# US 12,599,606 B2 · Therapies with 3rd generation EGFR tyrosine kinase inhibitors

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- Number: US 12,599,606 B2
- Document ID: US12599606B2
- Status: Granted
- Kind: B2
- Application number: 18/453,743
- Filed: 2023-08-22
- Published: 2024-06-06
- Granted: 2026-04-14
- Earliest claimed: 2019-05-14
- Assignees: Janssen Biotech, Inc.; Yuhan Corporation
- Applicants: Janssen Biotech, Inc.; Yuhan Corporation
- Inventors: Seonmi Kang; Sewoong Oh
- Web page: https://patentgrep.com/patent/US12599606B2

## CPC

- A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol
- A61P 35/00: Antineoplastic agents
- A61P 35/04: specific for metastasis
- 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 therapies with 3rd generation EGFR tyrosine kinase inhibitors. Embodiments of the invention relate to the administration of lazertinib to patients diagnosed with non-small cell lung cancer (NSCLC).

## Claims

### Claim 1

A method of treating cancer in a human subject comprising administering to the subject (i) lazertinib or a solvate, hydrate, tautomer, or a pharmaceutically acceptable salt thereof, in an amount of about 20 mg to about 320 mg once daily, and (ii) a therapeutically effective amount of an isolated bispecific anti-epidermal growth factor receptor (EGFR)/hepatocyte growth factor receptor (c-Met) antibody,
wherein the cancer is advanced or metastatic non-small cell lung cancer (NSCLC) with EGFR Exon 19 deletions or EGFR exon 21 L858R substitution mutations.

### Claim 2 (depends on 1)

The method of claim 1, wherein the subject exhibits brain metastasis.

### Claim 3 (depends on 1)

The method of claim 1, comprising administering the lazertinib to the subject in an amount of about 80 mg to about 240 mg once daily.

### Claim 4 (depends on 1)

The method of claim 1 comprising administering the lazertinib to the subject in an amount of about 240 mg once daily.

### Claim 5 (depends on 1)

The method of claim 1 comprising administering the lazertinib to the subject in an amount of about 160 mg once daily.

### Claim 6 (depends on 1)

The method of claim 1 comprising administering the lazertinib to the subject in an amount of about 80 mg once daily.

### Claim 7 (depends on 1)

The method of claim 1, wherein the bispecific anti-EGFR/c-Met antibody comprises a first domain that binds EGFR comprising a heavy chain complementarity determining region 1 (HCDR1) of SEQ ID NO: 1, a HCDR2 of SEQ ID NO: 2, a HCDR3 of SEQ ID NO: 3, a light chain complementarity determining region 1 (LCDR1) of SEQ ID NO: 4, a LCDR2 of SEQ ID NO: 5 and a LCDR3 of SEQ ID NO: 6 and a second domain that binds c-Met comprising a HCDR1 of SEQ ID NO: 7, a HCDR2 of SEQ ID NO: 8, a HCDR3 of SEQ ID NO: 9, a LCDR1 of SEQ ID NO: 10, a LCDR2 of SEQ ID NO: 11 and a LCDR3 of SEQ ID NO: 12.

### Claim 8 (depends on 1)

The method of claim 1, wherein the first domain that binds EGFR comprises a heavy chain variable region (VH) of SEQ ID NO: 13 and a light chain variable region (VL) of SEQ ID NO: 14 and the second domain that binds c-Met comprises the VH of SEQ ID NO: 15 and the VL of SEQ ID NO: 16.

### Claim 9 (depends on 1)

The method of claim 1, wherein the bispecific anti-EGFR/c-Met antibody is an IgG 1 isotype.

### Claim 10 (depends on 1)

The method of claim 1, wherein the bispecific anti-EGFR/c-Met antibody comprises a first heavy chain (HC1) of SEQ ID NO: 17, a first light chain (LC1) of SEQ ID NO: 18, a second heavy chain (HC2) of SEQ ID NO: 19 and a second light chain (LC2) of SEQ ID NO: 20.

### Claim 11 (depends on 1)

The method of claim 1, wherein the bispecific anti-EGFR/c-Met antibody has a biantennary glycan structure with a fucose content of between about 1% to about 15%.

### Claim 12 (depends on 1)

The method of claim 1, wherein the lazertinib is a lazertinib mesylate hydrate.