# US 11,110,087 B2 · Combination therapy of a type II anti-CD20 antibody with a selective Bcl-2 inhibitor

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- Number: US 11,110,087 B2
- Document ID: US11110087B2
- Status: Granted
- Kind: B2
- Application number: 17/187,468
- Filed: 2021-02-26
- Published: 2021-06-17
- Granted: 2021-09-07
- Earliest claimed: 2012-09-07
- Assignees: Genentech, Inc.; Hoffmann-La Roche Inc.; AbbVie Inc.
- Applicants: Genentech, Inc.; Hoffmann-La Roche Inc.; Abbvie Inc.
- Inventors: Deepak Sampath; Christian Klein; Wayne John Fairbrother; Sari L. Heitner Enschede; Rod A. Humerickhouse; Andrew W. Roberts; John F. Seymour
- Web page: https://patentgrep.com/patent/US11110087B2

## CPC

- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/02: Halogenated hydrocarbons
- A61K 31/04: Nitro compounds
- A61K 31/10: Sulfides; Sulfoxides; Sulfones
- A61K 31/18: Sulfonamides (compounds containing a para-N-benzene-sulfonyl-N- group A61K31/63)
- A61K 31/33: Heterocyclic compounds
- A61K 31/436: the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
- A61K 31/437: the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
- A61K 31/4375: the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
- A61K 31/45: having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
- A61K 31/505: Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K 31/63: Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
- A61K 39/39558: {against tumor tissues, cells, antigens}
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 16/2887: {against CD20}
- A61K 2039/545: {characterised by the dose, timing or administration schedule}
- A61K 2039/585: {wherein the target is cancer}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/73: Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
- 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 is directed to a combination therapy involving a type II anti-CD20 antibody and a selective Bcl-2 inhibitor for the treatment of a patient suffering from cancer, particularly, a CD20-expressing cancer.

## Claims

### Claim 1

A method for treating lymphoma or leukemia in a human patient, the method comprising orally administering once daily GDC-0199 to the patient in dosing cycles comprising escalating doses, wherein the escalating doses comprise a dose of 100 mg of GDC-0199 per day, followed by orally administering to the patient a dose of 200 mg of GDC-0199 per day, followed by orally administering to the patient a dose of 400 mg of GDC-0199 per day.

### Claim 2 (depends on 1)

The method of claim 1, wherein each dosing cycle is one day.

### Claim 3 (depends on 2)

The method of claim 2, wherein a starting dose of the escalating doses is administered for one dosing cycle and an ending dose of the escalating doses is administered in multiple dosing cycles.

### Claim 4 (depends on 3)

The method of claim 3, wherein the method is continued until disease progression.

### Claim 5 (depends on 1)

The method of claim 1, wherein the GDC-0199 is administered in combination with obinutuzumab.

### Claim 6 (depends on 5)

The method of claim 5, wherein an effective amount of the obinutuzumab is administered to the patient in combination with the GDC-0199 once in a 28 day cycle for 6 to 7 dosing cycles.

### Claim 7 (depends on 6)

The method of claim 6, wherein the effective amount of the obinutuzumab is 1000 mg.

### Claim 8 (depends on 1)

The method of claim 1, wherein the patient is administered 100 mg of GDC-0199 per day for one day, followed by 200 mg of GDC-0199 per day for one day, followed by 400 mg of GDC-0199 per day.

### Claim 9

A method for treating lymphoma or leukemia in a human patient, the method comprising orally administering once daily GDC-0199 in escalating doses to the patient, wherein the escalating doses comprise a dose of 100 mg of GDC-0199 per day, followed by orally administering to the patient a dose of 200 mg of GDC-0199 per day.

### Claim 10 (depends on 9)

The method of claim 9, wherein the method comprises administering three differing doses of GDC-0199.

### Claim 11 (depends on 10)

The method of claim 10, wherein the method comprises administering GDC-0199 in multiple dosing cycles and wherein a different dose of GDC-0199 is orally administered once daily to the patient in each of the first three dosing cycles.

### Claim 12 (depends on 11)

The method of claim 11, wherein each dosing cycle is one day.

### Claim 13 (depends on 12)

The method of claim 12, wherein a starting dose of the escalating doses is administered for one dosing cycle and an ending dose of the escalating doses is administered in multiple dosing cycles.

### Claim 14 (depends on 13)

The method of claim 13, wherein the method is continued until disease progression.

### Claim 15 (depends on 9)

The method of claim 9, wherein the GDC-0199 is administered in combination with obinutuzumab.

### Claim 16 (depends on 15)

The method of claim 15, wherein an effective amount of the obinutuzumab is administered to the patient in combination with the GDC-0199 once in a 28 day cycle for 6 to 7 dosing cycles.

### Claim 17 (depends on 16)

The method of claim 16, wherein the effective amount of the obinutuzumab is 1000 mg.

### Claim 18 (depends on 9)

The method of claim 9, wherein the patient is administered 100 mg of GDC-0199 per day for one day, followed by 200 mg of GDC-0199 per day for one day.

### Claim 19

A method for treating lymphoma or leukemia in a human patient, the method comprising orally administrating once daily GDC-0199 in escalating doses to the patient, wherein the escalating doses comprise a daily dose of 100 mg of GDC-0199.

### Claim 20 (depends on 19)

The method of claim 19, wherein the method comprises administering three differing doses of GDC-0199.

### Claim 21 (depends on 20)

The method of claim 20, wherein the dose of 100 mg of GDC-0199 is a starting dose of the escalating doses.

### Claim 22 (depends on 20)

The method of claim 20, wherein the method comprises administering GDC-0199 in multiple dosing cycles and wherein a different dose of GDC-0199 is orally administered once daily to the patient in each of the first three dosing cycles.

### Claim 23 (depends on 22)

The method of claim 22, wherein each dosing cycle is one day.

### Claim 24 (depends on 20)

The method of claim 20, wherein a starting dose of the escalating doses is administered for one dosing cycle and an ending dose of the escalating doses is administered in multiple dosing cycles.

### Claim 25 (depends on 24)

The method of claim 24, wherein the method is continued until disease progression.

### Claim 26 (depends on 19)

The method of claim 19, wherein the GDC-0199 is administered in combination with cytarabine.

### Claim 27 (depends on 19)

The method of claim 19, wherein the GDC-0199 is administered in combination with obinutuzumab.

### Claim 28 (depends on 27)

The method of claim 27, wherein an effective amount of the obinutuzumab is administered to the patient in combination with the GDC-0199 once in a 28 day cycle for 6 to 7 dosing cycles.

### Claim 29 (depends on 28)

The method of claim 28, wherein the effective amount of the obinutuzumab is 1000 mg.