公开(公告)号：US20210330612A1

公开(公告)日：2021-10-28

申请号：US17299948

申请日：2019-12-06

申请人： Radius Pharmaceuticals, Inc.

发明人： Hitisha PATEL ,  Teeru BIHANI ,  Heike ARLT ,  Nianjun TAO

IPC分类号： A61K31/137 ,  A61P35/00 ,  C12Q1/6886

摘要： Disclosed herein are methods of treating a CDK4/6 inhibitor resistant estrogen receptor alpha-positive cancer in a subject having either a wild-type estrogen receptor alpha and/or a mutant estrogen receptor alpha, the method comprising administering to the subject a therapeutically effective amount of elacestrant, or a pharmaceutically acceptable salt or solvate thereof, wherein the mutant estrogen receptor alpha comprises one or more mutations selected from the group consisting of D538G, Y537X1, L536X2, P535H, V534E, S463P, V392I, E380Q and combinations thereof, wherein: X1 is S, N, or C; and X2 is R or Q. In some embodiments, the CDK4/6 inhibitor resistant estrogen receptor alpha-positive cancer is selected from the group consisting of breast cancer, uterine cancer, ovarian cancer, and pituitary cancer.

公开(公告)号：US20220016052A1

公开(公告)日：2022-01-20

申请号：US17299361

申请日：2019-12-06

申请人： Radius Pharmaceuticals, Inc.

发明人： Hitisha PATEL ,  Teeru BIHANI ,  Heike ARLT ,  Nianjun TAO

IPC分类号： A61K31/137 ,  A61P35/00

摘要： Disclosed herein are methods of treating a drug resistant estrogen receptor alpha-positive cancer in a subject having a mutant estrogen receptor alpha, the method comprising administering to the subject a therapeutically effective amount of elacestrant, or a pharmaceutically acceptable salt or solvate thereof, wherein the mutant estrogen receptor alpha comprises one or more mutations selected from the group consisting of D538G, Y537X1, L536X2, P535H, V534E, S463P, V392I, E380Q and combinations thereof, wherein: X1 is S, N, or C; and X2 is R or Q. In some embodiments, the drug resistant estrogen receptor alpha-positive cancer is selected from the group consisting of breast cancer, uterine cancer, ovarian cancer, and pituitary cancer.