# Androgen receptor

Source: https://onco.cc/targets/androgen-receptor/  
OnCo record `androgen-receptor` (Target). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

The hormone switch that drives prostate cancer, attacked by castration and by pills that block the receptor.

## Summary

Androgen deprivation plus AR pathway inhibitors (abiraterone, enzalutamide, apalutamide, darolutamide) is standard in advanced prostate cancer. AR degraders, AR N-terminal domain inhibitors, and combinations with PARP or AKT inhibitors address castration resistance. AR is also a target in a subset of TNBC (luminal androgen receptor subtype).

## Fields

- Kind: Target
- Last checked: 2026-09-04
- Tags: hormonal
- Symbol: AR
- Class: nuclear-receptor
- Biology: Nuclear receptor; amplification, splice variants (AR-V7), and ligand-binding-domain mutations drive resistance.
- Where found: Prostate cancer; LAR-subtype TNBC; Salivary duct carcinoma; Triple-negative breast cancer: ar expression and luminal androgen receptor subtype 12-16%; Prostate cancer: high-level amplification of the gene, and of an upstream enhancer 1-57% depending on disease state; Prostate cancer: l702h, w742c/l, h875y, t878a, f877l 0.4-18% depending on disease state

## Notes

- Triple-negative breast cancer: the luminal androgen receptor subtype is 16% (Lehmann 2016, Bareche 2018); AR nuclear staining above 10% in 12% of ER/PR-negative patients screened for bicalutamide (Gucalp 2013); clinical benefit rates 19% (bicalutamide) and 25 to 33% (enzalutamide; Traina 2018). LAR tumours carry PIK3CA in 55% and are 75% HER2-enriched by PAM50 (Bareche 2018).

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Androgen_receptor
- Wikipedia: https://en.wikipedia.org/wiki/Androgen_receptor

## Connected records

- biomarkers: [AR amplification (gene and upstream enhancer)](https://onco.cc/biomarkers/ar-amplification/), [AR ligand-binding-domain mutation (L702H, W742C, H875Y, T878A, F877L)](https://onco.cc/biomarkers/ar-ligand-binding-domain-mutation/), [AR-V7 splice variant](https://onco.cc/biomarkers/ar-v7-splice-variant/), [Circulating tumour DNA fraction (and what a negative plasma result means)](https://onco.cc/biomarkers/ctdna-tumour-fraction/), [SPOP mutation](https://onco.cc/biomarkers/spop-mutation/), [TMPRSS2-ERG fusion (and the other ETS rearrangements)](https://onco.cc/biomarkers/tmprss2-erg-fusion/), [Treatment-emergent neuroendocrine transformation (recognising it)](https://onco.cc/biomarkers/nepc-transformation/)
- cancers: [Apocrine carcinoma of the breast](https://onco.cc/cancers/apocrine-carcinoma-breast/), [Luminal androgen receptor triple-negative breast cancer (LAR)](https://onco.cc/cancers/tnbc-luminal-androgen-receptor/), [Prostate cancer](https://onco.cc/cancers/prostate/), [Salivary gland cancers](https://onco.cc/cancers/salivary-gland/), [Triple-negative breast cancer (TNBC)](https://onco.cc/cancers/tnbc/)
- drugs: [Abiraterone acetate](https://onco.cc/drugs/abiraterone/), [Apalutamide](https://onco.cc/drugs/apalutamide/), [AZD9750](https://onco.cc/drugs/azd9750/), [Bicalutamide](https://onco.cc/drugs/bicalutamide/), [BMS-986365](https://onco.cc/drugs/bms-986365/), [Darolutamide](https://onco.cc/drugs/darolutamide/), [Degarelix](https://onco.cc/drugs/degarelix/), [Enzalutamide](https://onco.cc/drugs/enzalutamide/), [EP0062](https://onco.cc/drugs/ep0062/), [Fluoxymesterone](https://onco.cc/drugs/fluoxymesterone/), [Flutamide](https://onco.cc/drugs/flutamide/), [Galeterone](https://onco.cc/drugs/galeterone/), [Leuprolide (leuprorelin) and GnRH agonists](https://onco.cc/drugs/leuprolide/), [Masofaniten](https://onco.cc/drugs/masofaniten/), [Mevrometostat](https://onco.cc/drugs/mevrometostat/), [Nilutamide](https://onco.cc/drugs/nilutamide/), [QLH12016](https://onco.cc/drugs/qlh12016/), [Rezvilutamide](https://onco.cc/drugs/rezvilutamide/), [Triptorelin](https://onco.cc/drugs/triptorelin/)
- companies: [Monte Rosa Therapeutics](https://onco.cc/companies/monte-rosa/), [ORIC Pharmaceuticals](https://onco.cc/companies/oric-pharmaceuticals/), [Veru](https://onco.cc/companies/veru/)
- pathways: [Androgen receptor signalling](https://onco.cc/pathways/ar-signaling/), [Chemical carcinogenesis - receptor activation](https://onco.cc/pathways/chemical-carcinogenesis-receptor-activation/), [Lineage plasticity & neuroendocrine transformation](https://onco.cc/pathways/lineage-plasticity-neuroendocrine/), [Prostate cancer (KEGG map)](https://onco.cc/pathways/prostate-cancer-signalling/), [Resistance routes: how a blocked pathway comes back](https://onco.cc/pathways/resistance-routes-map/), [RNA splicing](https://onco.cc/pathways/rna-splicing/), [Transcriptional machinery & addiction](https://onco.cc/pathways/transcription-addiction/), [Ubiquitin-proteasome system & protein homeostasis](https://onco.cc/pathways/ubiquitin-proteasome-system/)
- terms: [Agonist and antagonist](https://onco.cc/terms/agonist-antagonist/), [Androgen receptor pathway inhibitor (ARPI)](https://onco.cc/terms/arpi/), [Androgen receptor-positive triple-negative breast cancer](https://onco.cc/terms/androgen-receptor-positive-tnbc/), [AR-V7 splice variant](https://onco.cc/terms/ar-v7/), [Bipolar androgen therapy (BAT)](https://onco.cc/terms/bipolar-androgen-therapy/), [Hormone therapy](https://onco.cc/terms/hormone-therapy/), [Intermittent androgen deprivation (IAD)](https://onco.cc/terms/intermittent-androgen-deprivation/), [Luminal androgen receptor (LAR) subtype](https://onco.cc/terms/luminal-androgen-receptor/), [mCRPC and mHSPC (castration-resistant vs hormone-sensitive prostate cancer)](https://onco.cc/terms/mcrpc-mhspc/), [Neuroendocrine differentiation in prostate cancer](https://onco.cc/terms/neuroendocrine-differentiation/), [PAM50 / intrinsic subtypes](https://onco.cc/terms/pam50/), [Receptor](https://onco.cc/terms/receptor/)
- key papers: [Abiraterone in metastatic prostate cancer without previous chemotherapy](https://onco.cc/key-papers/paper-abiraterone-acetate-prostate-n-engl-j-med-2013/), [AFFIRM: increased survival with enzalutamide in prostate cancer after chemotherapy](https://onco.cc/key-papers/paper-scher-affirm-enzalutamide-nejm-2012/), [Androgen receptor pathway-independent prostate cancer is sustained through FGF signalling](https://onco.cc/key-papers/paper-bluemn-double-negative-prostate-fgf-mapk-cancer-cell-2017/), [AR-V7 and resistance to enzalutamide and abiraterone in prostate cancer](https://onco.cc/key-papers/paper-antonarakis-ar-v7-resistance-nejm-2014/), [Circulating tumour DNA genomics correlate with resistance to abiraterone and enzalutamide in prostate cancer](https://onco.cc/key-papers/paper-annala-ctdna-resistance-abiraterone-enzalutamide-cancer-discov-2018/), [Combined tumour suppressor defects characterise clinically defined aggressive variant prostate cancers](https://onco.cc/key-papers/paper-aparicio-aggressive-variant-prostate-tumour-suppressors-ccr-2016/), [Comprehensive genomic analysis identifies novel subtypes and targets of triple-negative breast cancer](https://onco.cc/key-papers/paper-burstein-tnbc-genomic-subtypes-ccr-2015/), [Concordance of circulating tumour DNA and matched metastatic tissue biopsy in prostate cancer](https://onco.cc/key-papers/paper-wyatt-ctdna-tissue-concordance-mcrpc-jnci-2017/), [Detecting neuroendocrine prostate cancer through tissue-informed cell-free DNA methylation analysis](https://onco.cc/key-papers/paper-berchuck-cfdna-methylation-nepc-detection-ccr-2022/), [Differences in prostate cancer genomes by self-reported race](https://onco.cc/key-papers/paper-stopsack-prostate-genomes-by-race-ccr-2022/), [Divergent clonal evolution of castration-resistant neuroendocrine prostate cancer](https://onco.cc/key-papers/paper-beltran-nepc-divergent-evolution-nat-med-2016/), [Enzalutamide for the treatment of androgen receptor-expressing triple-negative breast cancer](https://onco.cc/key-papers/paper-traina-enzalutamide-ar-tnbc-jco-2018/), [Genomic analysis of circulating tumour DNA in 3,334 patients with advanced prostate cancer identifies targetable BRCA alterations and AR resistance mechanisms](https://onco.cc/key-papers/paper-tukachinsky-ctdna-3334-advanced-prostate-ccr-2021/), [Genomic and transcriptomic landscape of triple-negative breast cancers: subtypes and treatment strategies](https://onco.cc/key-papers/paper-jiang-fuscc-tnbc-landscape-cancer-cell-2019/), [Genomic correlates of clinical outcome in advanced prostate cancer](https://onco.cc/key-papers/paper-abida-genomic-correlates-outcome-mcrpc-pnas-2019/), [Genomic hallmarks and structural variation in metastatic prostate cancer](https://onco.cc/key-papers/paper-quigley-structural-variation-mcrpc-cell-2018/), [Genomics of lethal prostate cancer at diagnosis and castration resistance](https://onco.cc/key-papers/paper-mateo-genomics-lethal-prostate-diagnosis-castration-resistance-jci-2020/), [Huggins and Hodges 1941: the effect of castration, of oestrogen and of androgen injection on serum phosphatases in metastatic carcinoma of the prostate](https://onco.cc/key-papers/paper-huggins-hodges-castration-serum-phosphatases-prostate-1941/), [Identification of human triple-negative breast cancer subtypes and preclinical models for selection of targeted therapies](https://onco.cc/key-papers/paper-lehmann-tnbc-subtypes-jci-2011/), [In vivo amplification of the androgen receptor gene and progression of human prostate cancer](https://onco.cc/key-papers/paper-visakorpi-androgen-receptor-amplification-nat-genet-1995/), [Integrative genomic profiling of human prostate cancer](https://onco.cc/key-papers/paper-taylor-integrative-genomic-profiling-cancer-cell-2010/), [IPATential150: ipatasertib plus abiraterone and prednisolone in metastatic castration-resistant prostate cancer](https://onco.cc/key-papers/paper-ipatential150-ipatasertib-abiraterone-pten-lancet-2021/), [Molecular determinants of resistance to antiandrogen therapy](https://onco.cc/key-papers/paper-chen-androgen-receptor-overexpression-antiandrogen-resistance-nat-med-2004/), [Molecular profiling stratifies diverse phenotypes of treatment-refractory metastatic castration-resistant prostate cancer](https://onco.cc/key-papers/paper-labrecque-mcrpc-phenotypes-jci-2019/), [Mutation of the androgen-receptor gene in metastatic androgen-independent prostate cancer](https://onco.cc/key-papers/paper-taplin-ar-mutation-androgen-independent-prostate-nejm-1995/), [Nuclear-localised androgen receptor splice variant 7 in circulating tumour cells as a predictive biomarker in castration-resistant prostate cancer](https://onco.cc/key-papers/paper-scher-nuclear-arv7-taxane-vs-arsi-jama-oncol-2018/), [Oncogenic genomic alterations, clinical phenotypes and outcomes in metastatic castration-sensitive prostate cancer](https://onco.cc/key-papers/paper-stopsack-mcspc-genomic-alterations-outcomes-ccr-2020/), [Phase 1 trial of abiraterone acetate confirms that castration-resistant prostate cancer commonly remains hormone driven](https://onco.cc/key-papers/paper-attard-abiraterone-phase-1-cyp17-jco-2008/), [Phase II trial of bicalutamide in patients with androgen receptor-positive, estrogen receptor-negative metastatic breast cancer](https://onco.cc/key-papers/paper-gucalp-bicalutamide-ar-positive-tbcrc011-ccr-2013/), [PREVAIL: enzalutamide in metastatic prostate cancer before chemotherapy](https://onco.cc/key-papers/paper-beer-prevail-enzalutamide-nejm-2014/), [PROPHECY: prospective multicentre validation of androgen receptor splice variant 7 and hormone therapy resistance in high-risk castration-resistant prostate cancer](https://onco.cc/key-papers/paper-prophecy-arv7-validation-jco-2019/), [Proposed morphologic classification of prostate cancer with neuroendocrine differentiation](https://onco.cc/key-papers/paper-epstein-neuroendocrine-prostate-morphologic-classification-ajsp-2014/), [Prospective comprehensive genomic profiling of 3,476 primary and metastatic prostate tumours](https://onco.cc/key-papers/paper-chung-comprehensive-genomic-profiling-prostate-jco-po-2019/), [Rb1 and Trp53 cooperate to suppress prostate cancer lineage plasticity, metastasis and antiandrogen resistance](https://onco.cc/key-papers/paper-ku-rb1-trp53-lineage-plasticity-science-2017/), [Reciprocal feedback regulation of PI3K and androgen receptor signalling in PTEN-deficient prostate cancer](https://onco.cc/key-papers/paper-carver-pi3k-ar-reciprocal-feedback-prostate-cancer-cell-2011/), [Recurrent fusion of TMPRSS2 and ETS transcription factor genes in prostate cancer](https://onco.cc/key-papers/paper-tomlins-tmprss2-ets-fusion-science-2005/), [Refinement of Triple-Negative Breast Cancer Molecular Subtypes: Implications for Neoadjuvant Chemotherapy Selection](https://onco.cc/key-papers/paper-lehmann-tnbctype-4-refinement-plos-one-2016/), [RESTORE: bipolar androgen therapy after progression on enzalutamide in metastatic castration-resistant prostate cancer](https://onco.cc/key-papers/paper-teply-restore-bipolar-androgen-therapy-lancet-oncol-2018/), [SOX2 promotes lineage plasticity and antiandrogen resistance in TP53- and RB1-deficient prostate cancer](https://onco.cc/key-papers/paper-mu-sox2-lineage-plasticity-science-2017/), [STAMPEDE: adding abiraterone to hormone therapy at diagnosis of advanced prostate cancer](https://onco.cc/key-papers/paper-stampede-abiraterone-nejm-2017/), [SU2C-PCF: integrative clinical genomics of advanced prostate cancer](https://onco.cc/key-papers/paper-robinson-integrative-clinical-genomics-advanced-prostate-cell-2015/), [Substantial interindividual and limited intraindividual genomic diversity among tumours from men with metastatic prostate cancer](https://onco.cc/key-papers/paper-kumar-interindividual-genomic-diversity-metastatic-prostate-nat-med-2016/), [TCGA: the molecular taxonomy of primary prostate cancer](https://onco.cc/key-papers/paper-tcga-molecular-taxonomy-primary-prostate-cell-2015/), [The evolutionary history of lethal metastatic prostate cancer](https://onco.cc/key-papers/paper-gundem-evolutionary-history-lethal-metastatic-prostate-nature-2015/), [The first PROTAC: a chimeric molecule that tags a protein for destruction](https://onco.cc/key-papers/paper-protac-concept-sakamoto-pnas-2001/), [The mutational landscape of lethal castration-resistant prostate cancer](https://onco.cc/key-papers/paper-grasso-mutational-landscape-lethal-crpc-nature-2012/), [TRANSFORMER: bipolar androgen therapy versus enzalutamide in asymptomatic metastatic castration-resistant prostate cancer](https://onco.cc/key-papers/paper-denmeade-transformer-bipolar-androgen-therapy-jco-2021/), [Unravelling triple-negative breast cancer molecular heterogeneity using an integrative multiomic analysis](https://onco.cc/key-papers/paper-bareche-tnbc-multiomic-heterogeneity-ann-oncol-2018/), [Whole-genome and transcriptome sequencing of prostate cancer identifies new genetic alterations driving disease progression](https://onco.cc/key-papers/paper-ren-chinese-prostate-whole-genome-eur-urol-2018/)
- roadmaps: [Triple-negative breast cancer roadmap: from a remainder defined by three negative tests to immunotherapy, antibody-drug conjugates and the residual disease problem](https://onco.cc/roadmaps/tnbc-roadmap/)
- ideas: [Destroy the truncated androgen receptor that hormone drugs cannot touch](https://onco.cc/ideas/idea-bio1-arv7-degrader/), [Take high-dose testosterone to phase 3, with progression-free survival through the second line as the primary endpoint](https://onco.cc/ideas/idea-prostate-bipolar-androgen-therapy-phase-3-on-pfs2/), [Watch for the cancer changing cell type before the biopsy says neuroendocrine, and act on it](https://onco.cc/ideas/idea-prostate-plasticity-surveillance-before-it-is-neuroendocrine/)
- trials: [AFFIRM](https://onco.cc/trials/affirm/), [ARMOR3-SV](https://onco.cc/trials/armor3-sv/), [CARD](https://onco.cc/trials/card/), [COU-AA-301](https://onco.cc/trials/cou-aa-301/), [COU-AA-302](https://onco.cc/trials/cou-aa-302/), [IMbassador250](https://onco.cc/trials/imbassador250/), [KEYNOTE-641](https://onco.cc/trials/keynote-641/), [KEYNOTE-991](https://onco.cc/trials/keynote-991/), [PEACE-3 (EORTC 1333)](https://onco.cc/trials/peace-3/), [PREVAIL](https://onco.cc/trials/prevail/)
- technologies: [Androgen deprivation & AR pathway inhibitors](https://onco.cc/technologies/androgen-deprivation/), [PROTACs & molecular glues (targeted protein degradation)](https://onco.cc/technologies/protac-degrader/)
- targets: [5-alpha-reductase type 2 (SRD5A2)](https://onco.cc/targets/srd5a2/), [CYP17A1 (17-alpha-hydroxylase/17,20-lyase)](https://onco.cc/targets/cyp17a1/)
- people: [Andrew J. Armstrong](https://onco.cc/people/andrew-armstrong/), [Charles L. Sawyers](https://onco.cc/people/charles-sawyers/), [Christopher J. Sweeney](https://onco.cc/people/christopher-sweeney/), [Eric J. Small](https://onco.cc/people/eric-small/), [Howard I. Scher](https://onco.cc/people/howard-scher/), [Johann de Bono](https://onco.cc/people/johann-de-bono/), [Karim Fizazi](https://onco.cc/people/karim-fizazi/), [Kim N. Chi](https://onco.cc/people/kim-chi/), [Maha Hussain](https://onco.cc/people/maha-hussain/), [Matthew R. Smith](https://onco.cc/people/matthew-smith/), [Neeraj Agarwal](https://onco.cc/people/neeraj-agarwal/), [Owen N. Witte](https://onco.cc/people/owen-witte/), [Rahul Aggarwal](https://onco.cc/people/rahul-aggarwal/), [Shaomeng Wang](https://onco.cc/people/shaomeng-wang/)
- collections: [Prostate Cancer Foundation (PCF)](https://onco.cc/collections/prostate-cancer-foundation/)
- institutions: [Sidney Kimmel Comprehensive Cancer Center at Jefferson Health](https://onco.cc/institutions/jefferson-kimmel/), [University of Chicago Medicine Comprehensive Cancer Center](https://onco.cc/institutions/uchicago-cancer/)

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