What are Androgen receptor antagonist drugs?

Androgen receptor antagonist drugs are pharmacologic agents that share a common mechanism (typically targeting Androgen receptor (AR)). 4 are currently marketed, with 23 more in clinical development.

What are the marketed Androgen receptor antagonist drugs?

Marketed Androgen receptor antagonist drugs include Darolutamide Oral Tablet, ODM-201 Tablet A, Zoladex and Casodex, Maximum androgen blockade.

Androgen receptor antagonist

Name: Drug Landscape Pharmaceutical Database
Creator: Drug Landscape
Published: 2026-01-01
License: https://creativecommons.org/licenses/by/4.0/

4 marketed 23 in Phase 3

This page covers all Androgen receptor antagonist drugs tracked by Drug Landscape: marketed products and active clinical-stage compounds, targeting Androgen receptor (AR), GnRH receptor (Zoladex); androgen receptor (Casodex), Androgen receptor; testosterone synthesis pathway.

Targets

Androgen receptor (AR) · GnRH receptor (Zoladex); androgen receptor (Casodex) · Androgen receptor; testosterone synthesis pathway · Androgen receptor (AR) and microtubule-associated proteins · Androgen receptor · Androgen receptor (AR) and CYP17A1 · CYP17A1 (abiraterone) / Androgen receptor (enzalutamide) · CYP17A1 (abiraterone); androgen receptor (enzalutamide); glucocorticoid receptor (prednisone) · Androgen receptor; testosterone/DHT synthesis (if abiraterone included) · GnRH receptor (goserelin); androgen receptor (bicalutamide)

Marketed (4)

Darolutamide Oral Tablet · Santa Chiara Hospital · Oncology
Darolutamide is an androgen receptor antagonist that blocks the binding of androgens to the androgen receptor, inhibiting androgen-driven prostate cancer cell growth.
ODM-201 Tablet A · Orion Corporation, Orion Pharma · Oncology
ODM-201 is an androgen receptor antagonist that blocks the binding of androgens to the androgen receptor, inhibiting androgen-driven prostate cancer cell growth.
Zoladex and Casodex · AstraZeneca · Oncology
Zoladex suppresses testosterone production via GnRH agonism, while Casodex blocks androgen receptors, together providing dual hormonal blockade for androgen-dependent cancers.
Maximum androgen blockade · Wonju Severance Christian Hospital · Oncology
Maximum androgen blockade combines androgen receptor antagonists with androgen synthesis inhibitors to suppress testosterone production and block its effects in prostate cancer cells.

Phase 3 pipeline (23)

Antiandrogen+docetaxel · Göteborg University · Oncology
This combination blocks androgen signaling while simultaneously disrupting microtubule dynamics to inhibit cancer cell proliferation and survival.
Proxalutamide (GT0918) · Suzhou Kintor Pharmaceutical Inc, · Oncology
Proxalutamide is an androgen receptor antagonist.
AEZS-130 (formerly ARD-07) · AEterna Zentaris · Oncology
AEZS-130 is a selective androgen receptor (AR) antagonist that blocks androgen signaling in hormone-sensitive cancers.
Enzalutamide, Abiraterone · Veru Inc. · Oncology
This combination of an androgen receptor antagonist (enzalutamide) and a CYP17A1 inhibitor (abiraterone) blocks testosterone production and androgen signaling to treat hormone-sensitive prostate cancer.
Apalutamide Oral Tablet · Santa Chiara Hospital · Oncology
Apalutamide is an androgen receptor inhibitor that blocks the binding and nuclear translocation of androgens, preventing androgen-driven prostate cancer cell growth.
Abiraterone Acetate or Enzalutamide · National Cancer Institute, Naples · Oncology
Abiraterone acetate inhibits CYP17A1 to block androgen synthesis, while enzalutamide antagonizes the androgen receptor, both reducing androgen-driven prostate cancer growth.
Darolutamide continuous · The First Affiliated Hospital with Nanjing Medical University · Oncology
Darolutamide is an androgen receptor antagonist that blocks the binding of androgens to the androgen receptor, inhibiting androgen-driven prostate cancer cell growth.
Placebo with enzalutamide · Pfizer · Oncology
Enzalutamide is an androgen receptor inhibitor that blocks the binding and nuclear translocation of androgens, thereby suppressing androgen-driven prostate cancer cell growth.
Abiraterone with Prednisone or Enzalutamide · Curium US LLC · Oncology
Abiraterone inhibits CYP17A1 to block androgen synthesis, while enzalutamide antagonizes the androgen receptor, together suppressing testosterone-driven prostate cancer growth; prednisone provides glucocorticoid support to mitigate mineralocorticoid excess from abiraterone.
Antiandrogen Therapy · M.D. Anderson Cancer Center · Oncology
Antiandrogen therapy blocks the effects of androgens (male hormones) by inhibiting androgen receptor signaling, thereby slowing or stopping the growth of androgen-dependent cancer cells.
Androgen blockade + radiation therapy · Université de Sherbrooke · Oncology
Androgen blockade suppresses testosterone-driven prostate cancer cell growth, while radiation therapy delivers targeted cytotoxic damage to tumor cells.
Clascoterone 5% solution · Cassiopea SpA · Dermatology
Clascoterone is an androgen receptor antagonist that blocks androgen signaling in skin to reduce sebum production and acne lesions.
ADT+second-generation antiandrogens ± chemotherapy · The First Affiliated Hospital with Nanjing Medical University · Oncology
This combination suppresses androgen production and blocks androgen receptor signaling in prostate cancer cells, with optional chemotherapy to enhance cytotoxic effects.
Conventional NSAA · University of Sydney · Oncology
Conventional NSAA (non-selective androgen antagonist) blocks androgen receptor signaling to suppress testosterone-driven prostate cancer growth.
KX-826-（5%） BID · Suzhou Kintor Pharmaceutical Inc, · Dermatology
KX-826 is a topical androgen receptor antagonist that inhibits DHT-mediated signaling in hair follicles to treat androgenetic alopecia.
Enzalutamide capsule · CHU de Quebec-Universite Laval · Oncology
Enzalutamide is an androgen receptor inhibitor that blocks the binding and nuclear translocation of androgens, preventing androgen-driven gene transcription in prostate cancer cells.
Goserelin plus Bicalutamide · Speciality European Pharma Limited · Oncology
Goserelin suppresses testosterone production via GnRH receptor agonism, while bicalutamide blocks androgen receptor signaling, providing dual hormonal suppression for androgen-dependent cancers.
CB-03-01 cream, 1% · Cassiopea SpA · Dermatology
CB-03-01 is an androgen receptor antagonist that blocks the effects of androgens in the skin to reduce sebum production and inflammation associated with acne.
Androgen receptor targeted therapy · Universitaire Ziekenhuizen KU Leuven · Oncology
This therapy targets the androgen receptor to modulate hormone-dependent signaling pathways, typically used in hormone-sensitive cancers.
Darolutamide (BAY 1841788) · Canadian Cancer Trials Group · Oncology
Darolutamide is a non-steroidal androgen receptor inhibitor that blocks androgen signaling in prostate cancer cells.
Enzalutamide Soft Capsules · Jiangsu HengRui Medicine Co., Ltd. · Oncology
Enzalutamide is an androgen receptor inhibitor that blocks the binding and nuclear translocation of androgens, preventing androgen-driven gene transcription in prostate cancer cells.
Darolutamide intermittent · The First Affiliated Hospital with Nanjing Medical University · Oncology
Darolutamide is an androgen receptor antagonist that blocks the binding of androgens to the androgen receptor, inhibiting prostate cancer cell growth and survival.
Placebo plus enzalutamide · Pfizer · Oncology
Enzalutamide is an androgen receptor inhibitor that blocks the binding and nuclear translocation of androgens, thereby suppressing androgen-driven prostate cancer cell growth.