Last update 01 Nov 2024

AR Positive/ER Positive Breast Cancer

Last update 01 Nov 2024

Basic Info

Synonyms-

Introduction-

Drugs associated with AR Positive/ER Positive Breast Cancer

Enobosarm

Target

Mechanism

AR agonists

Active Org.

Veru, Inc.

Originator Org.

GTx, Inc.

Active Indication

Obesity [+1]

Inactive Indication

Advanced Triple-Negative Breast Carcinoma [+13]

Drug Highest PhasePhase 2

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with AR Positive/ER Positive Breast Cancer

EUCTR2015-001012-35-LT / Not yet recruitingPhase 2

A Phase 2 Open Label, Multi-Center, Multinational, Randomized, Parallel Design Study Investigating The Efficacy and Safety Of GTx-024 On Metastatic or Locally Advanced ER+/AR+ Breast Cancer (BC) in Postmenopausal Women - N/A

Start Date30 Sep 2015

Sponsor / Collaborator

GTx, Inc.

NCT02463032 / CompletedPhase 2

The purpose of this study is to determine if GTx-024 at different dosages (9 mg or 18 mg) is effective and safe in the treatment of patients with metastatic or locally advanced Estrogen Receptor (ER)+ and Androgen Receptor (AR)+ breast cancer in postmenopausal women.

Start Date01 Aug 2015

Sponsor / Collaborator

GTx, Inc.

NCT00972023 / TerminatedPhase 1IIT

A Pilot Study of Androgen Receptor as a Target for the Treatment of ER-/PR-/AR + Breast Cancer

RATIONALE: Dehydroepiandrosterone (DHEA) may slow the growth of tumor cells and be an effective treatment for women with breast cancer.
PURPOSE: This phase I trial is studying how well DHEA works in treating women undergoing surgery for stage I, stage II, or stage III breast cancer.

Start Date01 Feb 2010

Sponsor / Collaborator

Barbara Ann Karmanos Cancer Institute

[+1]

100 Clinical Results associated with AR Positive/ER Positive Breast Cancer

100 Translational Medicine associated with AR Positive/ER Positive Breast Cancer

0 Patents (Medical) associated with AR Positive/ER Positive Breast Cancer

Literatures (Medical) associated with AR Positive/ER Positive Breast Cancer

01 Jul 2024·Life Sciences

Androgen receptor: Structure, signaling, function and potential drug discovery biomarker in different breast cancer subtypes

Review

Author: Shukla, Nirali ; Rathore, Deepshikha ; Vora, Hemangini ; Shah, Jigna ; Dave, Heena ; Soni, Kinal ; Shah, Kanisha

The Androgen Receptor (AR) is emerging as an important factor in the pathogenesis of breast cancer (BC), which is the most common malignancy worldwide. >70 % of AR expression in primary and metastatic breast tumors has been observed which suggests that AR may be a new marker and a potential therapeutic target among AR-positive BC patients. Biological insight into AR-positive breast cancer reveals that AR may cross-talk with several vital signaling pathways, including key molecules and receptors. Downstream signaling of AR might also affect many clinically important pathways that are emerging as clinical targets in BC. AR exhibits different behaviors depending on the breast cancer molecular subtype. Preliminary clinical research using AR-targeted drugs, which have already been FDA-approved for prostate cancer (PC), has given promising results for AR-positive breast cancer patients. However, since AR positivity's prognostic and predictive value remains uncertain, it is difficult to identify and stratify patients who would benefit from AR-targeted therapies alone. Thus, the need of the hour is to target the androgen receptor as a monotherapy or in combination with other conventional therapies which has proven to be an effective clinical strategy for the treatment of prostate cancer patients, and these therapeutic strategies are increasingly being investigated in breast cancer. Therefore, in this manuscript, we review the role of AR in various cellular processes that promote tumorigenesis and aggressiveness, in different subtypes of breast cancer, as well as discuss ongoing efforts to target AR for the more effective treatment and prevention of breast cancer.

01 Feb 2024·Computational Biology and Chemistry

Targeting AR-positive breast cancer cells via drug repurposing approach

Article

Author: Sen, Plaboni ; Ghosh, Siddhartha Sankar ; Dutta, Parijat ; Kandasamy, Thirukumaran

Androgen Receptor (AR) is overexpressed in almost all the molecular subtypes of breast cancer. Besides aiding the tumorigenic environment of cancer by abnormal cell proliferation, AR also takes part in promoting cancer signaling pathways, thereby promoting aggressiveness. In this study, AR was selected as the target protein in breast cancer cells. Following this, a library of 1293 FDA-approved drugs was screened via molecular docking, MD simulation, and MMPBSA binding energy. Amongst the library of compounds, Adapalene exhibited the least binding energy of (-10.2 kCal/mol) in comparison to that of the chosen reference compound, Nilutamide (-8.6 kCal/mol). Furthermore, the in vitro efficacy of Adapalene was also determined in two different breast cancer cell lines such as MCF7 (AR-positive/ER-positive) and MDA-MB-231 (AR negative/TNBC). Initially, the cell viability assay (MTT) was performed, which endowed us with a lesser IC₅₀ value of Adapalene in comparison to Nilutamide in both cell lines. The IC₅₀ of Adapalene was found to be 12 μM and 39.4 μM in MCF7 and MDA-MB-231 cells, respectively. Furthermore, Adapalene also induced cellular ROS and apoptosis by 3.5-fold and 26.58% in MCF7 cells. However, the overall effect of Adapalene was significantly lower in the case of MDA-MB-231 cell lines, which could be attributed to its inherent nature of the absence of hormone receptors. Conclusively, Adapalene possesses greater therapeutic efficacy in comparison to the control drug, thereby hinting towards the potential use of Adapalene in the treatment of AR-positive breast cancer.

01 Jul 2023·Cell death discovery

Nuclear transport maintenance of USP22-AR by Importin-7 promotes breast cancer progression.

Article

Author: Cai, Geng-Xi ; Liu, Yuan ; Ye, Guo-Lin ; Kong, Wei-Yao ; Deng, Yuan-Fei ; Zhong, Shu-Yi ; Liu, Qing

The translocation of biological macromolecules between cytoplasm and nucleus is of great significance to maintain various life processes in both normal and cancer cells. Disturbance of transport function likely leads to an unbalanced state between tumor suppressors and tumor-promoting factors. In this study, based on the unbiased analysis of protein expression differences with a mass spectrometer between human breast malignant tumors and benign hyperplastic tissues, we identified that Importin-7, a nuclear transport factor, is highly expressed in breast cancer (BC) and predicts poor outcomes. Further studies showed that Importin-7 promotes cell cycle progression and proliferation. Mechanistically, through co-immunoprecipitation, immunofluorescence, and nuclear-cytoplasmic protein separation experiments, we discovered that AR and USP22 can bind to Importin-7 as cargoes to promote BC progression. In addition, this study provides a rationale for a therapeutic strategy to restream the malignant progression of AR-positive BC by inhibiting the high expression state of Importin-7. Moreover, the knockdown of Importin-7 increased the responsiveness of BC cells to the AR signaling inhibitor, enzalutamide, suggesting that targeting Importin-7 may be a potential therapeutic strategy.

Analysis

Perform a panoramic analysis of this field.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis

AR Positive/ER Positive Breast Cancer

Basic Info

Related

Analysis