# US 2019/0169307 A1 · Glycoprotein v inhibitors for use as coagulants

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- Number: US 2019/0169307 A1
- Document ID: US20190169307A1
- Status: Published application
- Kind: A1
- Application number: 16/065,300
- Filed: 2016-12-23
- Published: 2019-06-06
- Earliest claimed: 2015-12-23
- Assignees: Julius-Maximilians-UniversitäT WüRzburg
- Applicants: Julius-Maximilians-UniversitäT WüRzburg
- Inventors: Bernhard NIESWANDT; Sarah BECK; David STEGNER
- Web page: https://patentgrep.com/patent/US20190169307A1

## CPC

- C07K 16/2896: {against molecules with a "CD"-designation, not provided for elsewhere}
- A61K 31/7088: Compounds having three or more nucleosides or nucleotides
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 7/04: Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
- C12N 15/1138: {against receptors or cell surface proteins}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/32: specific for a neo-epitope on a complex, e.g. antibody-antigen or ligand-receptor
- C07K 2317/55: Fab or Fab'
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- C07K 2317/92: Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
- 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
- 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 relates to an inhibitor of platelet glycoprotein V (GPV) for use as a coagulant, and/or for use in the treatment or prevention of a hemorrhagic condition.

## Claims

### Claim 1

(canceled)

### Claim 2

A method for the treatment or prevention of a hemorrhagic condition comprising administering to a subject in need thereof an effective amount of an inhibitor of platelet glycoprotein V (GPV).

### Claim 3 (depends on 2)

The method according to claim 2, wherein the hemorrhagic condition is caused by a platelet disorder.

### Claim 4 (depends on 3)

The method according to claim 3, wherein the platelet disorder is characterized by a decreased number of platelets.

### Claim 5 (depends on 2)

The method according to claim 2, wherein the hemorrhagic condition is selected from the group consisting of inflammatory bleeding, hemorrhagic stroke, excessive bleeding due to sepsis, excessive bleeding due to thrombocytopenia, excessive bleeding due to disseminated intravascular coagulation (DIC), excessive bleeding due to chemotherapy, excessive bleeding due to hemolytic-uremic syndrome, excessive bleeding upon administration of soluble GPV, and excessive bleeding due to HIV infection.

### Claim 6 (depends on 2)

The method according to claim 2, wherein the GPV is human GPV.

### Claim 7 (depends on 2)

The method according to claim 2, wherein the inhibitor is an antibody directed against the extracellular domain of GPV, or a functional fragment or derivative of an antibody, the fragment or derivative being capable of binding to the extracellular domain of GPV.

### Claim 8 (depends on 7)

The method according to claim 7, wherein the antibody, fragment, or derivative binds to a region of the extracellular domain of GPV which is different from the collagen-binding site of GPV.

### Claim 9 (depends on 7)

The method according to claim 7, wherein the antibody, fragment, or derivative does not delay collagen-induced aggregation.

### Claim 10 (depends on 7)

The method according to claim 7, wherein the antibody is a monoclonal antibody or a functional fragment or functional derivative thereof.

### Claim 11 (depends on 2)

The method according to claim 2, wherein the inhibitor is a nucleic acid capable of reducing expression of GP5 mRNA.

### Claim 12 (depends on 2)

The method according to claim 2, wherein the inhibitor, upon administration to the subject, does not affect the number of platelets in the subject.

### Claim 13 (depends on 2)

The method according to claim 2, wherein the inhibitor is a coagulant.

### Claim 14 (depends on 2)

The method according to claim 2, wherein the treatment or prevention comprises administering to a subject, a pharmaceutically effective amount of the inhibitor.

### Claim 15 (depends on 14)

The method according to claim 14, wherein the treatment or prevention further comprises administering to the subject a coagulant other than the inhibitor.

### Claim 16 (depends on 15)

The method according to claim 15, wherein the coagulant other than the inhibitor is selected from the group consisting of an anti-fibrinolytic agent, a platelet concentrate, a coagulation factor concentrate, and fresh frozen plasma.

### Claim 17

A pharmaceutical composition comprising an inhibitor of platelet glycoprotein V (GPV) and a pharmaceutically acceptable excipient.

### Claim 18

(canceled)

### Claim 19 (depends on 17)

A method of treating or preventing a hemorrhagic condition in a subject, comprising administering to the subject an effective amount of the pharmaceutical composition of claim 17.

### Claim 20 (depends on 14)

The method of claim 14, wherein the subject is a human.

### Claim 21 (depends on 19)

The method of claim 19, wherein the subject is a human.
