{"entity":{"id":"androgen-receptor","kind":"target","name":"Androgen receptor","aka":[],"tldr":"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).","asOf":"2026-09-04","wikipedia":"https://en.wikipedia.org/wiki/Androgen_receptor","links":[{"label":"Wikipedia","url":"https://en.wikipedia.org/wiki/Androgen_receptor"}],"tags":["hormonal"],"related":["ar-v7-splice-variant"],"cancers":["prostate","tnbc"],"sections":[],"technologies":[],"targets":[],"drugs":["nilutamide","triptorelin","bms-986365","azd9750","ep0062","qlh12016"],"companies":["oric-pharmaceuticals"],"institutions":[],"pathways":["ar-signaling","prostate-cancer-signalling"],"terms":["pam50"],"trials":[],"people":[],"bottlenecks":[],"keyPapers":["paper-lehmann-tnbctype-4-refinement-plos-one-2016","paper-bareche-tnbc-multiomic-heterogeneity-ann-oncol-2018","paper-gucalp-bicalutamide-ar-positive-tbcrc011-ccr-2013","paper-traina-enzalutamide-ar-tnbc-jco-2018","paper-visakorpi-androgen-receptor-amplification-nat-genet-1995","paper-quigley-structural-variation-mcrpc-cell-2018","paper-abida-genomic-correlates-outcome-mcrpc-pnas-2019","paper-tukachinsky-ctdna-3334-advanced-prostate-ccr-2021"],"journals":[],"dependsOn":[],"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)."],"symbol":"AR","role":[],"sources":[],"specificity":"tumour-associated","distribution":"few-types","specificityNote":"Tumour-associated overexpression: HPA finds the RNA cancer enhanced in cancer (Breast Invasive Carcinoma (TCGA), Prostate Adenocarcinoma (TCGA)) and tissue enhanced in normal liver, so the tumour and the normal tissue it comes from share the target and the medicine relies on the difference in level. HPA AR: RNA tissue enhanced (liver 36 nTPM); high antibody staining in 2 normal tissues; highest cancer staining prostate cancer (7 of 8 high). Distribution: 2 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Prostate cancer, Breast cancer (all types)); approvals of single-target medicines aimed at it also list Salivary gland cancers, not counted; Open Targets associates it with 5 specific cancer types at or above 0.5 (prostate cancer, prostate carcinoma, prostate adenocarcinoma, Familial prostate cancer, breast cancer). (Rule 7 of scripts/fetch-target-specificity.ts.)","specificitySources":[{"label":"Human Protein Atlas AR tissue","url":"https://www.proteinatlas.org/ENSG00000169083-AR/tissue","note":"RNA tissue and blood lineage specificity, normal tissue antibody staining (version 25.1, CC BY-SA 3.0)"},{"label":"Human Protein Atlas AR pathology","url":"https://www.proteinatlas.org/ENSG00000169083-AR/pathology","note":"patients per staining level per cancer type (version 25.1, CC BY-SA 3.0)"},{"label":"Open Targets ENSG00000169083 associations","url":"https://platform.opentargets.org/target/ENSG00000169083/associations","note":"cancer associations at or above 0.5 (CC0)"}],"hgnc":"HGNC:644","ensembl":"ENSG00000169083","uniprot":"P10275","entrez":"367","firstDescribed":1988,"firstDescribedBasis":"sequence","firstDescribedNote":"Earliest sequence paper UniProt cites for the protein: Lubahn D.B. et al, Mol. Endocrinol, 1988, \"The human androgen receptor: complementary deoxyribonucleic acid cloning, sequence analysis and gene expression in prostate\".","firstDescribedSource":"https://pubmed.ncbi.nlm.nih.gov/3216866/","biology":"Nuclear receptor; amplification, splice variants (AR-V7), and ligand-binding-domain mutations drive resistance.","whereFound":["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"],"targetClass":"nuclear-receptor","prevalence":[{"cancerId":"prostate","pct":">95","measure":"AR-driven at diagnosis","source":"https://en.wikipedia.org/wiki/Androgen_receptor","note":"AR-V7 in ~20-40% of mCRPC"},{"cancerId":"tnbc","pct":"10-15","measure":"Luminal androgen receptor subtype","source":"https://en.wikipedia.org/wiki/Androgen_receptor"},{"cancerId":"tnbc","pct":"12-16","measure":"AR expression and luminal androgen receptor subtype","source":"https://doi.org/10.1371/journal.pone.0157368","note":"LAR was 16% of tumours by TNBCtype-4 and 9% by the original six-subtype call (Lehmann 2016); 77 of 485 classifiable TNBCs, 16%, with 92% of LAR patients aged 45 or over (Bareche 2018); AR nuclear staining above 10% in 12% of 424 ER/PR-negative patients screened for TBCRC 011 (Gucalp 2013); 78 of 118 enrolled enzalutamide patients had 10% or more nuclear AR (Traina 2018). AR mutation is rare: 2 of 123 in brca_tcga_pan_can_atlas_2018 (cBioPortal)."},{"cancerId":"prostate","pct":"1-57","measure":"High-level amplification of the gene, and of an upstream enhancer","source":"https://www.cbioportal.org/study/summary?id=prad_tcga_pan_can_atlas_2018","note":"cBioPortal high-level amplification: 5 of 489, 1.0%, in prad_tcga_pan_can_atlas_2018; 17 of 424, 4.0%, in prad_mcspc_mskcc_2020; 237 of 2,260, 10.5%, in prostate_msk_2024; 9 of 82, 11.0%, in the patient-contributed mpcproject_broad_2021; 217 of 444, 48.9%, in prad_su2c_2019; 78 of 150, 52.0%, in prad_su2c_2015; 85 of 149, 57.0%, in prad_fhcrc. High-level amplification of Xq11-q13 was found in 7 of 23 tumours recurring on androgen deprivation and none of the pre-treatment specimens from the same men (Visakorpi 1995); the upstream enhancer is amplified in 81% of 101 deeply sequenced castration-resistant genomes (Quigley 2018)."},{"cancerId":"prostate","pct":"0.4-18","measure":"L702H, W742C/L, H875Y, T878A, F877L","source":"https://www.cbioportal.org/study/summary?id=prad_su2c_2019","note":"cBioPortal samples with any AR mutation: 61 of 444, 13.7%, in prad_su2c_2019; 27 of 150, 18.0%, in prad_su2c_2015; 93 of 2,260, 4.1%, in prostate_msk_2024; 9 of 424, 2.1%, in prad_mcspc_mskcc_2020; 2 of 494, 0.4%, in prad_tcga_pan_can_atlas_2018. Allele records in prad_su2c_2019, 72 records: L702H 17, T878A 15, H875Y 11, W742C 8, W742L 4, F877L 3."}]},"route":"/targets/androgen-receptor/","neighbours":{"biomarker":[{"id":"ar-amplification","kind":"biomarker","name":"AR amplification (gene and upstream enhancer)","route":"/biomarkers/ar-amplification/"},{"id":"ar-ligand-binding-domain-mutation","kind":"biomarker","name":"AR ligand-binding-domain mutation (L702H, W742C, H875Y, T878A, F877L)","route":"/biomarkers/ar-ligand-binding-domain-mutation/"},{"id":"ar-v7-splice-variant","kind":"biomarker","name":"AR-V7 splice variant","route":"/biomarkers/ar-v7-splice-variant/"},{"id":"ctdna-tumour-fraction","kind":"biomarker","name":"Circulating tumour DNA fraction (and what a negative plasma result means)","route":"/biomarkers/ctdna-tumour-fraction/"},{"id":"spop-mutation","kind":"biomarker","name":"SPOP mutation","route":"/biomarkers/spop-mutation/"},{"id":"tmprss2-erg-fusion","kind":"biomarker","name":"TMPRSS2-ERG fusion (and the other ETS rearrangements)","route":"/biomarkers/tmprss2-erg-fusion/"},{"id":"nepc-transformation","kind":"biomarker","name":"Treatment-emergent neuroendocrine transformation (recognising it)","route":"/biomarkers/nepc-transformation/"}],"cancer":[{"id":"apocrine-carcinoma-breast","kind":"cancer","name":"Apocrine carcinoma of the breast","route":"/cancers/apocrine-carcinoma-breast/"},{"id":"tnbc-luminal-androgen-receptor","kind":"cancer","name":"Luminal androgen receptor triple-negative breast cancer (LAR)","route":"/cancers/tnbc-luminal-androgen-receptor/"},{"id":"prostate","kind":"cancer","name":"Prostate cancer","route":"/cancers/prostate/"},{"id":"salivary-gland","kind":"cancer","name":"Salivary gland cancers","route":"/cancers/salivary-gland/"},{"id":"tnbc","kind":"cancer","name":"Triple-negative breast cancer (TNBC)","route":"/cancers/tnbc/"}],"drug":[{"id":"abiraterone","kind":"drug","name":"Abiraterone acetate","route":"/drugs/abiraterone/"},{"id":"apalutamide","kind":"drug","name":"Apalutamide","route":"/drugs/apalutamide/"},{"id":"azd9750","kind":"drug","name":"AZD9750","route":"/drugs/azd9750/"},{"id":"bicalutamide","kind":"drug","name":"Bicalutamide","route":"/drugs/bicalutamide/"},{"id":"bms-986365","kind":"drug","name":"BMS-986365","route":"/drugs/bms-986365/"},{"id":"darolutamide","kind":"drug","name":"Darolutamide","route":"/drugs/darolutamide/"},{"id":"degarelix","kind":"drug","name":"Degarelix","route":"/drugs/degarelix/"},{"id":"enzalutamide","kind":"drug","name":"Enzalutamide","route":"/drugs/enzalutamide/"},{"id":"ep0062","kind":"drug","name":"EP0062","route":"/drugs/ep0062/"},{"id":"fluoxymesterone","kind":"drug","name":"Fluoxymesterone","route":"/drugs/fluoxymesterone/"},{"id":"flutamide","kind":"drug","name":"Flutamide","route":"/drugs/flutamide/"},{"id":"galeterone","kind":"drug","name":"Galeterone","route":"/drugs/galeterone/"},{"id":"leuprolide","kind":"drug","name":"Leuprolide (leuprorelin) and GnRH agonists","route":"/drugs/leuprolide/"},{"id":"masofaniten","kind":"drug","name":"Masofaniten","route":"/drugs/masofaniten/"},{"id":"mevrometostat","kind":"drug","name":"Mevrometostat","route":"/drugs/mevrometostat/"},{"id":"nilutamide","kind":"drug","name":"Nilutamide","route":"/drugs/nilutamide/"},{"id":"qlh12016","kind":"drug","name":"QLH12016","route":"/drugs/qlh12016/"},{"id":"rezvilutamide","kind":"drug","name":"Rezvilutamide","route":"/drugs/rezvilutamide/"},{"id":"triptorelin","kind":"drug","name":"Triptorelin","route":"/drugs/triptorelin/"}],"company":[{"id":"monte-rosa","kind":"company","name":"Monte Rosa Therapeutics","route":"/companies/monte-rosa/"},{"id":"oric-pharmaceuticals","kind":"company","name":"ORIC Pharmaceuticals","route":"/companies/oric-pharmaceuticals/"},{"id":"veru","kind":"company","name":"Veru","route":"/companies/veru/"}],"pathway":[{"id":"ar-signaling","kind":"pathway","name":"Androgen receptor signalling","route":"/pathways/ar-signaling/"},{"id":"chemical-carcinogenesis-receptor-activation","kind":"pathway","name":"Chemical carcinogenesis - receptor activation","route":"/pathways/chemical-carcinogenesis-receptor-activation/"},{"id":"lineage-plasticity-neuroendocrine","kind":"pathway","name":"Lineage plasticity & neuroendocrine transformation","route":"/pathways/lineage-plasticity-neuroendocrine/"},{"id":"prostate-cancer-signalling","kind":"pathway","name":"Prostate cancer (KEGG map)","route":"/pathways/prostate-cancer-signalling/"},{"id":"resistance-routes-map","kind":"pathway","name":"Resistance routes: how a blocked pathway comes back","route":"/pathways/resistance-routes-map/"},{"id":"rna-splicing","kind":"pathway","name":"RNA splicing","route":"/pathways/rna-splicing/"},{"id":"transcription-addiction","kind":"pathway","name":"Transcriptional machinery & addiction","route":"/pathways/transcription-addiction/"},{"id":"ubiquitin-proteasome-system","kind":"pathway","name":"Ubiquitin-proteasome system & protein homeostasis","route":"/pathways/ubiquitin-proteasome-system/"}],"term":[{"id":"agonist-antagonist","kind":"term","name":"Agonist and antagonist","route":"/terms/agonist-antagonist/"},{"id":"arpi","kind":"term","name":"Androgen receptor pathway inhibitor (ARPI)","route":"/terms/arpi/"},{"id":"androgen-receptor-positive-tnbc","kind":"term","name":"Androgen receptor-positive triple-negative breast cancer","route":"/terms/androgen-receptor-positive-tnbc/"},{"id":"ar-v7","kind":"term","name":"AR-V7 splice variant","route":"/terms/ar-v7/"},{"id":"bipolar-androgen-therapy","kind":"term","name":"Bipolar androgen therapy (BAT)","route":"/terms/bipolar-androgen-therapy/"},{"id":"hormone-therapy","kind":"term","name":"Hormone therapy","route":"/terms/hormone-therapy/"},{"id":"intermittent-androgen-deprivation","kind":"term","name":"Intermittent androgen deprivation (IAD)","route":"/terms/intermittent-androgen-deprivation/"},{"id":"luminal-androgen-receptor","kind":"term","name":"Luminal androgen receptor (LAR) subtype","route":"/terms/luminal-androgen-receptor/"},{"id":"mcrpc-mhspc","kind":"term","name":"mCRPC and mHSPC (castration-resistant vs hormone-sensitive prostate cancer)","route":"/terms/mcrpc-mhspc/"},{"id":"neuroendocrine-differentiation","kind":"term","name":"Neuroendocrine differentiation in prostate cancer","route":"/terms/neuroendocrine-differentiation/"},{"id":"pam50","kind":"term","name":"PAM50 / intrinsic subtypes","route":"/terms/pam50/"},{"id":"receptor","kind":"term","name":"Receptor","route":"/terms/receptor/"}],"paper":[{"id":"paper-abiraterone-acetate-prostate-n-engl-j-med-2013","kind":"paper","name":"Abiraterone in metastatic prostate cancer without previous 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