# US 12,109,212 B2 · Methods of treating cancer having an active Wnt/β-catenin pathway

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- Number: US 12,109,212 B2
- Document ID: US12109212B2
- Status: Granted
- Kind: B2
- Application number: 16/550,993
- Filed: 2019-08-26
- Published: 2020-04-02
- Granted: 2024-10-08
- Earliest claimed: 2012-03-30
- Assignees: Dana-Farber Cancer Institute, Inc.
- Applicants: Dana-Farber Cancer Institute, Inc.
- Inventors: William C. Hahn; Joseph Rosenbluh
- Web page: https://patentgrep.com/patent/US12109212B2

## CPC

- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 35/00: Antineoplastic agents
- C07K 14/47: from mammals
- C07K 14/4702: {Regulators; Modulating activity}
- C07K 14/4747: {Apoptosis related proteins}
- C12N 15/1135: {against oncogenes or tumor suppressor genes}
- G01N 33/5017: {for testing neoplastic activity}
- C12N 2310/14: interfering nucleic acids [NA]
- C12N 2310/3233: Morpholino-type ring
- C12N 2310/531: Stem-loop; Hairpin
- G01N 2500/10: involving cells
- 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
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

The present invention provides methods of treating a subject having a Wnt/beta-catenin active cancer by administering to said subject a compound that inhibits the expression or activity of YES1, BIRC5 or BCL2L1, a compound that inhibits YAP1-beta-catenin complex formation, a compound that inhibits YAP1-beta-catenin complex binding to DNA, a compound that inhibits YAP1-beta-catenin-TBX5 complex formation, or any combination thereof. The compound can be, for example, a nucleic acid, a peptide, an antibody or a small molecule. Methods of screening for therapeutic targets for treating cancer are included.

## Claims

### Claim 1

A method of reducing YES1 activity thereby treating a Wnt/β-catenin active cancer in a human subject in need thereof, the method consisting of administering to the human subject a therapeutic amount of dasatinib effective to reduce YES1 activity, wherein the Wnt/β-catenin active cancer is colon cancer, breast cancer, lung cancer, leukemia, prostate cancer, skin cancer, liver cancer, ovarian cancer, brain cancer, or parathyroid cancer.

### Claim 2

A method of reducing YES1 activity thereby treating a Wnt/β-catenin active cancer in a human subject in need thereof, the method consisting of administering to the human subject a therapeutic amount of dasatinib effective to reduce YES1 activity, wherein a level of β-catenin in the Wnt/β-catenin active cancer is unaffected upon administering the YES1 inhibitor.

### Claim 3 (depends on 2)

The method of claim 2, wherein the Wnt/β-catenin active cancer is colon cancer, breast cancer, lung cancer, leukemia, prostate cancer, skin cancer, liver cancer, ovarian cancer, brain cancer, or parathyroid cancer.

### Claim 4 (depends on 1)

The method of claim 1, wherein the mutational status of KRAS in the Wmt/β-catenin active cancer is normal.

### Claim 5 (depends on 1)

The method of claim 1, wherein the Wnt/β-catenin active cancer is colon cancer.

### Claim 6 (depends on 1)

The method of claim 1, wherein the Wnt/β-catenin active cancer is breast cancer.

### Claim 7 (depends on 1)

The method of claim 1, wherein the Wnt/β-catenin active cancer is lung cancer.

### Claim 8 (depends on 1)

The method of claim 1, wherein the Wnt/β-catenin active cancer is leukemia.

### Claim 9 (depends on 1)

The method of claim 1, wherein the Wnt/β-catenin active cancer is prostate cancer.

### Claim 10 (depends on 1)

The method of claim 1, wherein the Wnt/β-catenin active cancer is skin cancer.

### Claim 11 (depends on 1)

The method of claim 1, wherein the Wnt/β-catenin active cancer is liver cancer.

### Claim 12 (depends on 1)

The method of claim 1, wherein the Wnt/β-catenin active cancer is ovarian cancer.

### Claim 13 (depends on 1)

The method of claim 1, wherein the Wnt/β-catenin active cancer is brain cancer.

### Claim 14 (depends on 1)

The method of claim 1, wherein the Wnt/β-catenin active cancer is parathyroid cancer.