IP Library › Granted Patent US 12,582,617
Granted Patent B2
US 12,582,617 · App. 17/852,673 · Granted Mar 24, 2026

Methods for treating cancer

Inventor: Gary Hattersley (Stow, MA)
Assignee: RADIUS PHARMACEUTICALS, INC.
A61K31/137A61K31/138A61K31/436A61K31/519A61K31/675A61K45/06A61P35/00A61P35/04A61K2300/00
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Quick Facts
Patent No.
US 12,582,617
App. No.
17/852,673
Granted
Mar 24, 2026
Kind
B2
Abstract

Disclosed herein are methods of inhibiting tumor growth or producing tumor regression in a subject by administering to the subject a therapeutically effective amount of a combination of palbociclib and RAD1901.

Claims (18)

1 . A method of inhibiting tumor growth or producing tumor regression in a subject having a mutant estrogen receptor alpha-positive cancer comprising administering to said subject a therapeutically effective amount of a combination of palbociclib and RAD1901 having the structure:

or a salt or solvate thereof.

2 . The method of claim 1 , wherein the mutant estrogen receptor alpha-positive cancer is drug resistant.

3 . The method of claim 1 , wherein the cancer is selected from the group consisting of breast cancer, uterine cancer, ovarian cancer, and pituitary cancer.

4 . The method of claim 1 , wherein the cancer is a metastatic cancer.

5 . The method of claim 1 , wherein said cancer is positive for the mutant estrogen receptor alpha comprising one or more mutations selected from the group consisting of Y537X 1 , L536X 2 , P535H, V534E, S463P, V392I, E380Q and combinations thereof, wherein:

X 1 is S, N, or C, D538G; and X 2 is R or Q.

6 . The method of claim 5 , wherein the mutation is Y537S.

7 . The method of claim 1 , wherein the ratio of the concentration of RAD1901 or a salt or solvate thereof in the tumor to the concentration of RAD1901 or a salt or solvate thereof in plasma (T/P) following administration is at least about 15.

8 . The method of claim 1 , wherein the subject has osteoporosis or a higher risk of osteoporosis.

9 . The method of claim 1 , wherein the subject is a premenopausal woman.

10 . The method of claim 1 , wherein the subject is a postmenopausal woman who had relapsed or progressed after previous treatment with SERMs and/or AIs.

11 . The method of claim 1 , wherein the RAD1901 is administered in an amount of about 150 to about 1,500 mg q.d.

12 . The method of claim 1 , wherein the salt thereof is RAD1901 dihydrochloride.

13 . The method of claim 2 , wherein the tumor is resistant to a drug selected from the group consisting of anti-estrogens, aromatase inhibitors, and combinations thereof.

14 . The method of claim 13 , wherein the anti-estrogen is tamoxifen or fulvestrant.

15 . The method of claim 13 , wherein the aromatase inhibitors is aromasin.

16 . The method of claim 11 , wherein the RAD1901 is administered in an amount of 200 mg, 400 mg, or 500 mg per day.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 11, 2022
From: HATTERSLEY, GARY
To: RADIUS PHARMACEUTICALS, INC.
Reel/Frame 060469/0848 →
Continuity (17)
Division 16580914 · Sep 24, 2019
Continuation 15794861 · Oct 26, 2017
Continuation PCTUS2016030321 · Apr 29, 2016
Provisional Application 62323576 · Apr 15, 2016
Provisional Application 62323572 · Apr 15, 2016
Provisional Application 62265658 · Dec 10, 2015
Provisional Application 62265774 · Dec 10, 2015
Provisional Application 62265663 · Dec 10, 2015
Provisional Application 62265696 · Dec 10, 2015
Provisional Application 62252916 · Nov 9, 2015
Provisional Application 62252085 · Nov 6, 2015
Provisional Application 62192944 · Jul 15, 2015
Provisional Application 62192940 · Jul 15, 2015
Provisional Application 62158469 · May 7, 2015
Provisional Application 62155451 · Apr 30, 2015
Provisional Application 62154699 · Apr 29, 2015
Related Publication 20220339126A1 · Oct 27, 2022
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