# US 11,077,164 B2 · Weekly dosing regimens for anti-CD30 vc-PAB-MMAE antibody drug-conjugates

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- Number: US 11,077,164 B2
- Document ID: US11077164B2
- Status: Granted
- Kind: B2
- Application number: 17/142,816
- Filed: 2021-01-06
- Published: 2021-05-13
- Granted: 2021-08-03
- Earliest claimed: 2009-01-09
- Assignees: Seagen Inc.
- Applicants: Seagen Inc.
- Inventors: Eric Sievers; Dana Kennedy
- Web page: https://patentgrep.com/patent/US11077164B2

## CPC

- A61K 38/05: Dipeptides
- A61K 39/00: Medicinal preparations containing antigens or antibodies (materials for immunoassay G01N33/53)
- A61K 47/64: Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent (peptidic linkers A61K47/65)
- A61K 47/68031: {the drug being an auristatin}
- A61K 47/6811: {the drug being a protein or peptide, e.g. transferrin or bleomycin}
- A61K 47/6849: {the antibody targeting a receptor, a cell surface antigen or a cell surface determinant}
- A61K 47/6867: {the tumour determinant being from a cell of a blood cancer}
- 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
- A61P 35/02: specific for leukemia
- C07K 16/2878: {against the NGF-receptor/TNF-receptor superfamily, e.g. CD27, CD30, CD40, CD95}
- C07K 16/3061: {Blood cells}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/56: variable (Fv) region, i.e. VH and/or VL
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/77: Internalization into the cell
- 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

Methods for the treatment of CD30-expressing cancers are provided. The methods comprise administering to a subject in need thereof a weekly dose of from about 0.8 mg/kg to about 1.8 mg/kg of an antibody-drug conjugate compound having formula (I); or a pharmaceutically acceptable salt thereof; wherein: mAb is an anti-CD30 antibody unit, S is a sulfur atom of the antibody, A- is a Stretcher unit, and p is from about 3 to about 5.

## Claims

### Claim 1

A method for treating a CD30-expressing hematologic cancer in a human subject, the method comprising administering to a subject in need thereof a dose of a pharmaceutical composition comprising cAC10-MC-vc-PAB-MMAE antibody-drug conjugate, wherein the administered dose of cAC10-MC-vc-PAB-MMAE antibody-drug conjugate is 1.2 mg/kg of the subject's body weight and the pharmaceutical composition is administered once every two weeks,
and wherein the CD30-expressing hematologic cancer is Hodgkin Lymphoma.

### Claim 2 (depends on 1)

The method of claim 1, wherein the human subject is newly diagnosed and has not previously been treated for the CD30-expressing hematologic cancer.

### Claim 3 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition is administered for two or more treatment cycles.

### Claim 4 (depends on 3)

The method of claim 3, wherein the pharmaceutical composition is administered for 3 or more treatment cycles.

### Claim 5 (depends on 3)

The method of claim 3, wherein the pharmaceutical composition is administered for 4 or more treatment cycles.

### Claim 6 (depends on 3)

The method of claim 3, wherein the pharmaceutical composition is administered for 5 or more treatment cycles.

### Claim 7

A method for treating a CD30-expressing hematologic cancer in a human subject, the method comprising administering to a subject in need thereof a dose of a pharmaceutical composition comprising cAC10-MC-vc-PAB-MMAE antibody-drug conjugate, wherein the administered dose of cAC10-MC-vc-PAB-MMAE antibody-drug conjugate is 1.2 mg/kg of the subject's body weight and the pharmaceutical composition is administered once every two weeks,
and wherein the average number of MMAE molecules per cAC10 antibody of the cAC10-MC-vc-PAB-MMAE antibody-drug conjugate in the pharmaceutical composition is about 4.

### Claim 8 (depends on 7)

The method of claim 7, wherein the human subject is newly diagnosed and has not previously been treated for the CD30-expressing hematologic cancer.

### Claim 9 (depends on 7)

The method of claim 7, wherein the pharmaceutical composition is administered for two or more treatment cycles.

### Claim 10 (depends on 7)

The method of claim 7, wherein the pharmaceutical composition is administered for 3 or more treatment cycles.

### Claim 11 (depends on 7)

The method of claim 7, wherein the pharmaceutical composition is administered for 4 or more treatment cycles.

### Claim 12 (depends on 7)

The method of claim 7, wherein the pharmaceutical composition is administered for 5 or more treatment cycles.

### Claim 13

A method for treating a CD30-expressing hematologic cancer in a human subject, the method comprising administering to a subject in need thereof a dose of a pharmaceutical composition comprising (i) cAC10-MC-vc-PAB-MMAE antibody-drug conjugate, wherein the administered dose of cAC10-MC-vc-PAB-MMAE antibody-drug conjugate is 1.2 mg/kg of the subject's body weight and the pharmaceutical composition is administered once every two weeks,
wherein the CD30-expressing hematologic cancer is Hodgkin Lymphoma, and
wherein the average number of MMAE molecules per cAC10 antibody of the cAC10-MC-vc-PAB-MMAE antibody-drug conjugate in the pharmaceutical composition is about 4.

### Claim 14 (depends on 13)

The method of claim 13, wherein the human subject is newly diagnosed and has not previously been treated for the CD30-expressing hematologic cancer.

### Claim 15 (depends on 13)

The method of claim 13, wherein the pharmaceutical composition is administered for two or more treatment cycles.

### Claim 16 (depends on 13)

The method of claim 13, wherein the pharmaceutical composition is administered for 3 or more treatment cycles.

### Claim 17 (depends on 13)

The method of claim 13, wherein the pharmaceutical composition is administered for 4 or more treatment cycles.

### Claim 18 (depends on 13)

The method of claim 13, wherein the pharmaceutical composition is administered for 5 or more treatment cycles.
