# US 2014/0193407 A1 · Drug fusions and conjugates

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- Number: US 2014/0193407 A1
- Document ID: US20140193407A1
- Status: Published application
- Kind: A1
- Application number: 14/099,210
- Filed: 2013-12-06
- Published: 2014-07-10
- Earliest claimed: 2009-03-27
- Assignees: Glaxo Group Limited
- Applicants: Glaxo Group Limited
- Inventors: Christopher Herring; Lucy J. Holt; Laurent S. Jespers; Sebastian Mayer; Malgorzata Pupecka-Swider; Bruce J. Hamilton
- Web page: https://patentgrep.com/patent/US20140193407A1

## CPC

- C07K 16/18: against material from animals or humans
- A61K 38/26: Glucagons
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 47/6803: {Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates}
- A61K 47/6843: {the antibody targeting a material from animals or humans}
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/08: for glucose homeostasis (pancreatic hormones A61P5/48)
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/50: for increasing or potentiating the activity of insulin
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 7/12: Antidiuretics, e.g. drugs for diabetes insipidus (ADH A61P5/10)
- C07K 14/605: Glucagons
- C07K 2317/21: from primates, e.g. man
- C07K 2317/569: Single domain, e.g. dAb, sdAb, VHH, VNAR or nanobody®
- 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

## Abstract

The present invention relates to drug fusions that have improved serum half lives. These fusions and conjugates comprise polypeptides, immunoglobulin (antibody) single variable domains and GLP and/or exendin molecules. The invention further relates to uses, formulations, compositions and devices comprising such drug fusions and conjugates.

## Claims

### Claim 1

A drug fusion or conjugate comprising:
(a) an insulinotropic agent or an incretin drug selected from: (i) GLP-1, (ii) exendin-4, and (iii) PYY (Peptide YY), present as a fusion or a conjugate; and
(b) a dAb which binds serum albumin selected from: (i) the DOM 7h-14-10 domain antibody (dAb) (SEQ ID NO 26); (ii) the DOM 7h-11-15 dAb (SEQ ID NO 27); or (iii) the DOM 7h-14-10R108C domain antibody (dAb) (SEQ ID NO 42);
wherein the fusion or conjugate has an elimination half life in a human of 12 hours or more.

### Claim 2 (depends on 1)

The drug fusion or conjugate of claim 1, wherein said fusion or conjugate has an elimination half life in a human of 12-21 days.

### Claim 3 (depends on 1)

A drug fusion or conjugate according to claim 1 which is Exendin 4, (G4S)3, linker DOM7h-14-10 fusion (DMS7139)
(SEQ ID NO 24)
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSGGGGGSGGGG
SGGGGSDIQMTQSPSSLSASVGDRVTITCRASQWIGSQLSWYQQKPGKA
PKLLIMWRSSLQSGVPSRFSGSGSGTDFTLTISSLQPEDFATYYCAQGL
RHPKTFGQGTKVEIKR.

### Claim 4 (depends on 3)

The drug fusion or conjugate according to claim 3, where said fusion or conjugate has an elimination half life in a human of 12-21 days.

### Claim 5 (depends on 1)

A method of treating a metabolic disorder selected from the group consisting of hyperglycemia, impaired glucose tolerance, beta cell deficiency, diabetes (type 1 or type 2 diabetes or gestational diabetes), and obesity, wherein said method comprises administering a drug fusion or conjugate according to claim 1 to a subject.

### Claim 6 (depends on 5)

The method of claim 5, wherein said method further comprises the step of administering an additional therapeutic agent to said subject.

### Claim 7 (depends on 6)

The method of claim 6, wherein said additional therapeutic agent is administered to said subject concurrently with said drug fusion or conjugate.

### Claim 8 (depends on 6)

The method of claim 6, wherein said additional therapeutic agent is administered to said subject sequentially to said drug fusion or conjugate.

### Claim 9 (depends on 3)

A method of treating a metabolic disorder selected from the group consisting of hyperglycemia, impaired glucose tolerance, beta cell deficiency, diabetes (type 1 or type 2 diabetes or gestational diabetes), and obesity, wherein said method comprises administering a drug fusion or conjugate according to claim 3 to a subject.

### Claim 10 (depends on 9)

The method of claim 9, wherein said method further comprises the step of administering an additional therapeutic agent to said subject.

### Claim 11 (depends on 10)

The method of claim 10, wherein said additional therapeutic agent is administered to said subject concurrently with said drug fusion or conjugate.

### Claim 12 (depends on 10)

The method of claim 10, wherein said additional therapeutic agent is administered to said subject sequentially to said drug fusion or conjugate.

### Claim 13

A method of treating a metabolic disorder selected from the group consisting of hyperglycemia, impaired glucose tolerance, beta cell deficiency, diabetes (type 1 or type 2 diabetes or gestational diabetes), and obesity, wherein said method comprises administering Exendin 4, (G4S)3, linker DOM7h-14-10 fusion (DMS7139)
(SEQ ID NO 24)
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSGGGGGSGGGG
SGGGGSDIQMTQSPSSLSASVGDRVTITCRASQWIGSQLSWYQQKPGKA
PKLLIMWRSSLQSGVPSRFSGSGSGTDFTLTISSLQPEDFATYYCAQGL
RHPKTFGQGTKVEIKR
to a subject.

### Claim 14 (depends on 13)

The method of claim 13, wherein said method further comprises the step of administering an additional therapeutic agent to said subject.

### Claim 15 (depends on 13)

The method of claim 13, wherein said additional therapeutic agent is administered to said subject concurrently with said drug fusion or conjugate.

### Claim 16 (depends on 13)

The method of claim 13, wherein said additional therapeutic agent is administered to said subject sequentially to said drug fusion or conjugate.