# US 2021/0220310 A1 · Pharmaceutical compositions for the treatment of cancer

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- Number: US 2021/0220310 A1
- Document ID: US20210220310A1
- Status: Published application
- Kind: A1
- Application number: 17/055,182
- Filed: 2019-05-21
- Published: 2021-07-22
- Earliest claimed: 2018-05-22
- Assignees: Seleq Oy
- Applicants: Seleq Oy
- Inventors: Mikael Björnstedt; Adnane Achour; Hugh Salter; Tatiana Sandalova
- Web page: https://patentgrep.com/patent/US20210220310A1

## CPC

- A61K 31/00: Medicinal preparations containing organic active ingredients
- A61K 31/198: Alpha-amino acids, e.g. alanine or edetic acid [EDTA] (betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00)
- A61K 9/127: Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
- A61K 9/51: Nanocapsules; {Nanoparticles; (nanotubes A61K9/0092; polymeric micelles A61K9/1075; polymersomes A61K9/1273; pure drug nanoparticles A61K9/14; drug nanoparticles with adsorbed surface modifiers A61K9/141; conjugates, e.g. between drug and non-active nanoparticles, A61K47/50; preparations for in vivo diagnosis A61K49/00; with radioactive substances A61K51/00)}
- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61K 31/405: Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
- A61K 33/04: Sulfur, selenium or tellurium; Compounds thereof
- A61K 38/45: Transferases (2)
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 48/0058: {Nucleic acids adapted for tissue specific expression, e.g. having tissue specific promoters as part of a contruct}
- A61K 48/0066: {Manipulation of the nucleic acid to modify its expression pattern, e.g. enhance its duration of expression, achieved by the presence of particular introns in the delivered nucleic acid}
- A61P 35/00: Antineoplastic agents
- C12Y 206/01007: Kynurenine--oxoglutarate transaminase (2.6.1.7)
- 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
- C12Y: ENZYMES

## Abstract

A chemotherapeutically active pharmaceutical composition includes at least one pharmaceutically acceptable seleno amino acid derivative compound for use in the treatment of liver or pancreas cancer, wherein the chemotherapeutically active pharmaceutical composition is used in combination with an agent capable of increasing cytotoxicity of the seleno amino acid derivative compound.

## Claims

### Claim 1

A chemotherapeutically active pharmaceutical composition comprising at least one pharmaceutically acceptable seleno amino acid derivative compound for use in the treatment of liver or pancreas cancer, wherein said chemotherapeutically active pharmaceutical composition is used in combination with an agent capable of increasing cytotoxicity of the seleno amino acid derivative compound.

### Claim 2 (depends on 1)

A chemotherapeutically active pharmaceutical composition for use according to claim 1, wherein the seleno amino acid derivative compound is selenocysteine, selenocystine, selenium-methyl-L-selenocysteine or a pharmaceutically acceptable salt or ester thereof.

### Claim 3 (depends on 1)

A chemotherapeutically active pharmaceutical composition for use according to claim 1, wherein selenium amount in the at least one pharmaceutically acceptable seleno amino acid derivative compound ranges between 80-1200 micrograms.

### Claim 4 (depends on 2)

A chemotherapeutically active pharmaceutical composition for use according to claim 2, wherein the seleno amino acid derivative is selenium-methyl-L-selenocysteine and wherein selenium-methyl-L-selenocysteine is dosed between 200-2400 micrograms per day.

### Claim 5 (depends on 1)

A chemotherapeutically active pharmaceutical composition for use according to claim 1, wherein said agent capable of increasing cytotoxicity of the seleno amino acid derivative compound is selected from a group consisting of: indole pyruvic acid, phenyl pyruvic acid, α-keto-γ-methylthiobutyrate, dimethyl-2-oxoglutarate, L-phenylalanine, pyridoxal 5′-phosphate hydrate, L-tryptophan, homoserine, DL-propargylglycine, 2-amino-2-methyl-1,3-propanediol, N—N-dimethyl formamide and 3-indoleacetic acid.

### Claim 6 (depends on 1)

A chemotherapeutically active pharmaceutical composition for use according to claim 1, wherein said agent capable of increasing cytotoxicity of the seleno amino acid derivative compound is a mutant kynurenine aminotransferase I or III proteins having increased beta-elimination activity or a nucleic acid sequence coding for such a mutant protein.

### Claim 7 (depends on 6)

A chemotherapeutically active pharmaceutical composition for use according to claim 6, wherein said agent capable of increasing cytotoxicity of the seleno amino acid derivative compound is a mutant kynurenine aminotransferase I protein having a Tyr to His substitution at position 101 or a His to Phe substitution at position 279.

### Claim 8 (depends on 1)

A chemotherapeutically active pharmaceutical composition for use according to claim 1, wherein said agent capable of increasing cytotoxicity of the seleno amino acid derivative compound is administered separately.

### Claim 9 (depends on 1)

A chemotherapeutically active pharmaceutical composition for use according to claim 1, wherein said chemotherapeutically active pharmaceutical composition is used in combination with
a) indole pyruvic acid or phenyl pyruvic acid, and
b) a mutant kynurenine aminotransferase I protein having a Tyr to His substitution at position 101 or a His to Phe substitution at position 279, or a nucleic acid sequence coding for such a mutant kynurenine aminotransferase I protein.

### Claim 10 (depends on 6)

A chemotherapeutically active pharmaceutical composition for use according to claim 6, wherein the nucleic acid is controlled by the addition of microRNA switches regulating the expression of the nucleic acid such that it is down-regulated in normal tissue relative to tumorous tissue within the target organ.

### Claim 11 (depends on 6)

A chemotherapeutically active pharmaceutical composition for use according to claim 6, wherein the nucleic acid is delivered as a modified RNA encapsulated in a nanoparticle formulation trophic for the target organ and/or tumor.

### Claim 12 (depends on 6)

A chemotherapeutically active pharmaceutical composition for use according to claim 6, wherein the nucleic acid is delivered as an mRNA encapsulated within an exosome trophic for the target organ and/or tumor.

### Claim 13 (depends on 6)

A chemotherapeutically active pharmaceutical composition for use according to claim 6, wherein the nucleic acid is delivered via a viral construct trophic for the target organ.

### Claim 14 (depends on 1)

A chemotherapeutically active pharmaceutical composition for use according to claim 1, wherein the chemotherapeutically active pharmaceutical composition is one of an instant release formulation, a sustained release formulation, a controlled release formulation.

### Claim 15 (depends on 1)

A chemotherapeutically active pharmaceutical composition for use according to claim 1, wherein the chemotherapeutically active pharmaceutical composition is in an orally, intramuscularly or intravenously administrable form.

### Claim 16 (depends on 1)

A chemotherapeutically active pharmaceutical composition for use according claim 1, wherein the use of the chemotherapeutically active pharmaceutical composition comprises at least one of: a single dose, multiple uniform dosages, discrete dosages.

### Claim 17

A mutant kynurenine aminotransferase I or III protein having increased beta-elimination activity or a nucleic acid sequence coding for such a mutant protein.

### Claim 18

A method for treating liver or pancreas cancer, comprising administration of:
a) a chemotherapeutically active pharmaceutical composition comprising at least one pharmaceutically acceptable seleno amino acid derivative compound, and
b) an agent capable of increasing cytotoxicity of the seleno amino acid derivative compound.

### Claim 19 (depends on 18)

A method according to claim 18, having the further features.
