# US 7,745,419 B2 · Pharmaceutical composition for treating cancer

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- Number: US 7,745,419 B2
- Document ID: US7745419B2
- Status: Granted
- Kind: B2
- Application number: 12/234,271
- Filed: 2008-09-19
- Published: 2009-03-26
- Granted: 2010-06-29
- Earliest claimed: 2007-09-21
- Assignees: Korea University Industrial & Academic Collaboration Foundation
- Inventors: Yu-Kyoung Oh; Ga Yong Shim; Sang-Hee Kim
- Web page: https://patentgrep.com/patent/US7745419B2

## CPC

- A61K 31/7105: Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
- A61K 9/1272: comprising non-phosphatidyl surfactants as bilayer-forming substances, e.g. cationic lipids or non-phosphatidyl liposomes coated or grafted with polymers (lipids as modifying agents {A61K47/543})
- A61P 35/00: Antineoplastic agents
- C12N 15/113: Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; {Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing (when used in plants C12N15/8218)}
- C12N 2310/14: interfering nucleic acids [NA]
- 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
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

The present invention provides a small interfering RNA (siRNA) that is capable of inhibiting intracellular expression of Wnt1 through complementary binding to a Wnt1 transcript (mRNA transcript) base sequence and a pharmaceutical composition for treating cancer comprising the same. siRNA of the present invention which is complementary to a base sequence of a Wnt1 transcript (mRNA) provides apoptotic cancer cell death due to inhibition of expression of Wnt1 commonly expressed in cancer cells, by RNA-mediated interference (RNAi). Therefore, the composition of the present invention comprising the same can be used as an excellent anticancer drug.

## Claims

### Claim 1

A pharmaceutical composition comprising one or more small interfering RNAs (siRNAs) that are capable of inhibiting intracellular expression of Wnt1 through complementary binding to a Wnt1 transcript (mRNA transcript) base sequence as set forth in SEQ ID NO: 2.

### Claim 2 (depends on 1)

The composition of claim 1, wherein the siRNA is a chemically modified form.

### Claim 3 (depends on 1)

The composition of claim 1, which comprises the siRNA in the form of a complex with a nucleic acid delivery system.

### Claim 4 (depends on 3)

The composition of claim 3, wherein the nucleic acid delivery system is a cationic liposome.

### Claim 5 (depends on 4)

The composition of claim 4, wherein the cationic liposome includes at least one cationic lipid selected from the group consisting of 1,2-dioleoyl-sn-glycero-3-ethylphosphocholine (EDOPO), 1-palmitoyl-2-oleoyl-sn-glycero-3-ethylphosphocholine (EPOPO), 1,2-dimyristoyl-sn-glycero-3-ethylphosphocholine (EDMPC), 1,2-distearoyl-sn-glycero-3-ethylphosphocholine (SPC), 1,2-dipalmitoyl-sn-glycero-3-ethylphosphocholine (EDPPC), 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP), N-[1-(2,3-dioleyloxy)propyl]-N,N,N-trimethylammonium chloride (DOTMA) and 3β-[N-(N′,N′-dimethylaminoethane)-carbamoyl]cholesterol (DC-Cholesterol).

### Claim 6 (depends on 5)

The composition of claim 5, wherein the cationic liposome further includes at least one auxiliary lipid selected from the group consisting of 1,2-diacyl-sn-glycero-3-phosphoethanolamine (DOPE), 1,2-diphytanoyl-sn-glycero-3-phosphoethanolamine (DPhPE), 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), 1,2-dioleoyl-sn-glycero-3-[phospho-L-serine] (DOPS), 1,2-dioleoyl-sn-glycero-3-ethylphosphocholine (DO-Ethyl-PC), and cholesterol.

### Claim 7 (depends on 3)

The composition of claim 3, wherein the nucleic acid delivery system is a cationic polymer.

### Claim 8 (depends on 7)

The composition of claim 7, wherein the cationic polymer is selected from the group consisting of poly-L-lysine, poly-L-ornithine, poly-L-histidine, poly-L-arginine, bis(3-aminopropyl)terminated polytetrahydrofuran, polyacrylamide (PA), poly(α-[4-aminobutyl]-L-glycolic acid (PAGA), poly(2-aminoethyl propylene phosphate) (PPE-EA), cationic derivatives of cyclodextrin, poly(2-(dimethylamino)ethyl methacrylate (pDMAEMA), poly(4-vinylpyridine) (P4VP), O,O′-bis(2-aminopropyl)polypropylene glycol-block-polyethylene glycol-block-polypropylene glycol, chitosan, chitosan derivatives, polyethylenimine (PEI), polyethylenimine derivatives, polyamidoamine (PAMAM), fractured PAMAM and poly-N-ethyl-4-vinylpyridinium tribromide.

### Claim 9 (depends on 1)

The composition of claim 1, further comprising a cancer chemotherapeutic agent.

### Claim 10 (depends on 1)

The composition of claim 1, wherein the siRNA has a sense sequence of SEQ ID NO: 18 and an antisense sequence of SEQ ID NO: 19.

### Claim 11

An siRNA inhibiting expression of Wnt1 and having a sense sequence of SEQ ID NO: 18 and an antisense sequence of SEQ ID NO: 19.

### Claim 12 (depends on 1)

A method for treating cancer comprising administering to a subject in need thereof the composition of claim 1 in a pharmaceutically effective amount.

### Claim 13 (depends on 11)

A method for treating cancer comprising administering to a subject in need thereof the siRNA of claim 11 in a pharmaceutically effective amount.