# US 2013/0156850 A1 · Apo a-i mimetic peptides and methods of treatment

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 2013/0156850 A1
- Document ID: US20130156850A1
- Status: Published application
- Kind: A1
- Application number: 13/774,464
- Filed: 2013-02-22
- Published: 2013-06-20
- Earliest claimed: 2007-09-20
- Assignees: Abbott Cardiovascular Systems Inc.
- Inventors: Katsuyuki Murase; Li Zhao; Irina Astafieva; Paul M. Consigny
- Web page: https://patentgrep.com/patent/US20130156850A1

## CPC

- A61K 38/17: from animals; from humans {(enzyme inhibitors A61K38/005)}
- A61K 31/661: Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion {or mevinphos}
- A61K 38/10: Peptides having 12 to 20 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61K 38/1709: {from mammals}
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- 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

A method including advancing a delivery device through a lumen of a blood vessel to a particular region in the blood vessel; and introducing a synthetic apolipoprotein A-1 (Apo A-I) mimetic peptide into a wall of the blood vessel at the particular region, wherein the peptide has a property that renders the peptide effective in reverse cholesterol transport. A composition including a synthetic apolipoprotein A-I (Apo A-I) mimetic peptide, or combination of an Apo A-I synthetic peptide and an Acyl CoA cholesterol: acyltransferase (ACAT) inhibitor in a form suitable for delivery into a blood vessel, the peptide including an amino acid sequence in an order reverse to an order of an endogenous Apo A-I related peptide. A composition including an apolipoprotein A-1 (Apo A-I) synthetic peptide in a form suitable for delivery into a blood vessel, the peptide including an amino acid backbone that has less amino acid residues relative to endogenous Apo A-I and a chimera of helix 1 and helix 9 of Apo A-I.

## Claims

### Claim 1

A composition comprising:
an apolipoprotein A-I (Apo A-I) synthetic mimetic peptide in a form suitable for delivery into a blood vessel, wherein the Apo A-I synthetic mimetic peptide is selected from the group consisting of:
(i) An 18 amino acid peptide,
(SEQ ID NO: 1)
DWFKAFYDKVAEKFKEAF;
(ii) An 18 amino acid peptide,
(SEQ ID NO: 2)
DWLKAFYDKVAEKLKEAF;
(iii) A 33 amino acid peptide,
(SEQ ID NO: 3)
PALEDLRQGLLPVLESFKVFLSALEEYTKKLNTQ;
(SEQ ID NO: 4)
(iv) Ac-DWFKAFYDKVAEKFKEAF-NH2;
and
(SEQ ID NO: 5)
(v) Ac-PALEDLRQGLLPVLESFKVFLSALEEYTKKLNTQ-NH2.

### Claim 2 (depends on 1)

The composition of claim 1 further comprising:
a bioactive attached to a spatially distinct hydrophobic or charged domain of the mimetic peptide wherein the bioactive comprises at least one of a statin including atorvastatin, cerivastatin, fluvastatin, lovastatin, mevastatin, pitavastatin, pravastatin, rosuvastatin, and simvastatin; nitroglycerin; Acyl CoA cholesterol:acyltransferase (ACAT) inhibitor; anti-inflammatory steroids including corticosteroids; singlet oxygen generators including porphyrins and sub-classes thereof, including texaphyrins, sapphyrins, pentaphyrins, porphycenes and porphyrin vinylogues in addition to tin ethyl etiopurpurin, rostaporfin, and verteporfin; phthalocyanines; or immunosuppressant or anti-cancer agents including paclitaxel, sirolimus, everolimus, ABT-578, and eptoposide.

### Claim 3 (depends on 1)

The composition of claim 1 further comprising:
a carrier selected from the group consisting of a liposome, a polymerosome, a micelle, a particle, a gel, a microbubble, a precipitated peptide particle, a porous glass particle, and a rod.

### Claim 4 (depends on 3)

The composition of claim 3, further comprising, a hydrophobic sacrificial coating on the carrier wherein the coating is capable of mitigating premature peptide release upon oral delivery thereof.

### Claim 5 (depends on 3)

The composition of claim 3, further comprising, poly(ethylene glycol) bonded to the surface of the carrier.

### Claim 6 (depends on 1)

The composition of claim 1 wherein the peptide comprises a chimera of two alpha helices of endogenous Apo A-I.

### Claim 7

A composition comprising:
an apolipoprotein A-I (Apo A-I) synthetic mimetic peptide in a form suitable for delivery into a blood vessel, the mimetic peptide comprising an amino acid backbone having less amino acid residues relative to an amino acid backbone of endogenous Apo A-I peptide, wherein the mimetic peptide is a combination of helix 1 and helix 9 of endogenous Apo A-I peptide and comprises an amino acid sequence selected from the group consisting of SEQ ID NO: 9, SEQ ID NO: 10 and a racemate thereof.

### Claim 8 (depends on 7)

The composition of claim 7 wherein the combination is a 1/9 chimera from the α-carboxyl group.

### Claim 9 (depends on 7)

The composition of claim 7 wherein the combination is a 9/1 chimera from the α-carboxyl group.

### Claim 10 (depends on 7)

The composition of claim 7 wherein the mimetic peptide comprises an amino acid sequence in an order reverse to an amino acid sequence order of an endogenous Apo A-I peptide.

### Claim 11 (depends on 7)

The composition of claim 7 wherein the mimetic peptide is a racemate of SEQ ID NO: 9 or SEQ ID NO: 10.