Androgen deprivation & AR pathway inhibitors
Androgen deprivation lowers testosterone or blocks its receptor, and has been the foundation of prostate cancer treatment since 1941 (Nobel Prize 1966).
GnRH agonists/antagonists (leuprolide, relugolix) plus AR pathway inhibitors (abiraterone, enzalutamide, apalutamide, darolutamide) as triplet or doublet therapy in metastatic hormone-sensitive disease. Combined with PARP inhibitors in HRR-mutant, with capivasertib in PTEN-deficient (2026), and with 177Lu-PSMA in castration-resistant disease.
How it works
Suppress ligand or block AR; resistance via AR amplification, splice variants, and lineage plasticity.
- Prolonged disease control
- Metabolic and bone toxicity; castration resistance inevitable in metastatic disease
Abiraterone is a pill that shuts down testosterone production everywhere, including inside the tumour. Discovered at the Institute of Cancer Research, now generic and used from the first metastatic diagnosis.
An AR blocker approved for prostate cancer that has spread and for high-risk disease before it shows on scans.
The old antiandrogen pill used to block the testosterone flare from GnRH agonists and in combined androgen blockade; superseded by enzalutamide-class drugs.
Darolutamide is an AR blocker that barely enters the brain, so it causes fewer falls and cognitive side effects; it is approved with and without chemotherapy.
An injectable hormone blocker for prostate cancer that lowers testosterone within days without the initial surge caused by agonists.
The most widely used androgen-receptor blocker, approved across every stage of advanced prostate cancer, including rising PSA after surgery.
Leuprolide is the injectable that shuts off testosterone production, the foundation of hormone therapy for prostate cancer since the 1980s; it is also used for ovarian suppression in premenopausal breast cancer.
Relugolix is the first hormone-suppressing pill for prostate cancer, working within days and wearing off quickly when stopped.
Latest papers
topQuery for this technology: (TITLE:"androgen deprivation therapy" OR ABSTRACT:"androgen deprivation therapy" OR TITLE:"androgen receptor pathway inhibitor" OR ABSTRACT:"androgen receptor pathway inhibitor" OR TITLE:"enzalutamide" OR ABSTRACT:"enzalutamide" OR TITLE:"abiraterone" OR ABSTRACT:"abiraterone"). Results are unfiltered search hits about Androgen deprivation & AR pathway inhibitors, not a curated reading list.