# US 10,946,020 B2 · Compositions and methods for treating cancer

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- Number: US 10,946,020 B2
- Document ID: US10946020B2
- Status: Granted
- Kind: B2
- Application number: 16/091,000
- Filed: 2017-04-06
- Published: 2019-02-28
- Granted: 2021-03-16
- Earliest claimed: 2016-04-06
- Assignees: University of Virginia Patent Foundation
- Applicants: University of Virginia Patent Foundation
- Inventors: Benjamin Purow; Desiree Floyd; Inan Olmez; Thurl E. Harris, Jr.; Salome Boroda
- Web page: https://patentgrep.com/patent/US10946020B2

## CPC

- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 31/4706: 4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 35/00: Antineoplastic agents
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- 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

## Abstract

Ritanserin is shown to be an inhibitor of diacylglycerol kinase alpha (DGKα) and to be cytotoxic to glioblastoma and melanoma cells. Ritanserin treatment also provides chemo- and radiosensitization in cancer cells, prolonged survival in mouse models of glioblastoma, decreased melanoma tumor burden in mice, and shows synergistic cytotoxic effects with temozolomide and chloroquine, both singly and in combination. DGKα inhibition with ritanserin shows particular toxicity to the treatment-resistant mesenchymal subtype in glioblastoma and other cancers.

## Claims

### Claim 1

A method for treating a cancer in a subject in need thereof, wherein the method comprises administering to the subject a therapeutically effective amount of ritanserin, wherein the cancer is selected from the group consisting of mesenchymal cancer, melanoma and glioblastoma.

### Claim 2 (depends on 1)

The method of claim 1, wherein the method further comprises administering at least one second treatment to the subject.

### Claim 3 (depends on 2)

The method of claim 2, wherein the at least one second treatment is selected from the group consisting of a surgical resection of a tumor, radiotherapy, immunotherapy, alternating electric field therapy, and chemotherapy.

### Claim 4 (depends on 2)

The method of claim 2, wherein the method comprises administering to the subject at least one second treatment selected from the group consisting of temozolomide (TMZ), chloroquine, bevacizumab, imatinib, radiation, and an immunotherapeutic agent.

### Claim 5 (depends on 2)

The method of claim 2, wherein the method comprises administering to the subject at least two second treatments, wherein the at least two second treatments have synergistic activity with each other.

### Claim 6 (depends on 5)

The method of claim 5, wherein the at least two second treatments are TMZ and chloroquine.

### Claim 7 (depends on 1)

The method of claim 1, wherein the ritanserin is administered orally to the subject.

### Claim 8 (depends on 1)

The method of claim 1, wherein the subject is human.

### Claim 9

A method of inducing chemo- or radiosensitivity in a subject undergoing or scheduled to undergo treatment with a chemotherapeutic agent or radiation to treat a disease or disorder treatable thereby, the method comprising administering ritanserin to the subject, wherein the disease or disorder is selected from the group consisting of mesenchymal cancer.

### Claim 10 (depends on 9)

The method of claim 9, wherein administering the ritanserin is performed prior to and/or concurrently with the administration of a chemotherapeutic agent.

### Claim 11 (depends on 9)

The method of claim 9, wherein administering the ritanserin is performed prior to and/or concurrently with the administration of radiation.

### Claim 12

A method for inhibiting a cancer in a subject in need thereof, wherein the method comprises administering to the subject a therapeutically effective amount of ritanserin, wherein the cancer is a melanoma or a glioblastoma.