# US 2020/0390902 A1 · Antibody-Drug Conjugates Targeted at Human Aspartyl-(Asparaginyl)-B-Hydroxylase (HAAH)

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- Number: US 2020/0390902 A1
- Document ID: US20200390902A1
- Status: Published application
- Kind: A1
- Application number: 16/108,026
- Filed: 2018-08-21
- Published: 2020-12-17
- Earliest claimed: 2017-08-22
- Assignees: Panacea Pharmaceuticals, Inc.
- Applicants: Panacea Pharmaceuticals, Inc.
- Inventors: Hossein Ghanbari; Steven A. Fuller; Michael Lebowitz; Zhi-Gang Jiang
- Web page: https://patentgrep.com/patent/US20200390902A1

## CPC

- A61K 38/07: Tetrapeptides
- A61K 31/40: having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K 38/08: Peptides having 5 to 11 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61K 47/6803: {Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates}
- A61K 47/68031: {the drug being an auristatin}
- A61K 47/68033: {the drug being a maytansine}
- A61K 47/6871: {the antibody targeting an enzyme}
- A61K 47/6889: {Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment}
- A61P 35/00: Antineoplastic agents
- C07K 16/40: against enzymes
- A61K 2039/505: {comprising antibodies}
- 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

Disclosed are anti-HAAH antibodies and derivatives thereof conjugated to cytotoxic, cytostatic, immunosuppressive, or other therapeutic agents, as well as pharmaceutical compositions comprising the antibody- and antibody derivative-drug conjugates. Also disclosed are methods for the treatment of HAAH-expressing cancers, comprising administering to a subject the disclosed pharmaceutical compositions.

## Claims

### Claim 1

An antibody-drug conjugate comprising an anti-HAAH monoclonal antibody conjugated to at least one cytotoxic or cytostatic drug, and optionally a linker connecting the antibody and the cytotoxic or cytostatic drug.

### Claim 2 (depends on 1)

The antibody-drug conjugate of claim 1, wherein the anti-HAAH antibody is SNS622.

### Claim 3 (depends on 1)

The antibody-drug conjugate of claim 1, wherein the at least one drug is selected from an auristatin derivative, a maytansinoid and/or a duocarmycin derivative DUO.

### Claim 4 (depends on 1)

The antibody-drug conjugate of claim 1, wherein the auristatin derivative is selected from MMAE or MMAF.

### Claim 5 (depends on 1)

The antibody-drug conjugate of claim 1, wherein the maytansinoid is selected from DM1 or DM4.

### Claim 6 (depends on 1)

The antibody-drug conjugate of claim 1, wherein the duocarmycin derivative is DUO.

### Claim 7 (depends on 1)

The antibody-drug conjugate of claim 1, comprising at least one linker connecting the antibody to the drug.

### Claim 8 (depends on 7)

The antibody-drug conjugate of claim 7, wherein the at least one linker is selected from the group consisting of maleimidocaproyl (MC), valine citruline (vc), para amino benzyl alcohol (PABA), a 4-unit polyethylene glycol (PEG4), and N,N-Dimethylethanolamine (DMEA).

### Claim 9

A method of making an antibody-drug conjugate comprising, conjugating at least one cytotoxic or cytostatic drug to an anti-HAAH antibody, and optionally conjugating a linker connecting the drug and the antibody.

### Claim 10 (depends on 9)

The method of claim 9, wherein the anti-HAAH antibody is SNS622.

### Claim 11 (depends on 9)

The method of claim 9, wherein the at least one cytotoxic or cytostatic drug is an auristatin derivative.

### Claim 12 (depends on 9)

The method of claim 9, wherein the at least one cytotoxic cytostatic drug is a maytansinoid

### Claim 13 (depends on 9)

The method of claim 9, comprising at least one linker connecting the antibody to the drug.

### Claim 14 (depends on 13)

The method of claim 13, wherein the at least one linker is selected from the group consisting of maleimidocaproyl (MC), valine citruline (vc), para-amino benzyl alcohol (PABA), a 4-unit polyethylene glycol (PEG4), and N,N-Dimethylethanolamine (DMEA).

### Claim 15 (depends on 14)

The method of claim 14, wherein the at least one linker is valine citruline-para-amino benzyl alcohol (vc-PAB).

### Claim 16 (depends on 14)

The method of claim 14, wherein the linker is maleimidocaproyl (MC).

### Claim 17 (depends on 1)

A pharmaceutical composition comprising the antibody-drug conjugate of claim 1 and a pharmaceutically acceptable medium.

### Claim 18 (depends on 17)

A method of treating a patient in need thereof, comprising administering to the patient the pharmaceutical composition of claim 17.

### Claim 19 (depends on 1)

A method of treating cancer, comprising contacting a cancer with the antibody drug conjugate of claim 1.

### Claim 20 (depends on 19)

The method of claim 19 in which the cancer is selected form pancreatic, lung, breast or AML.