# US 12,492,261 B2 · Subcutaneous dosing of anti-CD20/anti-CD3 bispecific antibodies

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- Number: US 12,492,261 B2
- Document ID: US12492261B2
- Status: Granted
- Kind: B2
- Application number: 17/516,794
- Filed: 2021-11-02
- Published: 2022-05-19
- Granted: 2025-12-09
- Earliest claimed: 2020-11-04
- Assignees: Genentech, Inc.
- Applicants: Genentech, Inc.
- Inventors: Chi-Chung Li; Carol Elaine O'Hear; Hong Wang; Brendan Christian Bender; Iraj Hosseini
- Web page: https://patentgrep.com/patent/US12492261B2

## CPC

- C07K 16/2887: {against CD20}
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- C07K 16/2809: {against the T-cell receptor (TcR)-CD3 complex}
- C07K 16/2866: {against receptors for cytokines, lymphokines, interferons}
- A61K 2039/505: {comprising antibodies}
- A61K 2039/544: {to the airways}
- A61K 2039/545: {characterised by the dose, timing or administration schedule}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/31: multispecific
- C07K 2317/565: Complementarity determining region [CDR]
- 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 the treatment of subjects having CD20-positive cell proliferative disorders (e.g., B cell proliferative disorders, such as non-Hodgkin's lymphomas). More specifically, the invention pertains to the treatment of subjects having a B cell proliferative disorder by subcutaneous administration of an anti-CD20/anti-CD3 bispecific antibody.

## Claims

### Claim 1

A method of treating a subject having a non-Hodgkin's lymphoma (NHL) comprising subcutaneously administering to the subject mosunetuzumab in a dosing regimen comprising eight dosing cycles, wherein:
(a) the first dosing cycle comprises a first subcutaneous dose (C1D1), a second subcutaneous dose (C1D2), and a third subcutaneous dose (C1D3) of mosunetuzumab, wherein:
(i) the C1D1 is 5 mg;
(ii) the C1D2 is 45 mg; and
(iii) the C1D3 is 45 mg; and
(b) the second to eighth dosing cycles each comprises a single subcutaneous dose (C2D1-C8D1) of mosunetuzumab, wherein each of the C2D1-C8D1 of mosunetuzumab is 45 mg,
wherein the eight cycles are 21-day dosing cycles; or the first dosing cycle is a 21-day dosing cycle and the second to eighth dosing cycles are 28-day dosing cycles, and wherein the method comprises administering to the subject the C1D1, the C1D2, and the C1D3 on or about Days 1, 8, and 15, respectively, of the first dosing cycle and administering to the subject the C2D1-C8D1 on Day 1 of each of the second to eighth dosing cycles.

### Claim 2 (depends on 1)

The method of claim 1, wherein the NHL is a previously untreated (1L) NHL, a relapsed or refractory NHL, a diffuse-large B cell lymphoma (DLBCL), a follicular lymphoma (FL), a mantle cell lymphoma (MCL), a high-grade B cell lymphoma or an Ann Arbor stage III or IV NHL, or a primary mediastinal (thymic) large B cell lymphoma (PMLBCL).

### Claim 3 (depends on 2)

The method of claim 2, wherein the DLBCL is a Richter's transformation.

### Claim 4 (depends on 2)

The method of claim 2, wherein the FL is a transformed FL.

### Claim 5 (depends on 1)

The method of claim 1, wherein the subject had previously been administered at least one prior line of systemic therapy.

### Claim 6 (depends on 5)

The method of claim 5, wherein at least one prior line of systemic therapy comprised an anti-CD20 antibody or a Bruton's tyrosine kinase (BTK) inhibitor.

### Claim 7 (depends on 6)

The method of claim 6, wherein the prior line of systemic therapy comprising the anti-CD20 antibody additionally comprises an alkylating agent, vincristine, fludarabine, or an anthracycline.

### Claim 8 (depends on 1)

The method of claim 1, wherein the dosing regimen comprises one or more additional dosing cycles.

### Claim 9 (depends on 8)

The method of claim 8, wherein each additional dosing cycle is a 21-day dosing cycle or a 28-day dosing cycle.

### Claim 10 (depends on 8)

The method of claim 8, wherein each additional dosing cycle comprises administration of an additional dose of mosunetuzumab.

### Claim 11 (depends on 10)

The method of claim 10, wherein each additional dose of mosunetuzumab is 45 mg.

### Claim 12 (depends on 10)

The method of claim 10, wherein the method comprises administering to the subject each additional dose of mosunetuzumab on Day 1 of each respective additional dosing cycle.

### Claim 13 (depends on 1)

The method of claim 1, wherein mosunetuzumab is administered to the subject as a monotherapy or as a combination therapy.

### Claim 14 (depends on 1)

The method of claim 1, wherein mosunetuzumab is administered to the subject concurrently with an additional therapeutic agent, prior to the administration of an additional therapeutic agent, or subsequent to the administration of one or more additional therapeutic agent.

### Claim 15 (depends on 14)

The method of claim 14, wherein the additional therapeutic agent is obinutuzumab or tocilizumab.

### Claim 16 (depends on 1)

The method of claim 1, wherein the subject has a cytokine release syndrome event, and the method further comprises treating the symptoms of the cytokine release syndrome event while suspending treatment with mosunetuzumab.

### Claim 17 (depends on 16)

The method of claim 16, wherein the method further comprising administering to the subject an effective amount of tocilizumab and/or an effective amount of a corticosteroid to treat the cytokine release syndrome event.

### Claim 18 (depends on 1)

The method of claim 1, wherein the subject is a human.

### Claim 19 (depends on 8)

The method of claim 8, wherein the dosing regimen comprises one to nine additional dosing cycles.

### Claim 20 (depends on 19)

The method of claim 19, wherein each additional dosing cycle is a 21-day dosing cycle.

### Claim 21 (depends on 20)

The method of claim 20, wherein each additional dosing cycle comprises administration of an additional dose of mosunetuzumab.

### Claim 22 (depends on 21)

The method of claim 21, wherein each additional dose of mosunetuzumab is 45 mg.

### Claim 23 (depends on 21)

The method of claim 21, wherein the method comprises administering to the subject each additional dose of mosunetuzumab on Day 1 of each respective additional dosing cycle.

### Claim 24 (depends on 1)

The method of claim 1, wherein the dosing regimen comprises one to nine additional dosing cycles, wherein each additional dosing cycle is a 21-day dosing cycle, and wherein each additional dosing cycle comprises administration of an additional dose of 45 mg of mosunetuzumab on Day 1 of each respective additional dosing cycle.

### Claim 25 (depends on 19)

The method of claim 19, wherein each additional dosing cycle is a 28-day dosing cycle.

### Claim 26 (depends on 25)

The method of claim 25, wherein each additional dosing cycle comprises administration of an additional dose of mosunetuzumab.

### Claim 27 (depends on 26)

The method of claim 26, wherein each additional dose of mosunetuzumab is 45 mg.

### Claim 28 (depends on 26)

The method of claim 26, wherein the method comprises administering to the subject each additional dose of mosunetuzumab on Day 1 of each respective additional dosing cycle.

### Claim 29 (depends on 1)

The method of claim 1, wherein the dosing regimen comprises one to nine additional dosing cycles, wherein each additional dosing cycle is a 28-day dosing cycle, and wherein each additional dosing cycle comprises administration of an additional dose of 45 mg of mosunetuzumab on Day 1 of each respective additional dosing cycle.

### Claim 30 (depends on 8)

The method of claim 8, wherein the dosing regimen comprises nine additional dosing cycles.

### Claim 31 (depends on 30)

The method of claim 30, wherein each additional dosing cycle is a 21-day dosing cycle.

### Claim 32 (depends on 31)

The method of claim 31, wherein each additional dosing cycle comprises administration of an additional dose of mosunetuzumab.

### Claim 33 (depends on 32)

The method of claim 32, wherein each additional dose of mosunetuzumab is 45 mg.

### Claim 34 (depends on 32)

The method of claim 32, wherein the method comprises administering to the subject each additional dose of mosunetuzumab on Day 1 of each respective additional dosing cycle.

### Claim 35 (depends on 30)

The method of claim 30, wherein each additional dosing cycle is a 28-day dosing cycle.

### Claim 36 (depends on 35)

The method of claim 35, wherein each additional dosing cycle comprises administration of an additional dose of mosunetuzumab.

### Claim 37 (depends on 36)

The method of claim 36, wherein each additional dose of mosunetuzumab is 45 mg.

### Claim 38 (depends on 36)

The method of claim 36, wherein the method comprises administering to the subject each additional dose of mosunetuzumab on Day 1 of each respective additional dosing cycle.

### Claim 39 (depends on 1)

The method of claim 1, wherein the eight cycles are 21-day dosing cycles.

### Claim 40 (depends on 39)

The method of claim 39, wherein the dosing regimen comprises nine additional dosing cycles, wherein each additional dosing cycle is a 21-day dosing cycle, and wherein each additional dosing cycle comprises administration of an additional dose of 45 mg of mosunetuzumab on Day 1 of each respective additional dosing cycle.

### Claim 41 (depends on 1)

The method of claim 1, wherein the first dosing cycle is a 21-day dosing cycle and the second to eighth dosing cycles are 28-day dosing cycles.

### Claim 42 (depends on 41)

The method of claim 41, wherein the dosing regimen comprises nine additional dosing cycles, wherein each additional dosing cycle is a 28-day dosing cycle, and wherein each additional dosing cycle comprises administration of an additional dose of 45 mg of mosunetuzumab on Day 1 of each respective additional dosing cycle.