Enzalutamide

XTANDI

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Pronunciation: en-za-LOO-ta-mide (ex-TAN-dee)

Enzalutamide ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Enzalutamide ballicule

Enzalutamide XTANDI mascot mnemonic cartoon — Visual mnemonic: Enzalutamide mascot
**“Standing In salute am I”**

What it isAndrogen receptor antagonist blocking binding, nuclear translocation and DNA interaction; prostate cancer.

Why this oneTriple blockade of the receptor pathway gives survival benefit where first-generation antiandrogens fail.

What limits itSeizure risk, fatigue and falls. A strong CYP3A4 inducer, so co-prescribed drugs fail.

Enzalutamide molecular structure (skeletal formula) — Molecular structure: Enzalutamide

FDA-approved for

prostate cancer (2012)

FDA label

Read the full label on DailyMed ↗

FDA dosing	Population	Start	Target	Max
Prostate cancer (CRPC, mCSPC, or nmCSPC with high-risk BCR)	adult male	160 mg PO QD	160 mg PO QD	160 mg PO QD

Renal No adjustment for mild–moderate (CrCl >=30 mL/min); not studied in severe impairment/ESRD.

Hepatic No adjustment needed

Instructions

Swallow capsules/tablets whole with water; do not chew, dissolve, or open capsules, or cut/crush/chew tablets
With or without food
CRPC/mCSPC: also give a GnRH analog concurrently or have prior bilateral orchiectomy
For >=Grade 3 or intolerable toxicity, withhold ~1 week until <=Grade 2, then resume at same or reduced dose (120 mg or 80 mg)

Available strengths

cap 40 mg
tab 40, 80 mg

Cautions

Seizure (permanently discontinue if it occurs)
Posterior reversible encephalopathy syndrome (PRES)
Hypersensitivity
Ischemic heart disease
Falls and fractures
Embryo-fetal toxicity / loss of pregnancy — male contraception advised
Severe dysphagia/choking related to tablet size

Adverse reactions

Musculoskeletal pain
Fatigue
Hot flush
Constipation
Decreased appetite
Diarrhea
Hypertension
Hemorrhage
Falls
Fracture
Headache

Pregnancy Can cause fetal harm and loss of pregnancy (not indicated in females); based on animal data and mechanism of action.

Lactation Not indicated in females; no human data.

Cost

Enzalutamide (XTANDI)

Strength		#/mo	CostPlus
40 mg	tab	30 qd	not offered
80 mg	tab	30 qd	not offered
40 mg	cap	30 qd	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Enzalutamide is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2027 est.

NO BOXED WARNINGS

Principal riskSeizure risk; a strong CYP3A4 inducer

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryMultiple / indication-, trimester- or formulation-dependent

Defining liabilityThrombotic, metabolic, hepatic, skeletal or reproductive toxicity varies by hormonal target.

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Memory aids: interaction avatars

CYP2C19 inducer (moderate)

CYP2C8 substrate

CYP2C9 inducer (moderate)

CYP3A4 inducer (strong)

Open Enzalutamide in the interactive console ↗