预约演示

更新于：2025-01-23

AR

更新于：2025-01-23

基本信息

别名

AIS、Androgen receptor、AR

+ [11]

简介

Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues (PubMed:19022849). Transcription factor activity is modulated by bound coactivator and corepressor proteins like ZBTB7A that recruits NCOR1 and NCOR2 to the androgen response elements/ARE on target genes, negatively regulating androgen receptor signaling and androgen-induced cell proliferation (PubMed:20812024). Transcription activation is also down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3. Lacks the C-terminal ligand-binding domain and may therefore constitutively activate the transcription of a specific set of genes independently of steroid hormones. Lacks the C-terminal ligand-binding domain and may therefore constitutively activate the transcription of a specific set of genes independently of steroid hormones.

关联

424

项与 AR 相关的药物

Berdazimer sodium

靶点

作用机制

AR拮抗剂 [+1]

在研机构

Lnhc, Inc. [+2]

原研机构

NVN Liquidation, Inc.

在研适应症

传染性软疣 [+1]

非在研适应症

尖锐湿疣 [+3]

最高研发阶段批准上市

首次获批国家/地区

美国

首次获批日期2024-01-05

Rezvilutamide

瑞维鲁胺

靶点

作用机制

AR拮抗剂

在研机构

原研机构

在研适应症

非在研适应症

最高研发阶段批准上市

首次获批国家/地区

中国

首次获批日期2022-06-28

Proxalutamide

普克鲁胺

靶点

作用机制

AR拮抗剂

在研机构

原研机构

在研适应症

非在研适应症

最高研发阶段批准上市

首次获批国家/地区

巴拉圭

首次获批日期2021-07-16

2,281

项与 AR 相关的临床试验

NCT06660862

/ Not yet recruiting临床4期IIT

DAROSTEP: Evaluating Step Counts as a Biomarker and Its Relationship on Treatment Outcomes in Vulnerable Patients With Metastatic Hormone-Sensitive Prostate Cancer on Darolutamide and Androgen Deprivation Therapy

This prospective clinical trial aims to investigate the impact of darolutamide in combination with standard-of-care androgen deprivation on physical activity, specifically step count, and its correlation with important markers of safety in vulnerable adults who screen positive by a brief geriatric assessment (GA) and metastatic hormone-sensitive prostate cancer.

开始日期2025-11-01

申办/合作机构

The University of Chicago

NCT06782048

/ Not yet recruiting临床2期IIT

Pyrvinium for Reversal of Precancerous Metaplasia and Dysplasia in the Stomach

This study is carried out to find out if a drug called pyrvinium is able to convert pre-cancerous tissue in the stomach back to healthy tissue, to lower the chances of stomach cancer. Pyrvinium is a drug that has been used for a long time to treat pinworms in children and its anti-cancer properties are currently under investigation. Tests in animals have shown that pyrvinium made unhealthy tissue healthier and stopped some cells from growing in a bad way. Based on preclinical studies, the investigators hypothesise that the proportion of samples with pre-cancerous tissue in the stomach would decrease by 50% after exposure to pyrvinium at the 6-week timepoint, with anticipated durability of the response at the one-year follow-up.

开始日期2025-08-01

申办/合作机构

National University Hospital

[+1]

NCT01894308

/ Not yet recruiting临床2期

A Multiple-Dose, Single Period, Phase II Dose Ranging Study to Examine TDS-Testosterone 5% in Adult Male Subjects

This study is a continuation of previous studies done in healthy volunteers to prove the efficacy of delivering Testosterone, the male hormone, rapidly across intact skin in s series of doses from low to high in men with low-to-no natural testosterone production to measure their response to the varying doses. The results of this study will inform further studies which will be longer in length, as to the starting doses. The study will be conducted in London, U.K. at the Advanced Therapies Centre, The London Clinic.

开始日期2025-06-01

申办/合作机构

Transdermal Delivery Solutions Corp.

100 项与 AR 相关的临床结果

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100 项与 AR 相关的转化医学

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0 项与 AR 相关的专利（医药）

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34,784

项与 AR 相关的文献（医药）

2025-12-01·Immunologic Research

Baicalein attenuates ovalbumin-induced allergic rhinitis through the activation of nuclear receptor subfamily 4 group a member 1

Article

作者: Jian, Xuli ; Wang, Qianqian ; Xu, Lili ; Ge, Hongzhou ; Li, Zhen ; Xu, Ying

Baicalein, one of the major active flavonoids found in Scutellaria baicalensis, has been revealed to exhibit potent anti-inflammatory properties in allergic airway inflammation. This study aimed to explore the role of baicalein and its relevant mechanism in the treatment of allergic rhinitis (AR). The bioinformatics tools were used to predict the targets of baicalein and AR-related genes. AR mice were induced by ovalbumin (OVA) and treated with lentivirus-encapsulated knockdown of nuclear receptor subfamily 4 group A member 1 (NR4A1) or protein arginine N-methyltransferase 1 (PRMT1) plasmids and baicalein. IL-4/IL-13-induced human nasal mucosal epithelial cells (HNEpC) were transfected with knockdown of NR4A1 or PRMT1 plasmids and baicalein treatment. Baicalein alleviated AR-like symptoms and reduced the levels of immunoglobulin E, histamine, and LTC4 in serum and IL-4, IL-25, and IL-33 concentrations in nasal lavage fluids of mice induced with OVA by increasing NR4A1 expression. NR4A1 blocked the NFκB/p65 pathway by mediating transcriptional repression of PRMT1. Knockdown of PRMT1 overturned the effects of NR4A1 knockdown on IL-4/IL-13-induced HNEpC and OVA-induced mice. Collectively, these findings provide evidence that baicalein activation of NR4A1 mediates transcriptional repression of PRMT1 and relieves AR in mice by blocking the NFκB/p65 pathway.

2025-12-01·Histochemistry and Cell Biology

Protective effects of adipose-derived stem cells against testicular injury induced after ischemia–reperfusion by regulating autophagy

Article

作者: Elci, Mualla Pınar ; Demir, Hazal ; Alimogullari, Ebru ; Kartal, Bahar

The damaged organ may experience severe pathological alterations as a result of tissue ischemia-reperfusion (I/R). The study of stem cell-based repair therapies is actively being conducted, and the outcomes and therapeutic potential of these cells are both promising. Autophagy checks protein homeostasis by breaking down huge damaged proteins or organelles. The study's objective was to assess how ADSCs impact the autophagic process after testicular ischemia/reperfusion. In our investigation, 30 male rats were divided into five groups: control, ADSC, ischemia, I/R, and I/R + ADSC (n = 6). Hematoxylin-eosin (HE) was used to stain the testes, and histological changes were assessed. The immunoexpression of androgen receptor (AR), Beclin1, protein light chain 3B (LC3B), and p62 were examined. The seminiferous epithelium in the testis from the ischemia and I/R groups revealed significant degeneration with disorganized morphology, damaged spermatogenic cells, and interstitial space congestion, according to HE stain results. Johnsen's score were significantly better in I/R + ADSC group than in ischemia and I/R groups. We demonstrated that in rat testes from the I/R groups, immunostaining of Beclin 1 (p = 0.042) and LC3B (p = 0.011) were raised, and p62 (p = 0.047) and AR (p = 0.049) were decreased. Ischemia and I/R promoted testicular autophagy, therefore we can conclude that ADSCs prevent excessive autophagy. Additionally, these results show that the use of ADSCs cures testicular injury and dysfunction associated with I/R injury in rats even a little.

2025-09-01·Neural Regeneration Research

Reduced mesencephalic astrocyte–derived neurotrophic factor expression by mutant androgen receptor contributes to neurodegeneration in a model of spinal and bulbar muscular atrophy pathology

Article

作者: Xing, Tingting ; Qin, Yiyang ; Yin, Peng ; Zhu, Wenzhen ; Yang, Su ; Zhang, Yiran ; Li, Shihua ; Li, Xiao-Jiang ; Guo, Tingting

JOURNAL/nrgr/04.03/01300535-202509000-00027/figure1/v/2024-12-31T000210Z/r/image-tiff Spinal and bulbar muscular atrophy is a neurodegenerative disease caused by extended CAG trinucleotide repeats in the androgen receptor gene, which encodes a ligand-dependent transcription factor. The mutant androgen receptor protein, characterized by polyglutamine expansion, is prone to misfolding and forms aggregates in both the nucleus and cytoplasm in the brain in spinal and bulbar muscular atrophy patients. These aggregates alter protein–protein interactions and compromise transcriptional activity. In this study, we reported that in both cultured N2a cells and mouse brain, mutant androgen receptor with polyglutamine expansion causes reduced expression of mesencephalic astrocyte-derived neurotrophic factor. Overexpression of mesencephalic astrocyte-derived neurotrophic factor ameliorated the neurotoxicity of mutant androgen receptor through the inhibition of mutant androgen receptor aggregation. Conversely, knocking down endogenous mesencephalic astrocyte-derived neurotrophic factor in the mouse brain exacerbated neuronal damage and mutant androgen receptor aggregation. Our findings suggest that inhibition of mesencephalic astrocyte-derived neurotrophic factor expression by mutant androgen receptor is a potential mechanism underlying neurodegeneration in spinal and bulbar muscular atrophy.

1,574

项与 AR 相关的新闻（医药）

2025-01-20

·求实药社

MASH新药！海创药业中国临床试验完成首例受试者入组

来源：医药观澜 1月19日，海创药业宣布其自主研发的HP515片用于治疗非酒精性脂肪性肝炎（NASH，又称代谢性脂肪性肝炎，MASH）的临床试验于近日完成首例受试者入组。该研究是一项评估HP515片在健康受试者中单次和多次剂量递增给药的安全性、耐受性、药代动力学、药效动力学及食物影响的1期临床试验。 HP515片是海创药业自主研发的一种口服高选择性甲状腺激素受体β亚型（THR-β）激动剂。它能直接作用于THR-β激活下游基因转录，通过增强肝细胞脂质代谢活性、提高肝脏脂肪代谢、降低脂毒性达到对非酒精性脂肪性肝炎的改善效果。临床前研究结果显示，HP515在肝脏分布高，安全性好，并在消退MASH和改善肝纤维化方面具有显著效果。该产品已经先后在中国和美国获批临床，拟开发适应症为MASH。海创药业是一家专注于癌症和代谢性疾病的全球化创新药物企业。该公司现有产品管线中，AR抑制剂氘恩扎鲁胺（HC-1119）中国3期临床试验已达到主要研究终点，上市申请于2023年11月获NMPA受理。其余处于临床阶段的在研产品还包括URAT1抑制剂HP501、口服AR靶向蛋白降解嵌合体HP518、用于治疗ER+/HER2-晚期乳腺癌的口服靶向蛋白降解嵌合体HP568片，以及用于治疗血液系统恶性肿瘤的HP537片、用于治疗骨髓纤维化的HP560片等。免责声明：文章内容仅供参考，不构成投资建议。投资者据此操作，风险自担, 关于对文中陈述、观点判断保持中立，不对所包含内容的准确性、可靠性或完整性提供任何明示或暗示的保证。请读者仅作参考，并请自行承担全部责任。本公众号发布的各类文章重在分享，如有侵权请联系我们，我们将会删除。联系我们 I-RNA 2025 展位火热预定中！扫码立即咨询电话：13816031174 （同微信）赞助形式包括但不仅限于演讲席位、会场展位、会刊彩页、晚宴赞助、会议用品宣传等。点击此处“阅读全文”咨询更多！

临床3期ASH会议

2025-01-20

·医药观澜

海创药业1类MASH新药中国临床试验完成首例受试者入组

▎药明康德内容团队报道 1月19日，海创药业宣布其自主研发的HP515片用于治疗非酒精性脂肪性肝炎（NASH，又称代谢性脂肪性肝炎，MASH）的临床试验于近日完成首例受试者入组。该研究是一项评估HP515片在健康受试者中单次和多次剂量递增给药的安全性、耐受性、药代动力学、药效动力学及食物影响的1期临床试验。 HP515片是海创药业自主研发的一种口服高选择性甲状腺激素受体β亚型（THR-β）激动剂。它能直接作用于THR-β激活下游基因转录，通过增强肝细胞脂质代谢活性、提高肝脏脂肪代谢、降低脂毒性达到对非酒精性脂肪性肝炎的改善效果。临床前研究结果显示，HP515在肝脏分布高，安全性好，并在消退MASH和改善肝纤维化方面具有显著效果。该产品已经先后在中国和美国获批临床，拟开发适应症为MASH。海创药业是一家专注于癌症和代谢性疾病的全球化创新药物企业。该公司现有产品管线中，AR抑制剂氘恩扎鲁胺（HC-1119）中国3期临床试验已达到主要研究终点，上市申请于2023年11月获NMPA受理。其余处于临床阶段的在研产品还包括URAT1抑制剂HP501、口服AR靶向蛋白降解嵌合体HP518、用于治疗ER+/HER2-晚期乳腺癌的口服靶向蛋白降解嵌合体HP568片，以及用于治疗血液系统恶性肿瘤的HP537片、用于治疗骨髓纤维化的HP560片等。参考资料： [1] 海创药业HP515片用于治疗非酒精性脂肪性肝炎的中国临床试验完成首例受试者入组. Retrieved Jan 19, 2025, from https://mp.weixin.qq.com/s/qA-yub9dlvV2zhrsNCVL1A 本文由药明康德内容团队根据公开资料整理编辑，欢迎个人转发至朋友圈。转发授权或其他合作需求，请联系wuxi_media@wuxiapptec.com。免责声明：药明康德内容团队专注介绍全球生物医药健康研究进展。本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。

临床3期ASH会议申请上市

2025-01-17

·辉瑞制药

泰泽纳®首批处方成功落地，加速惠及更多晚期前列腺癌患者

近日，辉瑞前列腺癌创新药物泰泽纳®（TALZENNA®，通用名：甲苯磺酸他拉唑帕利胶囊）在北京、上海、天津、济南、石家庄、郑州、沈阳、温州、东莞、成都等多地开出全国首批处方，并将同步在30个省市的70个城市推动临床应用，为中国HRR突变的晚期前列腺癌患者带来更加个性化的精准治疗选择。泰泽纳®是具有独特双重作用机制的PARP抑制剂，已于去年年底获得中国国家药品监督管理局（NMPA）批准，与恩扎卢胺联合用于HRR（同源重组修复）基因突变的转移性去势抵抗性前列腺癌 (mCRPC) 成人患者，也是中国目前唯一获批HRR基因突变的mCRPC治疗的PARP抑制剂。辉瑞中国区总裁、RDPAC执行委员会主席、中国外商投资企业协会副会长Jean-Christophe Pointeau表示：“泰泽纳®在中国的快速获批及落地临床应用为国内众多前列腺癌患者提供了国际同步的精准治疗选择，这是辉瑞‘中国速度’的体现，也是辉瑞‘为患者带来改变其生活的突破创新’的又一实践。包括前列腺癌在内的泌尿系统肿瘤是中国男性常见恶性肿瘤，也是辉瑞重点聚焦的疾病领域之一，我们将持续加大研发投入，推动更多肿瘤治疗的科学突破，并进一步缩短创新药物在国内上市的窗口期，帮助肿瘤患者延长生命、改善生活质量，真正地‘Outdo Cancer’！” 辉瑞中国区总裁 Jean-Christophe Pointeau 前列腺癌是全球最常见的恶性肿瘤之一，在男性群体中的发病率仅次于肺癌[1]。然而，由于前列腺癌早期症状不明显，我国前列腺癌初诊病例以临床中晚期居多，晚期前列腺癌患者在接受过雄激素剥夺治疗后出现治疗抵抗，并出现转移，进入转移性去势抵抗性前列腺癌阶段，而mCRPC是前列腺癌的终末阶段，具有高度异质性和致死性，如果缺乏有效的治疗，mCRPC患者的中位生存时间一般不会超过3年[3]。约有25%的mCRPC患者携带HRR基因突变[4]，而这类患者肿瘤的恶性程度更高，疾病进展也更加迅速，在临床上存在巨大的未满足需求。国内外指南均建议对转移性前列腺癌患者进行基因检测，以指导用药, 尤其强调了检测HRR基因突变的重要性[5][6]。而基于精准检测后的PARP抑制剂联合新型内分泌药物也已成为各项权威指南推荐的mCRPC一线治疗方案。泰泽纳®具有抑制PARP酶及PARP捕获的双重作用机制，与雄激素受体抑制剂恩扎卢胺联用，可诱导携带HRR基因突变导致的肿瘤细胞死亡。临床研究数据证实，泰泽纳®联合恩扎卢胺治疗可显著改善HRR基因突变的mCRPC患者的临床结局[7]。泰泽纳®加速落地临床应用，将进一步助力中国前列腺癌的精准诊疗及患者生存结局的改善。 2024年9月，欧洲肿瘤内科学会（ESMO）年会期间，辉瑞公布了全球多中心III期注册临床研究TALAPRO-2的中国人群数据，进一步证实了泰泽纳®为患者带来的临床获益。而在今年2月即将举行的2025年美国临床肿瘤学会泌尿生殖肿瘤研讨会（ASCO GU 2025）期间，辉瑞将进一步公布TALAPRO-2研究的更多最新数据。关于泰泽纳® (通用名：甲苯磺酸他拉唑帕利胶囊) 滑动阅览泰泽纳®（通用名：甲苯磺酸他拉唑帕利胶囊) 是一种聚腺苷二磷酸核糖聚合酶（PARP，包括PARP1和PARP2）抑制剂，该酶在DNA修复中发挥作用。2023年6月，美国食品药品监督管理局（FDA）批准泰泽纳®联合恩扎卢胺用于同源重组修复（HRR）基因突变的转移性去势抵抗性前列腺癌（mCRPC）成人患者的治疗。2024年1月，欧洲药品管理局(EMA)批准泰泽纳®与恩扎卢胺联用治疗无临床化疗指征的mCRPC成人患者。2024年10月，中国国家药品监督管理局（NMPA）批准泰泽纳®联合恩扎卢胺用于HRR基因突变的转移性去势抵抗性前列腺癌 (mCRPC) 成人患者。关于辉瑞肿瘤滑动阅览在辉瑞肿瘤，我们身处癌症治疗新纪元的最前沿。我们拥有行业领先的产品组合和广泛的产品管线，覆盖抗体偶联药物（ADC）、小分子药物、双特异性抗体和其他免疫疗法，通过颠覆性的作用机制，从多个方向着手攻克癌症。我们致力于为乳腺癌、泌尿系统肿瘤、血液肿瘤、消化道肿瘤、妇科肿瘤和包括肺癌在内的胸部肿瘤等全球高发癌种提供变革性的治疗方案。在科学的驱动下，辉瑞致力于加快突破性创新的步伐，帮助肿瘤患者延长生命、改善生活质量。免责声明滑动阅览本新闻稿仅在于传递科学前沿信息，不构成对任何药物或治疗方案的推荐或推广。如您有药物或治疗方面的问题，请咨询医疗卫生专业人士。 [1] IARC. (2020). Global Cancer Observatory: Cancer Today. Lyon, France: International Agency for Research on Cancer. Retrieved from https://gco.iarc.fr/today. [2]国家癌症中心, 国家肿瘤质控中心前列腺癌质控专家委员会. 中国前列腺癌规范诊疗质量控制指标(2022版) [J] . 中华肿瘤杂志, 2022, 44(10) : 1011-1016. [2] National Cancer Center, Prostate Cancer Quality Control Expert Committee of the National Cancer Quality Control Center. Quality control index for standardized diagnosis and treatment of prostate cancer in China (2022 edition) [J]. Chinese Journal of Oncology, 2022, 44(10): 1011-1016. [3] Chen JR, Zhang YW, Zhang XM, et al. Comparison of systemic treatments for metastatic castration-resistant prostate cancer after docetaxel failure: a systematic review and network meta-analysis[J]. Front Pharmacol, 2022, 12:789319. DOI:10.3389/fphar.2021.789319. [4] Chung, J. H., Dewal, N., Sokol, E., Mathew, P., Whitehead, R., Millis, S. Z., Frampton, G. M., Bratslavsky, G., Pal, S. K., Lee, R. J., Necchi, A., Gregg, J. P., Lara, P., Jr, Antonarakis, E. S., Miller, V. A., Ross, J. S., Ali, S. M., & Agarwal, N. (2019). Prospective Comprehensive Genomic Profiling of Primary and Metastatic Prostate Tumors. JCO precision oncology, 3, PO.18.00283. [5] National Comprehensive Cancer Network. (2024). NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines®): Prostate Cancer. Version 3.2024. [6] 中国临床肿瘤学会指南工作委员会. (2023). 中国临床肿瘤学会（CSCO）前列腺癌诊疗指南2023. 人民卫生出版社. [6] Chinese Society of Clinical Oncology Guidance Working Committee (2023). Chinese Society of Clinical Oncology (CSCO). 2023 Guidelines for the Diagnosis and Treatment of Prostate Cancer. People's Medical Publishing House. [7] Fizazi, K., Azad, A. A., Matsubara, N., Carles, J., Fay, A. P., De Giorgi, U., Joung, J. Y., Fong, P. C. C., Voog, E., Jones, R. J., Shore, N. D., Dunshee, C., Zschäbitz, S., Oldenburg, J., Ye, D., Lin, X., Healy, C. G., Di Santo, N., Laird, A. D., Zohren, F., … Agarwal, N. (2024). First-line talazoparib with enzalutamide in HRR-deficient metastatic castration-resistant prostate cancer: the phase 3 TALAPRO-2 trial. Nature medicine, 30(1), 257–264. 往期 · 推荐博遏制耐药，拯救生命，我们在行动！疗创新引领全面守护 | 为血液病患者带去更多希望辉瑞创新药物 HYMPAVZI™（马塔西单抗/marstacimab-hncq）获FDA批准用于治疗血友病A及血友病B 【一键通达】药品问询不再难，医学信息解忧烦!

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