetite, diarrhea, hypertension; seizure, PRES, ischemic heart disease, falls, fractures, hypersensitivity reactions (permanently discontinue if severe).

Generic Drug Availability:


How Supplied:

Caps, tabs 40mg—120; Tabs 80mg—60