IP Library Granted Patent US 7,547,673
Granted Patent B2
US 7,547,673 · App. 10/243,550 · Granted Jun 16, 2009

Therapeutics for cancer using 3-bromopyruvate and other selective inhibitors of ATP production

Assignee: The Johns Hopkins University
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Quick Facts
Patent No.
US 7,547,673
App. No.
10/243,550
Granted
Jun 16, 2009
Kind
B2
Abstract

The present invention relates to methods of treating a cancerous tumor using selective inhibitors of ATP production. The present invention also relates to pharmaceutical preparations comprising such inhibitors and methods for administering them intraarterially directly to a tumor, as well as methods for identifying compositions that selectively inhibitor ATP production for use in the invention.

Claims (25)

1. A method of treating primary or secondary liver cancer in a subject comprising administering to a subject having a primary or secondary liver tumor an effective amount of a 3-halopyruvate or a salt thereof delivered by transcatheter hepatic intraarterial injection into the liver.

2. The method of claim 1 , wherein the 3-halopyruvate is 3-bromopyruvate.

3. A method of treating primary or secondary liver cancer in a subject comprising administering to a subject having a primary or secondary liver tumor a therapeutically effective amount of a 3-halopyruvate or a salt thereof and fluorouracil delivered by transcatheter hepatic intraarterial injection into the liver.

4. The method of claim 1 , wherein the 3-halopyruvate or salt thereof is provided in a sustained-release formulation.

5. The method of claim 3 , wherein the 3-halopyruvate is 3-bromopyruvate.

6. A method of treating primary or secondary liver cancer in a subject comprising administering to a subject having a primary or secondary liver tumor delivered by transcatheter hepatic intraarterial injection into the liver an effective amount of a compound represented by formula:

wherein, independently of each occurrence:

X represents a halide;

R 1 represents OR, H, N(R″)2, C1-C6 alkyl, C6-C12 aryl, C1-C6 heteroalkyl, or C6-C12 heteroaryl;

R″ represents H, C1-C6 alkyl, or C6-C12 aryl;

R represents H, alkali metal, C1-C6 alkyl, C6-C12 aryl or C(O)R′; and

R′ represents H, C1-C20 alkyl or C6-C12 aryl, or a salt thereof.

7. The method of claim 6 , wherein the halide is bromide.

8. A method of treating primary or secondary liver cancer in a subject comprising administering to a subject having a primary or secondary liver tumor delivered by transcatheter hepatic intraarterial injection into the liver an effective amount of a compound represented by formula:

wherein, independently of each occurrence:

X represents a halide;

R 1 represents OR, H, N(R″)2, C1-C6 alkyl, C6-C12 aryl, C1-C6 heteroalkyl, or C6-C12 heteroaryl;

R″ represents H, C1-C6 alkyl, or C6-C12 aryl;

R represents H, alkali metal, C1-C6 alkyl, C6-C12 aryl or C(O)R′; and

R′ represents H, C1-C20 alkyl or C6-C12 aryl, or a salt thereof and administering fluorouracil to said subject.

9. The method of claim 8 , wherein the halide is bromide.

10. A method of treating a liver tumor that has metastasized within the liver of a subject an effective amount of a 3-halopyruvate or a salt thereof delivered by transcatheter hepatic intraarterial injection into the liver.

11. The method of claim 10 , wherein the 3-halopyruvate is 3-bromopyruvate.

12. The method of claim 1 , wherein the 3-halopyruvate is administered directly to the blood supply of the tumor without embolization of the tumor.

13. The method of claim 1 , consisting of administering to a subject having a liver tumor an effective amount of a 3-halopyruvate or a salt thereof delivered by transcatheter hepatic intraarterial injection into the liver.

Assignments (2)
CONFIRMATORY LICENSE Recorded Sep 23, 2008
From: JOHNS HOPKINS UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 021576/0820 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 24, 2005
From: KO, YOUNG HE; GESCHWIND, JEAN-FRANCOIS H.; PEDERSEN, PETER L.
To: JOHN HOPKINS UNIVERSITY SCHOOL OF MEDICINE
Reel/Frame 016673/0077 →
Continuity (2)
Provisional Application 6031871000 · Sep 13, 2001
Related Publication 20030087961A1 · May 8, 2003