apalutamide
Erleada (apalutamide) is an oral androgen receptor inhibitor from Janssen for prostate cancer. It blocks the receptor that prostate tumour cells need to grow, and is used in non-metastatic castration-resistant disease and, with androgen deprivation therapy, in metastatic hormone-sensitive disease.
This page is based on FDA prescribing information and the EMA medicine record for apalutamide, 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
Prostate cancer cells are machines that run on a fuel called androgen. Castration therapy shuts off the fuel supply, but the machines keep idling, ready to burn any trace that appears. Apalutamide puts a lock over each machine's fuel intake, so even stray fuel cannot restart them.
In simple terms
Prostate cancer cells usually need male hormones, called androgens, to grow. Treatments that lower androgen levels work for a while, but cancers can adapt. Apalutamide blocks the androgen receptor itself, the switch that tells the cell to grow. With the switch jammed, cancer cells stop multiplying and many of them die, delaying the spread of the disease.
In depth
Apalutamide is a selective, high-affinity antagonist of the androgen receptor. It prevents androgen binding, blocks nuclear translocation of the receptor and inhibits AR-mediated transcription, including in tumours with AR overexpression. In preclinical models it reduces prostate cancer cell proliferation and induces apoptosis. A major metabolite, N-desmethyl apalutamide, is a less potent inhibitor of AR, and exhibited one-third the activity of apalutamide in an in vitro transcriptional reporter assay.
See it in motion
A schematic animation of the mechanism — simplified for clarity, not drawn to scale.
How apalutamide antagonises the androgen receptor
- Prostate cancer cells usually need male hormones, called androgens, to grow.
- Apalutamide is a selective, high-affinity antagonist of the androgen receptor. It prevents androgen binding, blocks nuclear translocation of the receptor and inhibits AR-mediated transcription, including in tumours with AR overexpression.
- In preclinical models it reduces prostate cancer cell proliferation and induces apoptosis.
- A major metabolite, N-desmethyl apalutamide, is a less potent inhibitor of AR, and exhibited one-third the activity of apalutamide in an in vitro transcriptional reporter assay.
Target: Androgen receptor (AR)
A hormone-activated receptor that drives growth and survival of prostate cells; most prostate cancers remain dependent on androgen receptor signalling even when blood testosterone is suppressed.
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 metastatic castration-sensitive prostate cancer
- Treatment of patients with non-metastatic castration-resistant prostate cancer
Approved uses in European Union
EMA- In adult men, for the treatment of non-metastatic castration-resistant prostate cancer who are at high risk of developing metastatic disease
- In adult men, for the treatment of metastatic hormone-sensitive prostate cancer in combination with androgen deprivation therapy
Official sources
The statements on this page trace back to these records.
- Erleada (apalutamide) — Summary of product characteristics and package leaflet, English version
European Medicines Agency
- DailyMed: Erleada (apalutamide) label
DailyMed, U.S. National Library of Medicine
- U.S. Food and Drug Administration: apalutamide prescribing information
U.S. Food and Drug Administration
- MedlinePlus: apalutamide
MedlinePlus, U.S. National Library of Medicine
- National Cancer Institute: apalutamide
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.