UW Carbone Cancer Center, University of Wisconsin, Madison, Madison, WI.
Department of Medicine, University of Rochester, Rochester, NY.
Clin Breast Cancer. 2023 Dec;23(8):813-824. doi: 10.1016/j.clbc.2023.06.009. Epub 2023 Jun 20.
Triple negative breast cancer (TNBC) is characterized by high rates of disease recurrence after definitive therapy, and median survival of less than 18 months in the metastatic setting. Systemic therapy options for TNBC consist primarily of cytotoxic chemotherapy-containing regimens, and while recently FDA-approved chemo-immunotherapy combinations and antibody-drug conjugates such as Sacituzumab govitecan have improved clinical outcomes, there remains an unmet need for more effective and less toxic therapies. A subset of TNBC expresses the androgen receptor (AR), a nuclear hormone steroid receptor that activates an androgen-responsive transcriptional program, and gene expression profiling has revealed a TNBC molecular subtype with AR expression and luminal and androgen responsive features. Both preclinical and clinical data suggest biologic similarities between luminal AR (LAR) TNBC and ER+ luminal breast cancer, including lower proliferative activity, relative chemoresistance, and high rates of oncogenic activating mutations in the phosphatidylinositol-3-kinase (PI3K) pathway. Preclinical LAR-TNBC models are sensitive to androgen signaling inhibitors (ASIs), and particularly given the availability of FDA-approved ASIs with robust efficacy in prostate cancer, there has been great interest in targeting this pathway in AR+ TNBC. Here, we review the underlying biology and completed and ongoing androgen-targeted therapy studies in early stage and metastatic AR+ TNBC.
三阴性乳腺癌(TNBC)的特点是在明确治疗后疾病复发率高,转移性疾病中位生存期不到 18 个月。TNBC 的系统治疗方案主要包括含细胞毒性化疗的方案,尽管最近 FDA 批准的化疗免疫联合治疗和抗体药物偶联物,如Sacituzumab govitecan,改善了临床结果,但仍需要更有效和毒性更小的治疗方法。TNBC 的一部分表达雄激素受体(AR),这是一种核激素甾体受体,可激活雄激素反应性转录程序,基因表达谱揭示了一种具有 AR 表达和管腔和雄激素反应特征的 TNBC 分子亚型。临床前和临床数据表明,AR 阳性(LAR)TNBC 和 ER+ 管腔乳腺癌之间存在生物学相似性,包括增殖活性较低、相对化疗耐药性和磷脂酰肌醇-3-激酶(PI3K)通路中致癌激活突变的高发生率。临床前 LAR-TNBC 模型对雄激素信号抑制剂(ASI)敏感,特别是鉴于在前列腺癌中具有强大疗效的 FDA 批准的 ASI 的可用性,因此在 AR+ TNBC 中靶向该途径具有很大的兴趣。在这里,我们回顾了早期和转移性 AR+ TNBC 中已完成和正在进行的雄激素靶向治疗研究的基础生物学。