OnCo
technologiesTechnologyStandard of care

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.

Schematic · not to scale
Androgen receptor · Antagonist in pocket · Testosterone removed

How it works

Suppress ligand or block AR; resistance via AR amplification, splice variants, and lineage plasticity.

Strengths
  • Prolonged disease control
Limitations
  • Metabolic and bone toxicity; castration resistance inevitable in metastatic disease
Since
1941

Products

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ApprovedSmall-molecule CYP17A1 inhibitor
Abiraterone acetate · Zytiga (generic)

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.

ApprovedSmall-molecule AR antagonist
Apalutamide · Erleada

An AR blocker approved for prostate cancer that has spread and for high-risk disease before it shows on scans.

Not mapped hereOral first-generation non-steroidal antiandrogen
Bicalutamide · Casodex

The old antiandrogen pill used to block the testosterone flare from GnRH agonists and in combined androgen blockade; superseded by enzalutamide-class drugs.

ApprovedSmall-molecule AR antagonist
Darolutamide · Nubeqa

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.

Not mapped hereGnRH antagonist depot
Degarelix · Firmagon

An injectable hormone blocker for prostate cancer that lowers testosterone within days without the initial surge caused by agonists.

ApprovedSmall-molecule AR antagonist
Enzalutamide · Xtandi

The most widely used androgen-receptor blocker, approved across every stage of advanced prostate cancer, including rising PSA after surgery.

Not mapped hereGnRH agonist depot
Leuprolide (leuprorelin) and GnRH agonists · Lupron / Eligard / Camcevi

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.

ApprovedOral GnRH antagonist
Relugolix · Orgovyx

Relugolix is the first hormone-suppressing pill for prostate cancer, working within days and wearing off quickly when stopped.

Key papers

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Latest papers

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Literature trend1,435 papers in the last 12 months+18% vs prior 12How this is computed
Latest papers · live from Europe PMC
Open in Europe PMC

Query 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.

Connected

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