Drug reference

Enzalutamide

Hormonal Anticancer Agent · Antineoplastic

Hormonal Anticancer AgentAntineoplasticATC null

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

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Mechanism

Enzalutamide is a potent orally active antiandrogen. It acts as a competitive antagonist at the androgen receptor.

Indications

Metastatic carcinoma of the prostateHormone-relapsed metastatic prostate cancer in patients who have no or mild symptoms after androgen deprivation therapy has failed, and before chemotherapy is indicatedHormone-relapsed metastatic prostate cancer if disease has progressed during or after treatment with a docetaxel-containing chemotherapy regimenNonmetastatic castration-resistant prostate cancer (CRPC)Metastatic CRPCMetastatic castration-sensitive prostate cancerProlongs survival in metastatic CRPC (chemotherapy-naïve or after docetaxel therapy)Prolongs metastasis-free and overall survival in men with nonmetastatic castration-resistant disease and rapidly rising circulating prostate-specific antigen (in combination with ADT)

Dosing

Adult: indication] can be used, initially for up to 10 weeks, to manage troublesome hot ﬂushes caused by long-term androgen suppression; cyproterone acetate can be considered as an alternative if medroxyprogesterone acetate is not effective or not tolerated.…

Pharmacokinetics

Onset

Median time to reach Cmax is 1 hour. Steady-state levels are achieved in 28 days.

Half-life

Approximately 6 days.

Metabolism

Metabolized by CYP2C8 and CYP3A4. Enzalutamide can induce multiple hepatic CYPs, including 3A4, 2C9, and 2C19.

Side effects

Common

FatigueBack painHot flushConstipationArthralgiaDecreased appetiteDiarrheaHypertensionSexual dysfunctionGynecomastiaBreast painHeadacheMusculoskeletal pain

Serious

Fractures
Falls
Cognitive impairment
Increased risk of short-term mortality in elderly prostate cancer patients with preexisting cardiovascular comorbidities
Seizures (occur infrequently, 0.5%–2.2% of patients) due to crossing the blood-brain barrier