# US 2017/0281576 A1 · Treatment of cancer with specific rxr agonists

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- Number: US 2017/0281576 A1
- Document ID: US20170281576A1
- Status: Published application
- Kind: A1
- Application number: 15/629,591
- Filed: 2017-06-21
- Published: 2017-10-05
- Earliest claimed: 2005-09-30
- Assignees: Io Therapeutics, Inc.
- Applicants: IO Therapeutics, Inc.
- Inventors: Roshantha A. Chandraratna
- Web page: https://patentgrep.com/patent/US20170281576A1

## CPC

- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61K 31/282: Platinum compounds
- A61K 31/337: having four-membered rings, e.g. taxol
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 35/00: Antineoplastic agents
- C12Q 1/6886: for cancer (immunoassay for cancer G01N33/575)
- C12Q 2600/158: Expression markers
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C12Q: MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS (immunoassay G01N33/53); COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES

## 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

### Claim 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 the Retinoic Acid Receptor (RAR) activating threshold and at or above the RXR effective dose, the RXR agonist has the 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 0.01 to about 100 mg/m2/day.

### Claim 2 (depends on 1)

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.

### Claim 3 (depends on 2)

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

### Claim 4 (depends on 3)

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

### Claim 5 (depends on 1)

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

### Claim 6 (depends on 1)

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.

### Claim 7 (depends on 6)

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.

### Claim 8 (depends on 1)

The method according to claim 1, wherein the dose of the RXR agonist is from about 0.1 to about 10 mg/m2/day.

### Claim 9 (depends on 1)

The method according to claim 1, wherein the dose of the RXR agonist is from about 0.5 to about 2 mg/m2/day.

### Claim 10 (depends on 1)

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

### Claim 11 (depends on 1)

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

### Claim 12 (depends on 1)

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