IP Library › Granted Patent US 12,629,370
Granted Patent B2
US 12,629,370 · App. 19/264,673 · Granted May 19, 2026

Treatment of prostate cancer

Inventors: Vijaykumar Reddy Rajasekhar (Apple Valley, CA); Brendan Mark Johnson (Chapel Hill, NC); David B. MacLean (Cambridge, MA); Lynn Seely (San Mateo, CA); Paul N. Mudd, Jr. (Cary, NC); Hélène M. Faessel (Cambridge, MA)
Assignees: Sumitomo Pharma Co., Ltd.; Takeda Pharmaceutical Company Limited
A61K31/501A61K9/0053A61K31/4166A61K31/513A61P35/00
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Quick Facts
Patent No.
US 12,629,370
App. No.
19/264,673
Granted
May 19, 2026
Kind
B2
Abstract

Methods for treating prostate cancer, including advanced prostate cancer, in a subject in need thereof, include administering once-daily to the subject, at least 80 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof. Another method includes: administering once-daily to the subject in need thereof, an oral load dose formulation having from 240 mg to 480 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof; and thereafter administering once-daily to the subject, an oral maintenance dose formulation having 80 mg to 160 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof.

Claims (30)

1 . A method of treating prostate cancer in a subject in need thereof, the method comprising:

(i) orally administering a loading dose of 360 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea to the subject; and

(ii) about one day after administering the loading dose, orally administering a 120 mg dose of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea to the subject once a day for a treatment period of 24 consecutive weeks or greater;

wherein one or more adverse cardiovascular events associated with Androgen Deprivation Therapy (ADT) in the subject are reduced.

2 . The method of claim 1 , wherein the prostate cancer is advanced prostate cancer.

3 . The method of claim 1 , wherein the reduction of one or more adverse cardiovascular events associated with ADT in the subject with prostate cancer is as compared to treatment with leuprolide.

4 . The method of claim 1 , wherein the subject is administered the maintenance dose once a day for a treatment period of 48 consecutive weeks or greater.

5 . The method of claim 1 , wherein the one or more adverse cardiovascular events is a myocardial infarction.

6 . The method of claim 3 , wherein the one or more adverse cardiovascular events is a myocardial infarction.

7 . The method of claim 1 , further comprising:

discontinuing administration of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea to the subject,

wherein the subject's serum testosterone concentration is at least about 280 ng/dl within about 90 days after discontinuing.

8 . The method of claim 1 , wherein the 120 mg dose is administered with food.

9 . A method of treating prostate cancer in a subject in need thereof, the method comprising:

(i) orally administering a loading dose of 360 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea to the subject; and

(ii) about one day after administering the loading dose, orally administering a 120 mg dose of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea to the subject once a day for a treatment period of 24 consecutive weeks or greater;

wherein the subject is at risk of a cardiovascular event associated with Androgen Deprivation Therapy (ADT).

10 . The method of claim 9 , wherein the prostate cancer is advanced prostate cancer.

11 . The method of claim 9 , wherein the administration of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea decreases the likelihood of developing a cardiovascular event in the subject with prostate cancer.

12 . The method of claim 9 , wherein the administration of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea decreases the likelihood of experiencing a cardiovascular event in the subject with prostate cancer.

13 . The method of claim 11 , wherein the decrease in likelihood of developing a cardiovascular event in the subject with prostate cancer is as compared to treatment with leuprolide.

14 . The method of claim 13 , wherein the cardiovascular event is a myocardial infarction.

15 . The method of claim 12 , wherein the decrease in likelihood of experiencing a cardiovascular event in the subject with prostate cancer is as compared to treatment with leuprolide.

16 . The method of claim 15 , wherein the cardiovascular event is a myocardial infarction.

17 . The method of claim 9 , wherein the subject is administered the maintenance dose once a day for a treatment period of 48 consecutive weeks or greater.

18 . The method of claim 9 , further comprising:

discontinuing administration of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea to the subject,

wherein the subject's serum testosterone concentration is at least about 280 ng/dL within about 90 days after discontinuing.

19 . The method of claim 9 , wherein the 120 mg dose is administered with food.

20 . The method of claim 9 , wherein the cardiovascular event is a myocardial infarction.

Assignments (14)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 8, 2025
From: SUMITOMO PHARMA SWITZERLAND GMBH
To: SUMITOMO PHARMA CO., LTD.
Reel/Frame 071971/0600 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 24, 2025
From: JOHNSON, BRENDAN MARK
To: ROIVANT SCIENCES, INC.
Reel/Frame 072283/0488 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 24, 2025
From: MUDD, PAUL N., JR.
To: ROIVANT SCIENCES, INC.
Reel/Frame 071828/0719 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 24, 2025
From: RAJASEKHAR, VIJAYKUMAR REDDY; SEELY, LYNN
To: MYOVANT SCIENCES, INC.
Reel/Frame 072283/0269 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 24, 2025
From: TAKEDA DEVELOPMENT CENTER AMERICAS, INC.
To: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Reel/Frame 072283/0801 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 24, 2025
From: MACLEAN, DAVID B.
To: MILLENNIUM PHARMACEUTICALS, INC.
Reel/Frame 071828/0691 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 24, 2025
From: RAJASEKHAR, VIJAYKUMAR REDDY; SEELY, LYNN
To: MYOVANT SCIENCES, INC.
Reel/Frame 071828/0748 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 24, 2025
From: ROIVANT SCIENCES, INC.
To: MYOVANT SCIENCES GMBH
Reel/Frame 072283/0659 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 24, 2025
From: MILLENNIUM PHARMACEUTICALS, INC.
To: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Reel/Frame 071828/0715 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 24, 2025
From: ROIVANT SCIENCES, INC.
To: MYOVANT SCIENCES GMBH
Reel/Frame 071828/0724 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 24, 2025
From: FAESSEL, HÉLÈNE M.
To: TAKEDA DEVELOPMENT CENTER AMERICAS, INC.
Reel/Frame 071828/0728 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 24, 2025
From: MYOVANT SCIENCES, INC.
To: MYOVANT SCIENCES GMBH
Reel/Frame 072283/0640 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 24, 2025
From: MYOVANT SCIENCES, INC.
To: MYOVANT SCIENCES GMBH
Reel/Frame 072283/0421 →
CHANGE OF NAME Recorded Jul 24, 2025
From: MYOVANT SCIENCES GMBH
To: SUMITOMO PHARMA SWITZERLAND GMBH
Reel/Frame 072283/0761 →
Continuity (11)
Continuation 18959460 · Nov 25, 2024
Continuation 18937891 · Nov 5, 2024
Continuation 18792752 · Aug 2, 2024
Continuation 17866203 · Jul 15, 2022
Continuation 16998900 · Aug 20, 2020
Continuation 16563161 · Sep 6, 2019
Continuation 16369729 · Mar 29, 2019
Continuation PCTEP2017074849 · Sep 29, 2017
Provisional Application 62402150 · Sep 30, 2016
Provisional Application 62402004 · Sep 30, 2016
Related Publication 20250332166A1 · Oct 30, 2025
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