# US 10,441,663 B2 · Methods for treating cancer

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- Number: US 10,441,663 B2
- Document ID: US10441663B2
- Status: Granted
- Kind: B2
- Application number: 15/822,437
- Filed: 2017-11-27
- Published: 2018-06-21
- Granted: 2019-10-15
- Earliest claimed: 2016-11-27
- Assignees: BicycleRD Limited
- Applicants: Bicycle Therapeutics Limited
- Inventors: Gavin Bennett; Daniel Paul Teufel
- Web page: https://patentgrep.com/patent/US10441663B2

## CPC

- A61K 47/64: Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent (peptidic linkers A61K47/65)
- A61K 38/12: Cyclic peptides {, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C (A61K38/043 - A61K38/046 take precedence)}
- A61P 35/00: Antineoplastic agents
- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- C07K 14/00: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- 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
- 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)

## Abstract

The present invention relates to a method of treating cancer in a subject.

## Claims

### Claim 1

A method of treating cancer in a patient, wherein the cancer is selected from the group consisting of a sarcoma, lung cancer, breast cancer, colon cancer, gastric cancer, and head and neck cancer, comprising administering to said patient a therapeutically effective amount of BT1718, or a pharmaceutically acceptable salt and/or composition thereof,
wherein
the sarcoma is an N-ras mutant/IDH1 mutant soft tissue sarcoma (STS);
the lung cancer is a Met-amplified squamous NSCLC, a Squamous cell NSCLC with wt EGFR, or a T790M EGFR-expressing lung adenocarcinoma;
the breast cancer is a triple negative breast cancer;
the colon cancer is a colorectal adenocarcinoma;
the gastric cancer is a FGFR-amplified gastric cancer; and
the head and neck cancer is a nasal septum squamous cell carcinoma,
and wherein BT1718 is a Bicycle drug conjugate of formula:

### Claim 2 (depends on 1)

The method of claim 1, wherein the cancer is an N-ras mutant/IDH1 mutant soft tissue sarcoma (STS).

### Claim 3 (depends on 1)

The method of claim 1, wherein the cancer is a triple negative breast cancer.

### Claim 4 (depends on 3)

The method of claim 3, wherein the triple negative breast cancer is a basaloid triple negative breast cancer.

### Claim 5 (depends on 1)

The method of claim 1, wherein the cancer is a colorectal adenocarcinoma.

### Claim 6 (depends on 1)

The method of claim 1, wherein the cancer is a FGFR-amplified gastric cancer.

### Claim 7 (depends on 1)

The method of claim 1, wherein the cancer is a nasal septum squamous cell carcinoma.

### Claim 8

A method of treating cancer in a patient, wherein the cancer is selected from the group consisting of a sarcoma, lung cancer, breast cancer, colon cancer, gastric cancer, and head and neck cancer, comprising administering to said patient a minimally effective dose of BT1718, or a pharmaceutically acceptable salt and/or composition thereof, wherein the minimally effective dose leads to tumor-stasis when administered intravenous twice a week (IV BIW),
wherein
the sarcoma is an N-ras mutant/IDH1 mutant soft tissue sarcoma (STS);
the lung cancer is a Met-amplified squamous NSCLC, a Squamous cell NSCLC with wt EGFR, or a T790M EGFR-expressing lung adenocarcinoma;
the breast cancer is a triple negative breast cancer;
the colon cancer is a colorectal adenocarcinoma;
the gastric cancer is a FGFR-amplified gastric cancer; and
the head and neck cancer is a nasal septum squamous cell carcinoma,
and wherein BT1718 is a Bicycle drug conjugate of formula:

### Claim 9 (depends on 8)

The method of claim 8, wherein the cancer is a triple negative breast cancer, and the minimally effective dose is <10 mg/kg.

### Claim 10 (depends on 8)

The method of claim 8, wherein the cancer is a FGFR-amplified gastric cancer, and the minimally effective dose is 3 mg/kg.

### Claim 11 (depends on 8)

The method of claim 8, wherein the cancer is an N-ras mutant/IDH1 mutant soft tissue sarcoma (STS), and the minimally effective dose is <3 mg/kg.

### Claim 12 (depends on 8)

The method of claim 8, wherein the cancer is a basaloid triple negative breast cancer, and the minimally effective dose is <10 mg/kg.

### Claim 13 (depends on 8)

The method of claim 8, wherein the cancer is a high pgp-expressing colorectal adenocarcinoma, and the minimally effective dose is >10 mg/kg.

### Claim 14 (depends on 8)

The method of claim 8, wherein the cancer is a colorectal adenocarcinoma, and the minimally effective dose is 10 mg/kg.

### Claim 15 (depends on 8)

The method of claim 8, wherein the cancer is a nasal septum squamous cell carcinoma, and the minimally effective dose is 10 mg/kg.

### Claim 16 (depends on 8)

The method of claim 8, wherein the cancer is a Met-amplified squamous NSCLC, and the minimally effective dose is <10 mg/kg.

### Claim 17 (depends on 8)

The method of claim 8, wherein the cancer is a Squamous cell NSCLC with wt EGFR, and the minimally effective dose is <10 mg/kg.

### Claim 18 (depends on 8)

The method of claim 8, wherein the cancer is a T790M EGFR-expressing lung adenocarcinoma, and the minimally effective dose is <10 mg/kg.

### Claim 19 (depends on 5)

The method of claim 5, wherein the colorectal adenocarcinoma is a high pgp-expressing colorectal adenocarcinoma.

### Claim 20 (depends on 1)

The method of claim 1, wherein the cancer is a Met-amplified squamous NSCLC.

### Claim 21 (depends on 1)

The method of claim 1, wherein the cancer is a Squamous cell NSCLC with wt EGFR.

### Claim 22 (depends on 1)

The method of claim 1, wherein the cancer is a T790M EGFR-expressing lung adenocarcinoma.