NON-INVASIVE METHOD OF EVALUATING BREAST CANCERS FOR SELECTIVE ANDROGEN RECEPTOR MODULATOR (SARM) THERAPY

    公开(公告)号:US20210128513A1

    公开(公告)日:2021-05-06

    申请号:US17066487

    申请日:2020-10-09

    摘要: This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed selective estrogen receptor modulator (SERM) (tamoxifen, toremifene, raloxifene), gonadotropin-releasing hormone (GnRH) agonist (goserelin), aromatase inhibitor (AI) (letrozole, anastrozole, exemestane), cyclin-dependent kinase 4/6 (CDK 4/6) inhibitor (palbociclib (Ibrance), ribociclib (Kisqali), abemaciclib (Vorzenio)), mTOR inhibitor (everolimus), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, neratinib (Nerlynx), olaparib (Lynparza) (an inhibitor of the enzyme poly ADP ribose polymerase (PARP)), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; HER2-positive; treating a subject suffering from ER mutant expressing breast cancer and/or treating breast cancer in a subject, by first determining the 18F-16β-fluoro-5α-dihydrotestosterone (18F-DHT) tumor uptake and identifying said subject as having AR-positive breast cancer based on 18F-DHT tumor uptake, comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

    SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
    9.
    发明申请
    SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 有权
    选择性受体降解剂(SARD)配体及其使用方法

    公开(公告)号:US20170029370A1

    公开(公告)日:2017-02-02

    申请号:US15222734

    申请日:2016-07-28

    摘要: This invention provides novel indole, indazole, benzimidazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

    摘要翻译: 本发明提供新型吲哚,吲唑,苯并咪唑,二氢吲哚,喹诺酮,异喹啉和咔唑选择性雄激素受体降解物(SARD)化合物,药物组合物及其在治疗前列腺癌,晚期前列腺癌,抗阉割前列腺癌,其他AR表达 癌症,雄激素性脱发或其他过度雄激素性皮肤疾病,肯尼迪氏病,肌萎缩性侧索硬化症(ALS),腹主动脉瘤(AAA)和子宫肌瘤,以及降低水平(通过降解)和/或活性(通过抑制) )包括雄激素受体全长(AR-FL)在内的任何雄激素受体(AR-FL),包括病原和/或抗性突变,AR-剪接变体(AR-SV)和AR的病原性多聚谷氨酰胺(polyQ)多态性。

    SARMS AND METHOD OF USE THEREOF
    10.
    发明申请
    SARMS AND METHOD OF USE THEREOF 有权
    SARMS及其使用方法

    公开(公告)号:US20170014371A1

    公开(公告)日:2017-01-19

    申请号:US15190732

    申请日:2016-06-23

    IPC分类号: A61K31/277 A61K45/06

    CPC分类号: A61K31/277 A61K45/06

    摘要: This invention is directed to substituted acylanilide compounds and uses thereof in treating muscular dystrophies such as Duchenne muscular dystrophy and Becker muscular dystrophy and in improving or preserving lung function and cardiac function in a subject suffering from Duchenne muscular dystrophy.

    摘要翻译: 本发明涉及取代的酰基酰苯胺化合物及其用于治疗肌营养不良症如杜氏肌营养不良症和贝克肌营养不良症,以及改善或维持患有杜氏肌营养不良症的受试者的肺功能和心脏功能。