# US 2025/0195533 A1 · Combination therapies for the treatment of cancer

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- Number: US 2025/0195533 A1
- Document ID: US20250195533A1
- Status: Published application
- Kind: A1
- Application number: 18/256,091
- Filed: 2021-12-10
- Published: 2025-06-19
- Earliest claimed: 2020-12-11
- Assignees: Erasca, Inc.
- Applicants: Erasca, Inc.
- Inventors: Leenus MARTIN; Leslie Harris BRAIL; Robert Field SHOEMAKER
- Web page: https://patentgrep.com/patent/US20250195533A1

## CPC

- A61K 31/5383: ortho- or peri-condensed with heterocyclic ring systems
- C07D 519/00: Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/4709: Non-condensed quinolines and containing further heterocyclic rings
- A61K 31/517: ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 35/00: Antineoplastic agents
- 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)
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present disclosure provides methods of treating cancer with combination therapies of a SHP2 inhibitor and a KRAS G12C inhibitor.

## Claims

### Claim 1

A method of treating a subject having cancer comprising administering to the subject a therapeutically effective amount of a compound of Formula I or its pharmaceutically acceptable salt:
in combination with a KRAS inhibitor.

### Claim 2 (depends on 1)

The method of claim 1, wherein the cancer comprises a KRAS G12, G13, H95, Q61, R68, or Y96 mutation.

### Claim 3 (depends on 1)

The method of claim 1, wherein the cancer has a G12C KRAS mutation, a G12D KRAS mutation, a G12R KRAS mutation, a G12S KRAS mutation, a G12V KRAS mutation, a G12W KRAS mutation, a G13D KRAS mutation, a H95D KRAS mutation, a H95Q KRAS mutation, a H95R KRAS mutation, a Q61H KRAS mutation, a 061K KRAS mutation, or a R68S KRAS mutation.

### Claim 4 (depends on 1)

The method of claim 1, wherein the cancer has a G12C KRAS mutation.

### Claim 5

(canceled)

### Claim 6

(canceled)

### Claim 7 (depends on 1)

The method of claim 1, wherein the KRAS inhibitor is selected from the group consisting of sotorasib, adagrasib, ARS-3248, GDC-6036, BI 1701963, tipifarnib, and BBP-454.

### Claim 8

(canceled)

### Claim 9

(canceled)

### Claim 10

(canceled)

### Claim 11

(canceled)

### Claim 12 (depends on 1)

The method of claim 1, wherein the method comprises administering a third MAPK pathway inhibitor.

### Claim 13 (depends on 1)

The method of claim 1, wherein the administration is oral.

### Claim 14 (depends on 1)

The method of claim 1, wherein the dosing of the compound of Formula I is in a range from 20 mg to 400 mg daily, 10 mg to 300 mg 10 mg to 140 mg 10 mg to 100 mg, or 5 mg to 50 mg.

### Claim 15

(canceled)

### Claim 16

(canceled)

### Claim 17

(canceled)

### Claim 18

(canceled)

### Claim 19

(canceled)

### Claim 20

A kit comprising a compound of Formula I or a pharmaceutically acceptable salt thereof:
and a KRAS inhibitor.

### Claim 21

(canceled)

### Claim 22

(canceled)

### Claim 23

(canceled)

### Claim 24

(canceled)

### Claim 25

(canceled)

### Claim 26

(canceled)

### Claim 27

(canceled)

### Claim 28

(canceled)

### Claim 29

(canceled)

### Claim 30

(canceled)

### Claim 31

(canceled)

### Claim 32 (depends on 1)

The method of claim 1, wherein the compound of Formula I, or a pharmaceutically acceptable salt thereof, is administered once or twice a day.

### Claim 33

(canceled)

### Claim 34

(canceled)

### Claim 35

(canceled)

### Claim 36

(canceled)

### Claim 37

(canceled)

### Claim 38

(canceled)

### Claim 39

(canceled)

### Claim 40

(canceled)

### Claim 41

(canceled)

### Claim 42

(canceled)

### Claim 43

(canceled)

### Claim 44

(canceled)

### Claim 45

(canceled)

### Claim 46

(canceled)

### Claim 47 (depends on 1)

The method of claim 1, wherein the cancer is selected from head and neck cancer, lung cancer, stomach cancer, liver cancer, colon cancer, colorectal cancer, kidney cancer, breast cancer, pancreatic cancer, pancreatic ductal adenocarcinoma (PDAC), juvenile myelomonocytic leukemia, neuroblastoma, melanoma, and acute myeloid leukemia.