enzalutamide
Xtandi (enzalutamide) is an androgen receptor inhibitor from Astellas for prostate cancer. It blocks androgen binding, receptor activation and nuclear signalling in one drug, and is used across castration-resistant and hormone-sensitive disease settings.
This page is based on FDA prescribing information and the EMA medicine record for enzalutamide, cross-checked with DailyMed and MedlinePlus; the mechanism is explained in plain language, and analogies are used only where they stay accurate.
How it works
Explains what the medicine does in the body, not dosing, side effects, or safety.
An analogy
Androgen signalling is a three-step delivery - the hormone docks, the receptor carries the parcel into the cell's control room, and the instructions get read aloud. Enzalutamide blocks the dock, escorts the carrier away from the door, and muffles the reading, so the growth orders never get acted on.
In simple terms
Prostate cancers usually depend on male hormones acting through the androgen receptor. Enzalutamide blocks the receptor itself: it stops androgens from binding, prevents the receptor from moving into the cell nucleus, and stops it from switching on growth genes. This multi-step blockade slows tumour growth and delays spread, even when blood hormone levels are already low.
In depth
Enzalutamide is a non-steroidal androgen receptor antagonist that competitively inhibits androgen binding, blocks nuclear translocation of the receptor and impairs AR-DNA interaction, a three-stage mechanism distinct from earlier antiandrogens. It retains activity against several resistance-associated AR variants, though amplification and splice variants can limit responses. It is administered orally across metastatic and non-metastatic prostate cancer settings.
See it in motion
A schematic animation of the mechanism — simplified for clarity, not drawn to scale.
Enzalutamide blocks the dock, escorts the carrier away from the door, and muffles the reading
- Androgen signalling is a three-step delivery - the hormone docks, the receptor carries the parcel into the cell's control room, and the instructions get read aloud.
- Enzalutamide blocks the receptor itself: it stops androgens from binding, prevents the receptor from moving into the cell nucleus, and stops it from switching on growth genes.
- It retains activity against several resistance-associated AR variants, though amplification and splice variants can limit responses.
- This multi-step blockade slows tumour growth and delays spread, even when blood hormone levels are already low.
Target: Androgen receptor (AR)
The receptor through which androgens drive prostate cancer growth; blocking its activation, nuclear entry and DNA binding cuts the growth programme at several points at once.
Approved uses
Approved uses differ by country and change over time. Always follow your local prescribing information.
Approved uses in United States
FDA- Treatment of patients with castration-resistant prostate cancer
- Treatment of patients with metastatic castration-sensitive prostate cancer
- Treatment of patients with non-metastatic castration-sensitive prostate cancer with biochemical recurrence at high risk for metastasis
Approved uses in European Union
EMA- As monotherapy or with androgen deprivation therapy, for adult men with high-risk biochemical recurrent non-metastatic hormone-sensitive prostate cancer who are unsuitable for salvage radiotherapy
- For adult men with metastatic hormone-sensitive prostate cancer in combination with androgen deprivation therapy
Official sources
The statements on this page trace back to these records.
- Xtandi (enzalutamide) — Summary of product characteristics and package leaflet, English version
European Medicines Agency
- DailyMed: Xtandi (enzalutamide) label
DailyMed, U.S. National Library of Medicine
- U.S. Food and Drug Administration: enzalutamide prescribing information
U.S. Food and Drug Administration
- MedlinePlus: enzalutamide
MedlinePlus, U.S. National Library of Medicine
- National Cancer Institute: enzalutamide
National Cancer Institute
This page explains how the medicine works — it isn’t the patient leaflet. For anything that applies to you, read the leaflet that came with your medicine or ask your pharmacist.
MedUnfold provides educational content and is not medical advice. Always follow your local prescribing information and healthcare professional.