Enzalutamide is an oral hormonal medicine that blocks the effects of androgens (male hormones) on prostate cancer cells. It belongs to a class of medicines called androgen receptor inhibitors, used across several stages of advanced prostate cancer. It is a prescription-only medicine.

• Therapeutic Class: Anti-cancer (oncology) hormonal therapy.

• Pharmacological Class: Androgen receptor (AR) signalling inhibitor.

• Drug Family: Non-steroidal anti-androgens (second-generation).

• ATC Classification: L02BB04 (Enzalutamide).

Approved: Metastatic castration-resistant prostate cancer (mCRPC); metastatic castration-sensitive prostate cancer (mCSPC); nonmetastatic castration-resistant prostate cancer (NM-CRPC); and nonmetastatic castration-sensitive prostate cancer with high-risk biochemical recurrence, with or without a GnRH analog.

Commonly used for: Men with advanced prostate cancer at various stages, whether or not the disease has spread, and whether or not it still responds to standard hormone-lowering therapy.

Off-label use (only under medical guidance): Occasionally explored in earlier-stage or active-surveillance settings within clinical trials; not routine outside its approved indications.

● Oral capsules: 40 mg.

● Oral tablets: 40 mg and 80 mg.

Prostate cancer cells often rely on androgens (like testosterone) binding to a receptor called the androgen receptor to grow and survive. Enzalutamide blocks this receptor at multiple steps: it stops androgens from binding to it, prevents the receptor from moving into the cell's nucleus, and blocks it from attaching to DNA — cutting off the growth signal more thoroughly than older anti-androgen medicines.

• Standard dose: 160 mg (four 40 mg capsules or tablets) taken orally once daily.

• Condition-wise dose: Patients should remain on androgen deprivation therapy (a GnRH analog) or have had prior surgical removal of the testes to maintain castrate testosterone levels while on enzalutamide.

• Route: Oral, with or without food, at approximately the same time each day; capsules/tablets should be swallowed whole and not chewed, dissolved, or opened.

• Missed dose: If a dose is missed, it is omitted — extra doses are not taken to make up for it; the next dose is taken at the regular scheduled time.

• Overdose: May increase the risk of seizures or other known side effects; requires medical attention.

• Common: Fatigue, hot flashes, joint pain, high blood pressure, and decreased appetite.

• Serious: Seizures (a specific risk associated with enzalutamide), posterior reversible encephalopathy syndrome (PRES, rare), falls and fractures, and ischaemic heart disease.

• Emergency symptoms: A seizure, sudden severe headache with confusion or vision changes, chest pain, or a fall resulting in injury.

• Recovery advice: The seizure risk, while low, means patients with a history of seizures or conditions that predispose to seizures should discuss this carefully with their oncologist before starting; fatigue often improves as the body adjusts to treatment.

• Pregnancy: Not applicable (used only in men); women who are or may become pregnant should avoid contact with the capsules/tablets.   

• Breastfeeding: Not applicable.

• Liver disease: No dose adjustment needed in mild to moderate impairment; use with caution in severe impairment.

• Kidney disease: No specific dose adjustment established for mild to moderate impairment; used with caution in severe impairment.

• Elderly: Commonly used in this age group, as prostate cancer is more common with age.

• Children: Not applicable; a male-specific cancer medicine used in adults.

● Strong CYP2C8 inhibitors (e.g., gemfibrozil): increase enzalutamide levels; co-administration should be avoided if possible, or the enzalutamide dose reduced to 80 mg once daily.

● Strong CYP3A4 inducers (e.g., rifampin): can reduce enzalutamide levels and effectiveness.

● CYP3A4, CYP2C9, and CYP2C19 substrates with a narrow therapeutic index (e.g., warfarin, certain anti-seizure medicines): enzalutamide can reduce the levels of these drugs, requiring monitoring or dose adjustment.

● Medicines that lower the seizure threshold: used with added caution, given enzalutamide's own seizure risk.

● Blood pressure checks periodically.

● PSA (prostate-specific antigen) levels to monitor treatment response.

● Assessment for seizure risk factors before starting and throughout treatment.

● Fall and fracture risk assessment, particularly in older patients.

Abiraterone acetate, Apalutamide, Darolutamide (other hormonal therapies for advanced prostate cancer, different specific mechanisms/side-effect profiles).

Used alongside ongoing androgen deprivation therapy (GnRH analog) or surgical castration; also studied and used in combination with talazoparib (a PARP inhibitor) in certain BRCA-related or HRR-mutated prostate cancers.

● Prostate Cancer Medicines

● Hormonal (Endocrine) Cancer Therapies

● Androgen Receptor Inhibitors

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1. https://www.accessdata.fda.gov/drugsatfda_docs/label

2. https://www.oncologynewscentral.com/drugs/guide/enzalutamide-prostate-cancer

The information on this page is for educational purposes only and is not a substitute for medical advice. Please consult your oncologist to know if this treatment is appropriate for your condition.