# US 10,765,738 B2 · Combination of anti-FGFR4-antibody and bile acid sequestrant

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- Number: US 10,765,738 B2
- Document ID: US10765738B2
- Status: Granted
- Kind: B2
- Application number: 15/575,255
- Filed: 2016-05-18
- Published: 2018-05-17
- Granted: 2020-09-08
- Earliest claimed: 2015-05-19
- Assignees: Daiichi Sankyo Europe GmbH; Daiichi Sankyo Company, Limited
- Applicants: Daiichi Sankyo Europe GmbH; Daiichi Sankyo Company Limited
- Inventors: Reimar Abraham; Mauricio Redondo-Müller
- Web page: https://patentgrep.com/patent/US10765738B2

## CPC

- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 31/07: Retinol compounds, e.g. vitamin A (retinoic acids A61K31/203)
- A61K 31/122: having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
- A61K 31/355: Tocopherols, e.g. vitamin E
- A61K 31/395: having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K 31/59: Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
- A61K 31/785: Polymers containing nitrogen
- A61K 31/787: containing heterocyclic rings having nitrogen as a ring hetero atom
- A61K 38/179: {for growth factors; for growth regulators}
- A61K 39/395: Antibodies (agglutinins A61K38/36 {; as drug carriers A61K47/50}); Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 13/12: of the kidneys
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 35/00: Antineoplastic agents
- C07K 16/2863: {against receptors for growth factors, growth regulators}
- A61K 2039/505: {comprising antibodies}
- A61K 2039/507: {Comprising a combination of two or more separate antibodies}
- A61K 2039/54: {characterised by the route of administration}
- A61K 2039/545: {characterised by the dose, timing or administration schedule}
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- 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
- 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)

## Abstract

The present invention relates to the amelioration of toxic effects that are caused by therapies aimed at FGFR4-inhibition. In particular, the invention relates to the combination of FGFR4 inhibitors and agents capable of reducing bile acid levels and to the use thereof in the treatment of diseases.

## Claims

### Claim 1

A pharmaceutical composition or kit comprising an anti-FGFR4 antibody in combination with a bile acid sequestrant, wherein (i) the anti-FGFR4 antibody comprises a heavy chain variable region according to SEQ ID NO: 54 and a light chain variable region according to SEQ ID NO: 62, and (ii) the bile acid sequestrant comprises colestyramine.

### Claim 2 (depends on 1)

The pharmaceutical composition or kit of claim 1, wherein the anti-FGFR4 antibody is directed against an epitope comprising the amino acid sequence RYNY (SEQ ID NO: 69) of human FGFR4 (SEQ ID NO: 70).

### Claim 3 (depends on 1)

The pharmaceutical composition or kit of claim 1, further comprising one or more vitamins.

### Claim 4 (depends on 1)

The pharmaceutical composition or kit of claim 1, further comprising one or more fat-soluble vitamins selected from vitamin A, D, E, and K.

### Claim 5 (depends on 1)

The pharmaceutical composition or kit of claim 1, in combination with one or more physiologically acceptable carriers, diluents, and adjuvants.

### Claim 6 (depends on 5)

The pharmaceutical composition or kit of claim 5, wherein the anti-FGFR4 antibody and the bile acid sequestrant are provided in the form of a single composition or in the form of at least two distinct compositions.

### Claim 7 (depends on 5)

The pharmaceutical composition or kit of claim 5, additionally comprising one or more fat-soluble vitamins comprising one or more of vitamin A, D, E, and K.

### Claim 8

A pharmaceutical composition or kit comprising an anti-FGFR4 antibody in combination with a bile acid sequestrant, wherein (i) the anti-FGFR4 antibody comprises a heavy chain comprising a CDRH1 as shown in SEQ ID NO: 3, a CDRH2 as shown in SEQ ID NO: 8 and a CDRH3 as shown in SEQ ID NO: 15 and a light chain comprising a CORL1 as shown in SEQ ID NO: 23, a CDRL2 as shown in SEQ ID NO: 25 and a CDRL3 as shown in SEQ ID NO: 30, and (ii) the bile acid sequestrant comprises colestyramine.