IP Library Granted Patent US 9,592,229
Granted Patent B2
US 9,592,229 · App. 14/382,546 · Granted Mar 14, 2017

Potent anticancer activity via dual compound activation

Inventors: Paul J. Hergenrother (Champaign, IL); Rachel C. Botham (Champaign, IL); Timothy M. Fan (Mahomet, IL); Mark J. Gilbert (Seattle, WA); Michael K. Handley (Windsor, CO); Theodore M. Tarasow (San Ramon, CA)
Assignees: The Board of Trustees of the University of Illinois; Vanquish Oncology, Inc.
A61K31/495A61K31/437A61K47/40A61K9/008A61K9/0019A61K9/2054A61K9/4858
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Quick Facts
Patent No.
US 9,592,229
App. No.
14/382,546
Granted
Mar 14, 2017
Kind
B2
Abstract

The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods the use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.

Claims (33)

1. A composition comprising (a) a compound of Formula (I):

wherein R is H or Me;

(b) the compound PAC-1:

and (c) a pharmaceutically acceptable diluent, excipient, or carrier.

2. The composition of claim 1 wherein R of Formula (I) is H.

3. The composition of claim 1 wherein R of Formula (I) is Me.

4. The composition of claim 1 wherein the carrier comprises water and optionally a buffer, a cyclodextrin, or a combination thereof.

5. The composition of claim 4 wherein the carrier comprises a cyclodextrin wherein the cyclodextrin is 2-hydroxypropyl-β-cyclodextrin.

6. A method of inhibiting the growth or proliferation of cancer cells comprising contacting cancer cells with an effective amount of a composition of claim 1 , thereby inhibiting the growth or proliferation of the cancer cells.

7. The method of claim 6 wherein the cancer cells are cells of anal cancer, bladder cancer, breast cancer, cervical cancer, colorectal cancer, gastric cancer, head and neck cancer, leukemia, lung cancer Hodgkin's lymphoma, Non-Hodgkin's lymphoma, malignant lymphoma, neuroblastomas, ophthalmic cancer, osteogenic carcinomas, ovarian cancer, prostate cancer, renal cancer melanoma, soft tissue sarcomas, thyroid cancer, or Wilms' tumor.

8. The method of claim 6 wherein the cancer cells are breast cancer cells, leukemia cells, or lymphoma cells.

9. A method of activating procaspase-3 to caspase-3 comprising contacting the procaspase-3 with a composition of claim 1 .

10. The method of claim 9 wherein the contacting is in vitro.

11. The method of claim 9 wherein the contacting is in vivo.

12. A method of potentiating the activity of a compound of Formula (I):

wherein R is H or Me;

comprising contacting a cancer cell with a combination of the compound of Formula I and an effective activating amount of PAC-1:

wherein the PAC-1 potentiates the activity of the compound of Formula (I) toward the cancer cell.

13. A method of inducing apoptosis in a cancer cell comprising contacting the cancer cell with an effective amount of a compound of Formula (I):

wherein R is H or Me;

and an effective amount of the compound PAC-1:

wherein apoptosis is thereby induced in the cancer cell.

14. The method of claim 13 wherein the cancer cell is contacted with the compound of Formula (I) and the PAC-1 concurrently.

15. The method of claim 13 wherein the cancer cell is contacted with the compound of Formula (I) prior to contacting the cancer cell with PAC-1.

16. The method of claim 13 wherein the cancer cell is contacted with PAC-1 prior to contacting the cancer cell with the compound of Formula (I).

17. A method of inhibiting cancer, arresting cancer, relieving cancer, reversing the progression of cancer, reversing the severity of cancer, and/or therapeutically treating cancer, in a patient in need thereof comprising administering to the patient, concurrently or sequentially, a therapeutically effective amount of a compound of Formula (I):

wherein R is H or Me;

and an effective amount of the compound PAC-1:

wherein the cancer is breast cancer, leukemia, or lymphoma.

18. The method of claim 17 wherein the compound of Formula (I) and the compound PAC-1 are administered concurrently.

19. The method of claim 17 wherein the compound of Formula (I) and the compound PAC-1 are administered sequentially.

20. The method of claim 19 wherein the compound of Formula (I) is administered before the compound PAC-1.

21. The method of claim 19 wherein the compound of Formula (I) is administered after the compound PAC-1.

Assignments (3)
CONFIRMATORY LICENSE Recorded Jun 8, 2017
From: UNIVERSITY OF ILLINOIS AT URBANA-CHAMPAIGN
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 042732/0303 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 6, 2014
From: GILBERT, MARK J.; HANDLEY, MICHAEL K.; TARASOW, THEODORE M.
To: VANQUISH ONCOLOGY, INC.
Reel/Frame 033892/0252 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 6, 2014
From: HERGENROTHER, PAUL J.; BOTHAM, RACHEL C.; FAN, TIMOTHY M.
To: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
Reel/Frame 033892/0258 →
Continuity (2)
Provisional Application 61605819 · Mar 2, 2012
Related Publication 20150099759A1 · Apr 9, 2015