IP Library Granted Patent US 12,533,427
Granted Patent B2
US 12,533,427 · App. 16/758,081 · Granted Jan 27, 2026

Radioactive antitumor agent

Inventors: Yukie Yoshii (Chiba, JP); Hiroki Matsumoto (Tokyo, JP)
Assignee: NATIONAL INSTITUTES FOR QUANTUM SCIENCE & TECHNOLOGY
A61K51/0478A61P35/00
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Quick Facts
Patent No.
US 12,533,427
App. No.
16/758,081
Granted
Jan 27, 2026
Kind
B2
Abstract

This radioactive antitumor agent comprises a radioactive dithiosemicarbazone-copper complex as an active ingredient, and is characterized by being used in such a way that the radioactive dithiosemicarbazone-copper complex is administered multiple times to an organism requiring tumor treatment, at a radioactive dose that avoids dose-limiting toxicity, as determined on the basis of hematological parameters. The multiple administration preferably consists of intermittent administration at time intervals allowing the hematological parameters to return to a normal range.

Claims (10)

1 . A method of treating a tumor, which comprises performing multiple administration, at a predetermined time interval, of a radioactive antitumor agent comprising a radioactive dithiosemicarbazone-copper complex as an active ingredient to a living body in need of internal radiotherapy of the tumor at a radioactive dose that (1) effectively kills tumor cells/tissues as determined on the basis of tumor growth inhibition and survival prolongation, and (2) avoids dose-limiting toxicity as determined on the basis of a hematological parameter selected from the group consisting of white blood cell count, red blood cell count and platelet count,

wherein the radioactive dose is from 30 MBq/kg to 450 MBq/kg, and

the radioactive dithiosemicarbazone-copper complex is represented by the following formula (1):

 wherein R 1 , R 2 , R 3 , and R 4 are each independently selected from the group consisting of a hydrogen atom, an alkyl group, and an alkoxy group, and Cu is a radioisotope of copper selected from the group consisting of 64 Cu and 67 Cu, and

wherein the tumor is a malignant brain tumor.

2 . The method according to claim 1 , wherein the radioactive dose is a radioactive dose that is from 75 MBg/kg to 300 MBg/kg and avoids statistically significant decrease in two or more kinds of blood cell counts at a significance level set to 5%.

3 . The method according to claim 1 , wherein the multiple administration consists of intermittent administration at a time interval during which the hematological parameter recovers to a normal range.

4 . The method according to claim 3 , wherein the time interval during which the hematological parameter recovers to a normal range is a time interval during which the hematological parameter recovers to be equal to the hematological parameter before administration.

5 . The method according to claim 1 , wherein the radioactive dose is from 100 MBq/kg to 200 MBq/kg.

6 . The method according to claim 1 , wherein the malignant brain tumor is malignant glioblastoma.

Assignments (2)
CHANGE OF NAME Recorded May 29, 2024
From: NATIONAL INSTITUTES FOR QUANTUM & RADIOLOGICAL SCIENCE &TECHNOLOGY
To: NATIONAL INSTITUTES FOR QUANTUM SCIENCE &TECHNOLOGY
Reel/Frame 067567/0125 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 22, 2020
From: YOSHII, YUKIE; MATSUMOTO, HIROKI
To: NATIONAL INSTITUTES FOR QUANTUM AND RADIOLOGICAL SCIENCE AND TECHNOLOGY
Reel/Frame 052460/0299 →
Priority Claims (1)
JP 2017-212180 · Nov 1, 2017 · national
Continuity (1)
Related Publication 20200360544A1 · Nov 19, 2020
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