# US 11,078,270 B2 · Use of negative functional modulators of erythropoietin for therapy

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- Number: US 11,078,270 B2
- Document ID: US11078270B2
- Status: Granted
- Kind: B2
- Application number: 15/318,007
- Filed: 2015-06-12
- Published: 2017-04-27
- Granted: 2021-08-03
- Earliest claimed: 2014-06-12
- Assignees: Andremacon S.R.L.
- Applicants: Andremacon S.R.L.
- Inventors: Giovanni Marfia; Stefania Elena Navone; Giuseppe Scalvini; Laura Riboni; Rolando Campanella
- Web page: https://patentgrep.com/patent/US11078270B2

## CPC

- C07K 16/26: against hormones {; against hormone releasing or inhibiting factors}
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- 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 39/39541: {against normal tissues, cells}
- 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 35/00: Antineoplastic agents
- C07K 14/72: for hormones {(for neuromediators C07K14/70571)}
- C07K 16/22: against growth factors {; against growth regulators}
- C07K 16/2863: {against receptors for growth factors, growth regulators}
- C07K 16/2869: {against hormone receptors (for antibodies against neuromediator receptors C07K16/286)}
- C12N 15/1136: {against growth factors, growth regulators, cytokines, lymphokines or hormones}
- G01N 33/5023: {on expression patterns}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/34: Identification of a linear epitope shorter than 20 amino acid residues or of a conformational epitope defined by amino acid residues
- C12N 2310/14: interfering nucleic acids [NA]
- G01N 2500/04: Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
- G01N 2500/10: involving cells
- 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)
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

The invention relates to negative functional modulators of erythropoietin (EPO) for use in the treatment of cancers, in the therapy of autoimmune -based and non-autoimmune based chronic inflammatory diseases, and in the treatment of patients under-going organ or tissue transplant, or for the treatment of hemophilic arthropathy, hemophilia A and B, von Willebrand disease, angiodysplasia, proliferative disorders and neurological diseases characterized in their pathogenesis by primary neuroinflammation and/or neuroinflammation secondary to other causes. Such modulators are anti-EPO antibodies and their derivatives: anti-EPO receptor antibodies (EPOR), antisense oligonucleotides, decoy DNA, decoy RNA, ribozyme, antagomir, shRNA, LNA and/or siRNAs that inhibit the expression of the gene encoding EPO or EPOR.

## Claims

### Claim 1

A method of treating with negative functional modulators of erythropoietin (EPO) subjects suffering from glioblastoma multiforme wherein said modulators are molecules that bind EPO selected from the group consisting of
(i) anti EPO-antibodies, that recognize and bind the AA 28-189 of human EPO (amino acids 1-162 of SEQ ID NO: 2); wherein said negative functional modulator is an anti-EPO polyclonal antibody (H-162),
said method comprising administering to said subjects an effective amount of said negative functional modulators of erythropoietin (EPO).

### Claim 2 (depends on 1)

The method according to claim 1, comprising administering to said subjects a pharmaceutical composition comprising the modulator according to claim 1 and pharmaceutically acceptable excipients.

### Claim 3 (depends on 2)

The method according to claim 2 wherein said pharmaceutical composition further comprises a therapeutically effective amount of one or more natural or synthetic molecules that act on the receptors of S1P, wherein said molecules are selected from the group consisting of FTY720-P, SW-2871, VPC24191, AUY954, SEW2871 (5-[4-phenyl-5-(trifluoromethyl)-2-thienyl]-3-[trifluoromethyl)phenyl]-1,2,4-oxadiazole), VPC23153, DS-GS- 44 and VPC01091.

### Claim 4 (depends on 3)

The method according to claim 3, wherein said FTY720 is administered in combination with said anti-EPO polyclonal antibody (H-162).

### Claim 5 (depends on 2)

The method according to claim 2, wherein said pharmaceutical composition is formulated as tablets, powder, granules, capsules, liquid agents, injections, suppositories, or slow-release agents.

### Claim 6 (depends on 2)

The method according to claim 2, wherein said pharmaceutical composition is administered orally, parenterally, topically, rectally, intravenously, subcutaneously, intramuscularly, intranasally, intravaginally, through the oral mucosa, the lung mucosa or by transocular administration.