# US 12,599,593 B2 · Methods and compositions for treating non-ERK MAPK pathway inhibitor-resistant cancers

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- Number: US 12,599,593 B2
- Document ID: US12599593B2
- Status: Granted
- Kind: B2
- Application number: 17/561,076
- Filed: 2021-12-23
- Published: 2022-04-21
- Granted: 2026-04-14
- Earliest claimed: 2013-12-20
- Assignees: Biomed Valley Discoveries, Inc.
- Applicants: Biomed Valley Discoveries, Inc.
- Inventors: Saurabh Saha; Dean Welsch; Gary Decrescenzo; Jeffrey Roix
- Web page: https://patentgrep.com/patent/US12599593B2

## CPC

- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61K 31/506: not condensed and containing further heterocyclic rings
- 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 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 31/12: Antivirals
- A61P 35/00: Antineoplastic agents
- A61P 35/04: specific for metastasis
- A61P 37/04: Immunostimulants
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C12Q 1/6886: for cancer (immunoassay for cancer G01N33/575)
- G01N 33/5758: {involving compounds serving as markers for tumours, cancers or neoplasias, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides or metabolites}
- C12Q 2600/106: Pharmacogenomics, i.e. genetic variability in individual responses to drugs and drug metabolism
- C12Q 2600/156: Polymorphic or mutational markers
- 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
- C12Q: MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS (immunoassay G01N33/53); COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

The present invention provides, inter alia, methods, pharmaceutical compositions, and kits for treating or ameliorating the effects of a cancer in a subject, which cancer is refractory or resistant to non-ERK MAPK pathway inhibitor therapy. Also provided are methods for identifying a subject having cancer who would benefit from therapy with an ERK inhibitor and methods for inhibiting phosphorylation of RSK in a cancer cell that is refractory or resistant to a non-ERK MAPK pathway inhibitor.

## Claims

### Claim 1

A method for treating or ameliorating effects of a cancer selected from pancreatic cancer, papillary thyroid cancer, colorectal cancer, non-small cell lung cancer, ovarian cancer, endometrioid endometrial cancer or melanoma in a subject, comprising administering to the subject an effective amount of (i) BVD-523 (ulixertinib) that has a structure of
or a pharmaceutically acceptable salt thereof, and (ii) SCH772984.

### Claim 2 (depends on 1)

The method of claim 1, wherein the cancer is melanoma.

### Claim 3 (depends on 1)

The method of claim 1, wherein the cancer is pancreatic cancer.

### Claim 4 (depends on 1)

The method of claim 1, wherein the subject is selected from the group consisting of humans, primates, farm animals, and domestic animals.

### Claim 5 (depends on 1)

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

### Claim 6 (depends on 1)

The method of claim 1, wherein the subject has previously received an anti-cancer agent selected from a RAS inhibitor, a RAF inhibitor, a MEK inhibitor, and combinations thereof.

### Claim 7 (depends on 1)

The method of claim 1, comprising administering to the subject at least 100 mg/kg body weight BID of BVD-523 or a pharmaceutically acceptable salt thereof.

### Claim 8 (depends on 7)

The method of claim 7, comprising administering to the subject 600 mg/kg body weight BID of BVD-523 or a pharmaceutically acceptable salt thereof.