IP Library Granted Patent US 10,039,731
Granted Patent B2
US 10,039,731 · App. 15/629,591 · Granted Aug 7, 2018

Treatment of cancer with specific RXR agonists

Inventor: Roshantha A. Chandraratna (San Juan Capistrano, CA)
Assignee: Io Therapeutics, Inc.
A61K31/192A61K31/282A61K31/337A61K45/06C12Q1/6886C12Q2600/158
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Quick Facts
Patent No.
US 10,039,731
App. No.
15/629,591
Granted
Aug 7, 2018
Kind
B2
Abstract

A method of treating cancer is disclosed comprising administering to a patient in need of such treatment a RXR agonist at a level below the RAR activating threshold and at or above the RXR effective dose.

Claims (13)

1. A method of treating colorectal cancer comprising administering to a patient in need of such treatment a retinoid X receptor (RXR) agonist at a dose below its Retinoic Acid Receptor (RAR) activating threshold and at or above its RXR effective dose, the RXR agonist has a chemical structure

where R is H, lower alkyl or 1 to 6 carbons, or a pharmaceutically acceptable salt of the compound, and the dose of the RXR agonist is from about 1 to about 20 mg/m 2 /day.

2. The method according to claim 1 , wherein the RAR activating threshold and the RXR effective dose for the patient is determined by dosing the patient with increasing concentrations of a RXR agonist to until the RXR effective dose and the RAR activating threshold are reached.

3. The method according to claim 2 , wherein the RXR effective dose is determined by measuring a reduction of the patient's TSH levels or at least one RAR biomarker expressed by the patient.

4. The method according to claim 3 , wherein the RAR biomarker is selected from the group consisting of CYP26 level, CRBPI level and combinations thereof.

5. The method according to claim 1 , further comprising measuring the patient's C max of the RXR agonist, and adjusting the dose to maintain the patient's C max at an optimal level.

6. The method according to claim 1 , further comprising treating the patient with at least one other agent selected from the group consisting of anti-cancer agents, triglyceride lowering agents and TSH modulating agents.

7. The method according to claim 6 , wherein the anti-cancer agent is selected from the group consisting of a platinum-based compounds, cytotoxic drugs, and mixtures thereof.

8. The method according to claim 1 , wherein the dose of the RXR agonist is from about 1 to about 10 mg/m 2 /day.

9. The method according to claim 1 , wherein the dose of the RXR agonist is from about 10 to about 20 mg/m 2 /day.

10. The method according to claim 1 , wherein the RXR agonist is 3,7-di methyl-6(S),7(S)-methano,7-[1,1,4,4-tetramethyl-1,2,3,4-tetrahydronaphth-7-yl]2(E),4(E) heptadienoic acid.

11. The method according to claim 1 , wherein the colorectal cancer is colon cancer.

12. The method according to claim 1 , wherein the colorectal cancer is rectal cancer.

Assignments (4)
CHANGE OF NAME Recorded Oct 5, 2017
From: IO THERAPEUTICS, LLC
To: IO THERAPEUTICS, INC.
Reel/Frame 043798/0069 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 22, 2017
From: CHANDRARATNA, ROSHANTHA A.
To: VITAE PHARMACEUTICALS, INC.
Reel/Frame 042787/0596 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 22, 2017
From: VITAE PHARMACEUTICALS, INC.
To: NURX PHARMACEUTICALS, INC.
Reel/Frame 042787/0705 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 22, 2017
From: NURX PHARMACEUTICALS, INC.
To: IO THERAPEUTICS, LLC
Reel/Frame 042787/0877 →
Continuity (6)
Continuation 14994031 · Jan 12, 2016
Continuation 13323510 · Dec 12, 2011
Division 12079938 · Mar 28, 2008
Continuation In Part PCTUS2006038252 · Oct 2, 2006
Provisional Application 60722264 · Sep 30, 2005
Related Publication 20170281576A1 · Oct 5, 2017
Cited By (1)
US 12,383,521