HESTER, DENNIS MARTIN,海斯特 丹尼斯,海斯特 丹尼斯,VAUGHN, JASON MICHAEL,沃恩 杰森,沃恩 傑森
申请号：
TW109112959
公开号：
TW202031248A
申请日:
2015.12.04
申请国别(地区):
TW
年份:
2020
代理人:
摘要：
The present invention concerns pharmaceutical formulations of ARN-509, which can be administered to a mammal, in particular a human, suffering from an androgen receptor (AR)-related disease or condition, in particular cancer, more in particular prostate cancer, including but not limited to castration-resistant prostate cancer, metastat-ic castration resistant prostate cancer, chemotherapy-naive metastatic castration resistant prostate cancer, biochemically relapsed hormone sensitive prostate cancer, or high-risk, non-metastatic castration-resistant prostate cancer. In one aspect, these formulations comprise a solid dispersion of ARN-509 and HPMCAS. In one aspect, the solid dispersion of ARN-509 and HPMCAS is obtainable, in particular is obtained, by melt-extruding a mixture comprising ARN-509 and HPMCAS and optionally subsequently milling said melt-extruded mixture. In one aspect, the solid dispersion of ARN-509 and HPMCAS is obtainable, in particular is obtained, by spray drying a mixture comprising ARN-509 and HPMCAS in a suitable solvent.本發明涉及ARN-509的藥物配製物，它們可以被給予罹患以下項的哺乳動物，特別是人：雄激素受體(AR)相關疾病或病症，特別是癌症，更特別是前列腺癌，包括但不限於去勢抵抗性前列腺癌、轉移性去勢抵抗性前列腺癌、化療初治轉移性去勢抵抗性前列腺癌、生化復發型激素敏感性前列腺癌、或者高風險非轉移性去勢抵抗性前列腺癌。在一個方面中，該等配製物包括ARN-509和HPMCAS的固體分散體。在一個方面中，ARN-509和HPMCAS的固體分散體係可藉由熔融擠出一包括ARN-509和HPMCAS的混合物並可隨意地隨後碾磨所述熔融擠出的混合物獲得的，特別是藉由這樣做而獲得。在一個方面中，ARN-509和HPMCAS的固體分散體係可藉由噴霧乾燥一包括ARN-509和HPMCAS於適合的溶劑中的混合物獲得的，特別是藉由這樣做而獲得。
