# US 8,772,259 B2 · Aptamer to FGF2 and use thereof

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- Number: US 8,772,259 B2
- Document ID: US8772259B2
- Status: Granted
- Kind: B2
- Application number: 13/578,023
- Filed: 2011-02-10
- Published: 2013-02-14
- Granted: 2014-07-08
- Earliest claimed: 2010-02-12
- Assignees: Ribomic Inc.
- Applicants: Yoshikazu Nakamura; Akira Ishiguro; Maiko Sakamoto
- Inventors: Yoshikazu Nakamura; Akira Ishiguro; Maiko Sakamoto
- Web page: https://patentgrep.com/patent/US8772259B2

## CPC

- C12N 15/115: Aptamers, i.e. nucleic acids binding a target molecule specifically and with high affinity without hybridising therewith {; Nucleic acids binding to non-nucleic acids, e.g. aptamers}
- 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 31/712: Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 19/00: Drugs for skeletal disorders
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- C12N 2310/16: Aptamers
- C12N 2310/322: 2'-R Modification
- C12N 2310/344: Position-specific modifications, e.g. on every purine, at the 3'-end
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- 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

Provided are an aptamer having an inhibitory activity on FGF2; a complex containing an aptamer having a binding activity or an inhibitory activity on FGF2, and a functional substance (e.g., affinity substance, labeling substance, enzyme, drug delivery vehicle, or drug and the like); a medicament, diagnostic reagent or label containing an aptamer having a binding activity or an inhibitory activity on FGF2, or a complex containing said aptamer and a functional substance; and the like.

## Claims

### Claim 1

An aptamer that binds to FGF2, which inhibits binding of FGF2 and an FGF2 receptor but does not inhibit binding of FGF1 and an FGF1 receptor, which comprises the sequence shown by SEQ ID NO: 36.

### Claim 2 (depends on 1)

The aptamer according to claim 1, wherein a pyrimidine nucleotide of the aptamer is a modified nucleotide.

### Claim 3

An aptamer that binds to FGF2, which inhibits binding of FGF2 and an FGF2 receptor but does not inhibit binding of FGF1 and an FGF1 receptor, which comprises:
a nucleotide sequence selected from SEQ ID NOs: 36 and 43-57 wherein uracil may be thymine, and wherein,
(i) the 2′-position of ribose of each pyrimidine nucleotide of the aptamer is the same or different and is a fluorine atom, or is substituted by a hydrogen atom, a hydroxy group and or a methoxy group,
(ii) the 2′-position of ribose of each purine nucleotide of the aptamer is the same or different, and is a hydroxy group, or is substituted by a hydrogen atom, a methoxy group or a fluorine atom.

### Claim 4 (depends on 3)

The aptamer according to claim 3, wherein a nucleotide of the aptamer is modified.

### Claim 5 (depends on 1)

A complex comprising the aptamer according to claim 1 and a functional substance, wherein the functional substance is an affinity substance, a labeling substance, an enzyme, a drug delivery vehicle or a drug.

### Claim 6 (depends on 3)

A medicament comprising the aptamer according to claim 3 or a complex comprising the aptamer according to claim 3 and a functional substance, wherein the functional substance is an affinity substance, a labeling substance, an enzyme, a drug delivery vehicle or a drug.

### Claim 7 (depends on 6)

The medicament according to claim 6, which is for the treatment or prophylaxis of cancer, an autoimmune disease, an allergic disease, an inflammatory disease, heart dysplasia, angiodysplasia or skeletal dysplasia.

### Claim 8 (depends on 3)

A diagnostic reagent comprising the aptamer according to claim 3 or a complex comprising the aptamer according to claim 3 and a functional substance.