# US 10,370,434 B2 · Methods and compositions for the treatment of cancer

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- Number: US 10,370,434 B2
- Document ID: US10370434B2
- Status: Granted
- Kind: B2
- Application number: 14/889,656
- Filed: 2014-05-07
- Published: 2016-05-05
- Granted: 2019-08-06
- Earliest claimed: 2013-05-07
- Assignees: Fundacio Privada Institut d'Investigacio Oncologica de Vall Hebron
- Applicants: Fundació Privada Institut D'Investigació OncolòGica De Vall Hebron
- Inventors: Laura Soucek; Marie-Eve Beaulieu
- Web page: https://patentgrep.com/patent/US10370434B2

## CPC

- C07K 14/82: Translation products from oncogenes
- A61K 38/08: Peptides having 5 to 11 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61K 38/10: Peptides having 12 to 20 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61K 39/0011: {Cancer antigens}
- A61K 39/001152: {Transcription factors, e.g. SOX or c-MYC}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 7/06: having 5 to 11 amino acids
- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- C07K 2319/00: Fusion polypeptide
- C07K 2319/09: containing a nuclear localisation signal
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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)
- 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
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The invention relates to a Myc dominant negative mutant, called Omomyc, for use in medicine and for use in the prevention and/or treatment of cancer. The invention also refers to a fusion protein comprising Omomyc and pharmaceutical composition thereof and their use in medicine and, in particular, for treatment of cancer.

## Claims

### Claim 1

A method for treatment of cancer that comprises administering to a subject in need thereof a therapeutically effective amount of a polypeptide of SEQ ID NO: 1 or a functionally equivalent variant thereof having a degree of identity with respect to SEQ ID NO: 1 greater than 70% and wherein the functionally equivalent variant is a polypeptide which results from an insertion or addition of one amino acid and/or from a deletion of one or more amino acids and/or from a conservative substitution of one or more amino acids with respect to the polypeptide of SEQ ID NO: 1, and wherein the method does not involve the administration of the nucleic acid encoding Omomyc or the functionally equivalent variant thereof.

### Claim 2

A conjugate comprising:
(i) a polypeptide of SEQ ID NO: 1 or a functionally equivalent variant thereof having a degree of identity with respect to SEQ ID NO: 1 greater than 70%, and
(ii) a chemical moiety that facilitates cellular uptake of the polypeptide or of the functionally equivalent variant thereof.

### Claim 3 (depends on 2)

The conjugate according to claim 2, wherein the chemical moiety that facilitates cellular uptake of the polypeptide or of the functionally equivalent variant thereof is a cell penetrating peptide and wherein said cell penetrating peptide and said polypeptide or the functionally equivalent variant thereof form a fusion protein.

### Claim 4 (depends on 3)

The conjugate according to claim 3, wherein the cell-penetrating peptide sequence is selected from the group consisting of GRKKRRQRRR (SEQ ID NO: 28) and RRRRRRLR (SEQ ID NO: 29).

### Claim 5 (depends on 2)

The conjugate according to claim 2, further comprising a nuclear-localization signal.

### Claim 6 (depends on 5)

The conjugate according to claim 5, wherein the nuclear localization signal is selected from the group consisting of PKKKRKV (SEQ ID NO: 39), PAAKRVKLD (SEQ ID NO: 50) and KRPAATKKAGQAKKKK (SEQ ID NO: 40).

### Claim 7 (depends on 2)

The conjugate according to claim 2, wherein the functionally equivalent variant of the polypeptide of SEQ ID NO: 1 is selected from the group consisting of SEQ ID NO: 47 and SEQ ID NO: 48.

### Claim 8 (depends on 2)

A pharmaceutical composition comprising a pharmaceutically active amount of the conjugate according to claim 2 and a pharmaceutically acceptable excipient.

### Claim 9 (depends on 2)

A method for treatment of cancer that comprises administering to a subject in need thereof a therapeutically effective amount of the conjugate according to claim 2.

### Claim 10 (depends on 2)

A composition comprising, together or separately:
(i) a polypeptide of SEQ ID NO: 1, a functionally equivalent variant thereof having a degree of identity with respect to SEQ ID NO: 1 greater than 70% or a conjugate according to claim 2, and
(ii) an antitumoral agent.

### Claim 11 (depends on 10)

The composition according to claim 10, wherein the antitumoral agent is selected from the group consisting of a cytotoxic agent, an antiangiogenic agent and an antimetastatic agent.

### Claim 12 (depends on 10)

The composition according to claim 10, wherein the functionally equivalent variant of the polypeptide of SEQ ID NO: 1 is selected from the group consisting of SEQ ID NO: 47 and SEQ ID NO: 48.

### Claim 13 (depends on 10)

A pharmaceutical composition comprising a pharmaceutically active amount of the composition according to claim 10 and a pharmaceutically acceptable excipient.

### Claim 14 (depends on 10)

A method for treatment of cancer that comprises administering to a subject in need thereof a therapeutically effective amount of a composition according to claim 10.

### Claim 15 (depends on 13)

A method for treatment of cancer that comprises administering to a subject in need thereof a therapeutically effective amount of the pharmaceutical composition according to claim 13.
