# US 10,441,587 B2 · Treatment of lung cancer with inhibitors of glutaminase

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- Number: US 10,441,587 B2
- Document ID: US10441587B2
- Status: Granted
- Kind: B2
- Application number: 15/091,816
- Filed: 2016-04-06
- Published: 2016-10-06
- Granted: 2019-10-15
- Earliest claimed: 2015-04-06
- Assignees: Calithera Biosciences, Inc.
- Applicants: Calithera Biosciences, Inc.
- Inventors: Francesco Parlati; Melissa G. Works; Mirna L. M. Rodriguez; Dong Zhang
- Web page: https://patentgrep.com/patent/US10441587B2

## CPC

- A61K 31/501: not condensed and containing further heterocyclic rings
- A61K 31/4184: condensed with carbocyclic rings, e.g. benzimidazoles
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 35/00: Antineoplastic agents
- 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)
- C12Q 2600/106: Pharmacogenomics, i.e. genetic variability in individual responses to drugs and drug metabolism
- C12Q 2600/156: Polymorphic or mutational markers
- C12Q 2600/158: Expression 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

## Abstract

The invention relates to methods of treating lung cancer using glutaminase inhibitors. In particular, results demonstrate that lung cancers characterized by an EGFR or KRAS mutation are treated by glutaminase inhibitors.

## Claims

### Claim 1

A method for therapeutically treating lung cancer in a patient, the method comprising:
a) determining whether the lung cancer is characterized by a KRAS mutation or EGFR mutation; and
b) if the lung cancer is characterized by a KRAS mutation or EGFR mutation, then administering to the patient an effective amount of a compound of Formula III:
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein the mutation results in an expression level of KRAS or EGFR that is different from normal lung cells, or in a level of constitutive activity of KRAS or EGFR that is different from normal lung cells.

### Claim 3 (depends on 1)

The method of claim 1, wherein the mutation results in overexpression or increased constitutive activity of KRAS or EGFR.

### Claim 4 (depends on 3)

The method of claim 3, wherein the mutation is an amplification of the gene encoding KRAS or EGFR.

### Claim 5 (depends on 3)

The method of claim 3, wherein the mutation is a deletion in the gene encoding KRAS or EGFR.

### Claim 6 (depends on 3)

The method of claim 3, wherein the mutation is an insertion in the gene encoding KRAS or EGFR.

### Claim 7 (depends on 3)

The method of claim 3, wherein the mutation is a point mutation resulting in a change of at least one amino acid residue in the amino acid sequence of KRAS or EGFR protein.

### Claim 8 (depends on 1)

The method of claim 1, wherein the lung cancer is non-small cell lung carcinoma (NSCLC).

### Claim 9 (depends on 1)

The method of claim 1, further comprising conjointly administering radiation therapy.

### Claim 10 (depends on 1)

The method of claim 1, further comprising conjointly administering one or more additional chemotherapeutic agents.

### Claim 11 (depends on 10)

The method of claim 10, wherein the one or more additional chemotherapeutic agents are selected from afatinib dimaleate, bevacizumab, carboplatin, ceritinib, cisplatin, crizotinib, docetaxel, doxorubicin hydrochloride; erlotinib hydrochloride, etoposide, gefitinib, gemcitabine hydrochloride, mechlorethamine hydrochloride, methotrexate, paclitaxel, pemetrexed disodium, ramucirumab, topotecan hydrochloride, vinorelbine tartrate.

### Claim 12 (depends on 10)

The method of claim 10, wherein the one or more additional chemotherapeutic agents is selumetinib.