IP Library › Granted Patent US 12,721,913
Granted Patent B2
US 12,721,913 · App. 18/012,740 · Granted Sep 1, 2026

DR5 radioimmunotherapy in the treatment of solid cancers

Inventors: Dale Ludwig (Rockaway, NJ); Eileen Geoghegan (Mamaroneck, NY)
Assignee: Actinium Pharmaceuticals, Inc.
A61K51/1027A61K45/06A61K51/1093A61P35/00
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Quick Facts
Patent No.
US 12,721,913
App. No.
18/012,740
Granted
Sep 1, 2026
Kind
B2
Abstract

Methods for treating a proliferative disease or disorder by administering an antibody radio-conjugate alone or in combination with an immune checkpoint therapy such as an antibody against an immune checkpoint inhibitor, and/or a DNA damage response inhibitor. The proliferative disease or disorder may be a solid cancer, such as breast cancer, ovarian cancer, or prostate cancer.

Claims (19)

1 . A method for treating a cancer in a human subject, the method comprising:

administering to the subject a therapeutically effective amount of either or both of: (i) an immune checkpoint therapy selected from the group consisting of an antibody against PD-1, PD-L1, PD-L2, CTLA-4, or a combination thereof, and or (ii) a DNA damage response inhibitor (DDRi) comprising olaparib, niraparib, rucaparib, or talazoparib; and

administering to the subject a therapeutically effective amount of a radiolabeled antibody against DR5, wherein the radiolabel comprises 225 Ac, 213 Bi, 227 Th, 212 Pb, 211 At, 177 Lu, 90 Y, 131 I, or 67 Cu,

wherein

administering the therapeutically effective amount of the radiolabeled antibody against DR5 is performed at least one day after administering the therapeutically effective amount of either or both of the immune checkpoint therapy and the DDRi, or

administering the therapeutically effective amount of either or both of the immune checkpoint therapy and the DDRi is performed at least one day after administering the therapeutically effective amount of the radiolabeled antibody against DR5.

2 . The method of claim 1 , wherein the cancer is a solid cancer.

3 . The method of claim 2 , wherein the solid cancer is breast cancer, triple negative breast cancer, ovarian cancer, or prostate cancer.

4 . The method of claim 3 , wherein the subject possesses a deleterious BRCA1/2 mutation.

5 . The method of claim 1 , wherein the radiolabel is 225 Ac, and the therapeutically effective amount of the 225 Ac radiolabeled antibody against DR5 comprises a radiation dose of 0.1 to 10 uCi/kg body weight of the subject, and a protein dose of 0.1 mg/kg to 16 mg/kg body weight of the subject.

6 . The method of claim 1 , wherein the radiolabel is 177 Lu, and the therapeutically effective amount of the 177 Lu radiolabeled antibody against DR5 comprises a radiation dose of 10 mCi to 500 mCi, and a protein dose of 0.1 mg/kg to 16 mg/kg body weight of the subject.

7 . The method of claim 1 , wherein the radiolabel is 131 I, and the therapeutically effective amount of the 131 I radiolabeled antibody against DR5 comprises a radiation dose of 10 mCi to 200 mCi, and a protein dose of 0.1 mg/kg to 16 mg/kg body weight of the subject.

8 . The method of claim 1 , wherein the radiolabeled antibody against DR5 comprises an antibody against DR5 selected from mapatumumab, conatumumab, lexatumumab, tigatuzumab, drozitumab, and LBY-135, or comprises a DR5-binding antibody fragment of any of said antibodies against DR5.

9 . The method of claim 5 , wherein the 225 Ac radiolabeled antibody against DR5 comprises mapatumumab, or a DR5-binding fragment thereof.

10 . The method of claim 5 , wherein the 225 Ac radiolabeled antibody against DR5 comprises conatumumab, or a DR5-binding fragment thereof.

11 . The method of claim 5 , wherein the 225 Ac radiolabeled antibody against DR5 comprises lexatumumab, or a DR5-binding fragment thereof.

12 . The method of claim 5 , wherein the 225 Ac radiolabeled antibody against DR5 comprises tigatuzumab, or a DR5-binding fragment thereof.

13 . The method of claim 5 , wherein the 225 Ac radiolabeled antibody against DR5 comprises drozitumab, or a DR5-binding fragment thereof.

14 . The method of claim 5 , wherein the 225 Ac radiolabeled antibody against DR5 comprises LBY-135, or a DR5-binding fragment thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 30, 2023
From: GEOGHEGAN, EILEEN; LUDWIG, DALE L.
To: ACTINIUM PHARMACEUTICALS, INC.
Reel/Frame 063797/0399 →
Continuity (2)
Provisional Application 63042651 · Jun 23, 2020
Related Publication 20230302168A1 · Sep 28, 2023
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