Androgen receptor (AR)

Predictive

Supports Resistance

accepted

EID9547

This multicenter clinical trial study (PROPHECY) enrolled 118 patients with metastatic castration-resistant prostate cancers (CRPC) on Abiraterone or Enzalutamide treatment. The Johns Hopkins Universi… (full text at CIViC)

PMID 30865549 · Armstrong et al., 2019 · Open in CIViC

〃

Predictive

Supports Resistance

accepted

EID12463

A cross-sectional cohort study was performed in 161 men with metastatic prostate cancer undergoing a change in treatment to determine if pre-therapy AR-V7 nuclear protein expression in circulating tum… (full text at CIViC)

PMID 27262168 · Scher et al., 2016 · Open in CIViC

〃

Predictive

Supports Resistance

accepted

EID12464

A blinded, multi-institutional cohort study was performed in 142 men with metastatic, castration-resistant prostate cancer to determine if pre-therapy nuclear-localized expression of AR-V7 protein in … (full text at CIViC)

PMID 29955787 · Scher et al., 2018 · Open in CIViC

Abiraterone + EnzalutamideSubstitutes

Predictive

Supports Resistance

accepted

EID863

This prospective study enrolled 31 Enzalutamide-treated (group 1) and 31 Abiraterone-treated (group 2) patients with metastatic castration-resistant prostate cancers (CRPC). AR-V7 variant was detected… (full text at CIViC)

PMID 25184630 · Antonarakis et al., 2014 · Open in CIViC

AR Mutation1
Bicalutamide + Cyproterone Acetate + Flutamide + NilutamideSubstitutes	Malignant Prostate Neoplasm	Predictive	B	Supports Resistance	4	accepted	EID1521 In a study of 150 patients with metastatic castration resistant prostate cancer (mCRPC), 71.3% of cases (n=107) harbored androgen receptor (AR) pathway aberrations. Within the AR mutation cohort, 78… (full text at CIViC) PMID 26000489 · Robinson et al., 2015 · Open in CIViC	civic

AR Mutation1

Bicalutamide + Cyproterone Acetate + Flutamide + NilutamideSubstitutes

Predictive

Supports Resistance

accepted

EID1521

In a study of 150 patients with metastatic castration resistant prostate cancer (mCRPC), 71.3% of cases (n=107) harbored androgen receptor (AR) pathway aberrations. Within the AR mutation cohort, 78… (full text at CIViC)

PMID 26000489 · Robinson et al., 2015 · Open in CIViC

AR F877L1
Apalutamide + EnzalutamideSubstitutes	Malignant Prostate Neoplasm	Predictive	D	Supports Resistance	4	accepted	EID447 Mutations F876L in the ligand binding domain of the androgen receptor confered resistance to enzalutamide and ARN-509, causing these compounds to function as partial agonists in two prostate cancer ce… (full text at CIViC) PMID 23779130 · Joseph et al., 2013 · Open in CIViC	civic

AR F877L1

Apalutamide + EnzalutamideSubstitutes

Predictive

Supports Resistance

accepted

EID447

Mutations F876L in the ligand binding domain of the androgen receptor confered resistance to enzalutamide and ARN-509, causing these compounds to function as partial agonists in two prostate cancer ce… (full text at CIViC)

PMID 23779130 · Joseph et al., 2013 · Open in CIViC

AR W7421
Bicalutamide	Prostate Carcinoma	Predictive	D	Supports Resistance	4	accepted	EID448 LNCaP-FGC cells with mutations at codon 741 (W741C, W741L) were able to use bicalutamide as an AR agonist, promoting cell growth and increased prostate-specific antigen secretion. PMID 12517791 · Hara et al., 2003 · Open in CIViC	civic

AR W7421

Bicalutamide

Prostate Carcinoma

Predictive

Supports Resistance

accepted

EID448

LNCaP-FGC cells with mutations at codon 741 (W741C, W741L) were able to use bicalutamide as an AR agonist, promoting cell growth and increased prostate-specific antigen secretion.

PMID 12517791 · Hara et al., 2003 · Open in CIViC

Drug	Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
Abiraterone	EU EMA	Castration-Resistant Prostate Carcinoma	Abiraterone Accord is indicated with prednisone or prednisolone for: the treatment of newly diagnosed high risk metastatic hormone sensitive prostate cancer (mHSPC) in adult men in combination with androgen deprivation therapy (ADT) the treatment of metastatic castration resistant prostate cancer (mCRPC) in adult men who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy in whom chemotherapy is not yet clinically indicated the treatment of mCRPC in adult men whose disease has progressed on or after a docetaxel based chemotherapy regimen.	approved	Apr 26, 2021	ema
Abiraterone	EU EMA	Castration-Resistant Prostate Carcinoma	Zytiga is indicated with prednisone or prednisolone for: the treatment of metastatic castration resistant prostate cancer in adult men who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy in whom chemotherapy is not yet clinically indicated the treatment of metastatic castration resistant prostate cancer in adult men whose disease has progressed on or after a docetaxel based chemotherapy regimen.accelerated	approved	Sep 5, 2011	ema
Abiraterone	US FDA	—	Efficacy supplement 2019-06-03 (see label)	approved	Jun 3, 2019	openfda
Abiraterone	US FDA	Castration-Resistant Prostate Carcinoma	Abiraterone Acetate is indicated in combination with methylprednisolone for the treatment of patients with metastatic castration-resistant prostate cancer. Abiraterone Acetate is a CYP17 inhibitor indicated in combination with methylprednisolone for the treatment of patients with metastatic castration-resistant prostate cancer (CRPC). ( 1 )	approved	May 22, 2018	openfda
Abiraterone	US FDA	—	Efficacy supplement 2018-02-07 (see label)	approved	Feb 7, 2018	openfda
Abiraterone	US FDA	—	Efficacy supplement 2015-03-20 (see label)	approved	Mar 20, 2015	openfda
Abiraterone	US FDA	—	Efficacy supplement 2012-12-10 (see label)	approved	Dec 10, 2012	openfda
Abiraterone	US FDA	—	ZYTIGA is indicated in combination with prednisone for the treatment of patients with Metastatic castration-resistant prostate cancer (CRPC) Metastatic high-risk castration-sensitive prostate cancer (CSPC) ZYTIGA is a CYP17 inhibitor indicated in combination with prednisone for the treatment of patients with metastatic castration-resistant prostate cancer (CRPC). ( 1 ) metastatic high-risk castration-sensitive prostate cancer (CSPC). ( 1 )	approved	Apr 28, 2011	openfda
Apalutamide	CA Health Canada	—	Marketed in Canada as ERLEADA (DIN 02540185) under ATC L02BB05 APALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Nov 1, 2023	health-canada-dpd
Apalutamide	CA Health Canada	—	Marketed in Canada as ERLEADA (DIN 02478374) under ATC L02BB05 APALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Jul 27, 2018	health-canada-dpd
Apalutamide	EU EMA	Nonmetastatic Castration-Resistant Prostate Carcinoma	Erleada is indicated: in adult men for the treatment of non metastatic castration resistant prostate cancer (nmCRPC) who are at high risk of developing metastatic disease. in adult men for the treatment of metastatic hormone-sensitive prostate cancer (mHSPC) in combination with androgen deprivation therapy (ADT).	approved	Jan 14, 2019	ema
Apalutamide	US FDA	—	Efficacy supplement 2023-12-19 (see label)	approved	Dec 19, 2023	openfda
Apalutamide	US FDA	—	Efficacy supplement 2021-09-07 (see label)	approved	Sep 7, 2021	openfda
Apalutamide	US FDA	—	Efficacy supplement 2020-11-20 (see label)	approved	Nov 20, 2020	openfda
Apalutamide	US FDA	—	Efficacy supplement 2019-09-17 (see label)	approved	Sep 17, 2019	openfda
Apalutamide	US FDA	Nonmetastatic Castration-Resistant Prostate Carcinoma	ERLEADA is indicated for the treatment of patients with Metastatic castration-sensitive prostate cancer (mCSPC) Non-metastatic castration-resistant prostate cancer (nmCRPC) ERLEADA is an androgen receptor inhibitor indicated for the treatment of patients with metastatic castration-sensitive prostate cancer. ( 1 ) non-metastatic castration-resistant prostate cancer. ( 1 )	approved	Feb 14, 2018	openfda
Bicalutamide	CA Health Canada	—	Marketed in Canada as BICALUTAMIDE (DIN 02519178) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Apr 28, 2022	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as VAN-BICALUTAMIDE (DIN 02428709) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Post Marketsince Aug 7, 2019	Jun 22, 2015	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as RAN-BICALUTAMIDE (DIN 02371324) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Post Marketsince Aug 23, 2022	Sep 7, 2012	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as BICALUTAMIDE (DIN 02382423) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Post Marketsince Jan 22, 2020	Jun 10, 2012	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as AVA-BICALUTAMIDE (DIN 02360993) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Post Marketsince Aug 21, 2014	Nov 23, 2011	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as JAMP BICALUTAMIDE (DIN 02357216) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Oct 21, 2010	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as ACH-BICALUTAMIDE (DIN 02325985) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	May 5, 2010	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as BICALUTAMIDE (DIN 02325233) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Post Marketsince Jun 20, 2014	Jun 22, 2009	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as PRO-BICALUTAMIDE (DIN 02311038) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Jul 9, 2008	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as DOM-BICALUTAMIDE (DIN 02281139) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Post Marketsince May 9, 2025	Apr 16, 2008	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as MYLAN-BICALUTAMIDE (DIN 02302403) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Post Marketsince Jan 9, 2017	Dec 20, 2007	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as APO-BICALUTAMIDE (DIN 02296063) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Dormantsince May 14, 2023	Nov 5, 2007	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as PHL-BICALUTAMIDE (DIN 02281163) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Post Marketsince Jul 21, 2006	Jul 21, 2006	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as RATIO-BICALUTAMIDE (DIN 02277700) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Post Marketsince Sep 19, 2014	Mar 13, 2006	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as TEVA-BICALUTAMIDE (DIN 02270226) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Feb 10, 2006	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as PMS-BICALUTAMIDE (DIN 02275589) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Feb 8, 2006	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as SANDOZ BICALUTAMIDE (DIN 02276089) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Post Marketsince Aug 1, 2019	Feb 8, 2006	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as ACT BICALUTAMIDE (DIN 02274337) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Post Marketsince Jul 11, 2018	Feb 7, 2006	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as CASODEX (DIN 02184478) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Post Marketsince Mar 7, 2025	Dec 31, 1996	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as NTP-BICALUTAMIDE (DIN 02358557) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Pre Marketsince Aug 6, 2015	—	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as NU-BICALUTAMIDE (DIN 02336545) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled (Unreturned Annual)since Mar 28, 2018	—	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as NRA-BICALUTAMIDE (DIN 02565919) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approved	—	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as MED-BICALUTAMIDE (DIN 02407531) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approved	—	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as AG-BICALUTAMIDE (DIN 02374412) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Pre Marketsince Jul 14, 2026	—	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as ACCEL-BICALUTAMIDE TABLETS USP (DIN 02400731) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Pre Marketsince May 19, 2017	—	health-canada-dpd
Bicalutamide	CA Health Canada	—	Marketed in Canada as BICALUTAMIDE TABLETS (DIN 02360098) under ATC L02BB03 BICALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	withdrawnsource: Cancelled Pre Marketsince Mar 10, 2023	—	health-canada-dpd
Bicalutamide	US FDA	—	Efficacy supplement 1997-12-12 (see label)	approved	Dec 12, 1997	openfda
Bicalutamide	US FDA	Prostate Carcinoma	1. INDICATIONS AND USAGE Bicalutamide tablets 50 mg daily is indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog for the treatment of Stage D 2 metastatic carcinoma of the prostate. Bicalutamide tablets 150 mg daily is not approved for use alone or with other treatments [see Clinical Studies (14.2) ]. Bicalutamide tablets 50 mg is an androgen receptor inhibitor indicated for use in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analog for the treatment of Stage D 2 metastatic carcinoma of the prostate. (1) Bicalutamide tablets 150 mg daily is not approved for use alone or with other treatments. (1)	approved	Oct 4, 1995	openfda
Enzalutamide	CA Health Canada	—	Marketed in Canada as AURO-ENZALUTAMIDE (DIN 02494736) under ATC L02BB04 ENZALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Mar 30, 2026	health-canada-dpd
Enzalutamide	CA Health Canada	—	Marketed in Canada as REDDY-ENZALUTAMIDE (DIN 02558424) under ATC L02BB04 ENZALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Mar 30, 2026	health-canada-dpd
Enzalutamide	CA Health Canada	—	Marketed in Canada as APO-ENZALUTAMIDE (DIN 02562677) under ATC L02BB04 ENZALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Mar 30, 2026	health-canada-dpd
Enzalutamide	CA Health Canada	—	Marketed in Canada as JAMP ENZALUTAMIDE (DIN 02515229) under ATC L02BB04 ENZALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Feb 20, 2026	health-canada-dpd
Enzalutamide	CA Health Canada	—	Marketed in Canada as XTANDI (DIN 02407329) under ATC L02BB04 ENZALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Jun 7, 2013	health-canada-dpd
Enzalutamide	CA Health Canada	—	Marketed in Canada as PRO-ENZALUTAMIDE (DIN 02569124) under ATC L02BB04 ENZALUTAMIDE. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approved	—	health-canada-dpd

Drug

Jurisdiction · authority

Cancer

Indication

Status

Approval date

Source

Castration-Resistant Prostate Carcinoma

EU EMA

Abiraterone Accord is indicated with prednisone or prednisolone for: the treatment of newly diagnosed high risk metastatic hormone sensitive prostate cancer (mHSPC) in adult men in combination with androgen deprivation therapy (ADT) the treatment of metastatic castration resistant prostate cancer (mCRPC) in adult men who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy in whom chemotherapy is not yet clinically indicated the treatment of mCRPC in adult men whose disease has progressed on or after a docetaxel based chemotherapy regimen.

approved

Apr 26, 2021

ema

Castration-Resistant Prostate Carcinoma

EU EMA

Zytiga is indicated with prednisone or prednisolone for: the treatment of metastatic castration resistant prostate cancer in adult men who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy in whom chemotherapy is not yet clinically indicated the treatment of metastatic castration resistant prostate cancer in adult men whose disease has progressed on or after a docetaxel based chemotherapy regimen.accelerated

approved

Sep 5, 2011

ema

US FDA

—

Efficacy supplement 2019-06-03 (see label)

approved

Jun 3, 2019

Castration-Resistant Prostate Carcinoma

US FDA

Abiraterone Acetate is indicated in combination with methylprednisolone for the treatment of patients with metastatic castration-resistant prostate cancer. Abiraterone Acetate is a CYP17 inhibitor indicated in combination with methylprednisolone for the treatment of patients with metastatic castration-resistant prostate cancer (CRPC). ( 1 )

approved

May 22, 2018

US FDA

—

Efficacy supplement 2018-02-07 (see label)

approved

Feb 7, 2018

US FDA

—

Efficacy supplement 2015-03-20 (see label)

approved

Mar 20, 2015

US FDA

—

Efficacy supplement 2012-12-10 (see label)

approved

Dec 10, 2012

US FDA

—

ZYTIGA is indicated in combination with prednisone for the treatment of patients with Metastatic castration-resistant prostate cancer (CRPC) Metastatic high-risk castration-sensitive prostate cancer (CSPC) ZYTIGA is a CYP17 inhibitor indicated in combination with prednisone for the treatment of patients with metastatic castration-resistant prostate cancer (CRPC). ( 1 ) metastatic high-risk castration-sensitive prostate cancer (CSPC). ( 1 )

approved

Apr 28, 2011