# US 2022/0031801 A1 · METHODS OF TREATING PROSTATE CANCER WITH GnRH ANTAGONIST

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- Number: US 2022/0031801 A1
- Document ID: US20220031801A1
- Status: Published application
- Kind: A1
- Application number: 17/199,733
- Filed: 2021-03-12
- Published: 2022-02-03
- Earliest claimed: 2008-02-11
- Assignees: Ferring B.V.
- Applicants: Ferring B.V.
- Inventors: Tine Kold Olesen; Bo-Eric Persson; Per Cantor; Egbert A. van der Meulen; Jens-Kristian Slott Jensen
- Web page: https://patentgrep.com/patent/US20220031801A1

## CPC

- A61K 38/09: Luteinising hormone-releasing hormone [LHRH] {, i.e. Gonadotropin-releasing hormone [GnRH]}; Related peptides
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 38/08: Peptides having 5 to 11 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention provides methods and dosing regimens for safely and effectively treating androgen-dependent prostate cancer with a gonadotrophin releasing hormone (GnRH) antagonist without causing a testosterone spike and/or other side effect of GnRH agonist therapy such as a urinary tract infection, or an arthralgia-related or cardiovascular side effect.

## Claims

### Claim at position 1

1-89. (canceled)

### Claim 90

A method of treating advanced stage prostate cancer in a subject, comprising:
administering an initial dose of 160-320 mg of degarelix to the subject and a maintenance dose of 60-160 mg of degarelix to the subject, wherein the maintenance dose is administered once every 20-36 days thereafter,
wherein the treated subject has a decreased likelihood of developing arthralgia or musculoskeletal stiffness during treatment compared to a treatment with a gonadotrophin releasing hormone (GnRH) agonist.

### Claim 91

A method of treating advanced stage prostate cancer in a subject, comprising:
administering an initial dose of 160-320 mg of degarelix to the subject and a maintenance dose of 60-160 mg of degarelix to the subject, wherein the maintenance dose is administered once every 20-36 days thereafter,
wherein the treated subject has a decreased likelihood of developing noninfective cystitis during treatment compared to a treatment with a gonadotrophin releasing hormone (GnRH) agonist.

### Claim 92

A method of treating advanced stage prostate cancer in a subject, comprising:
administering an initial dose of 160-320 mg of degarelix to the subject and a maintenance dose of 60-160 mg of degarelix to the subject, wherein the maintenance dose is administered once every 20-36 days thereafter,
wherein the treated subject has a decreased likelihood of developing a urinary or renal system disorder during treatment compared to a treatment with a gonadotrophin releasing hormone (GnRH) agonist.

### Claim 93

A method of treating advanced stage prostate cancer in a subject, comprising:
administering an initial dose of 160-320 mg of degarelix to the subject and a maintenance dose of 60-160 mg of degarelix to the subject, wherein the maintenance dose is administered once every 20-36 days thereafter,
wherein the treated subject has a decreased likelihood of developing erectile dysfunction during treatment compared to a treatment with a gonadotrophin releasing hormone (GnRH) agonist.

### Claim 94

A method of treating advanced stage prostate cancer in a subject, comprising:
administering an initial dose of 160-320 mg of degarelix to the subject and a maintenance dose of 60-160 mg of degarelix to the subject, wherein the maintenance dose is administered once every 20-36 days thereafter,
wherein the treated subject has at least about a 50% decrease in prostate specific antigen (PSA) by day 14 of treatment.

### Claim 95 (depends on 90)

The method of claim 90, wherein the subject is less than 65 years old.

### Claim 96 (depends on 90)

The method of claim 90, wherein the initial dose is 240 mg of degarelix and the maintenance dose is about 80 mg of degarelix, wherein the maintenance dose is administered once every approximately 28 days of treatment.

### Claim 97 (depends on 90)

The method of claim 90, wherein the initial dose of degarelix is administered as two subcutaneous injections.

### Claim 98 (depends on 90)

The method of claim 90, wherein the maintenance dose of degarelix is administered monthly.

### Claim 99 (depends on 90)

The method of claim 90, wherein the GnRH agonist is leuprolide.

### Claim 100 (depends on 90)

The method of claim 90, wherein the subject has a body mass index of less than 30 kg/m2.

### Claim 101 (depends on 90)

The method of claim 90, wherein the initial dose of degarelix is administered at a concentration ranging from 5 mg/mL to 40 mg/mL.

### Claim 102 (depends on 90)

The method of claim 90, wherein the initial dose of degarelix is administered at a concentration of 40 mg/mL.

### Claim 103 (depends on 90)

The method of claim 90, wherein the maintenance dose of degarelix is administered as a single injection.

### Claim 104 (depends on 90)

The method of claim 90, wherein the maintenance dose of degarelix is administered at a concentration ranging from 5 mg/mL to 40 mg/mL.

### Claim 105 (depends on 90)

The method of claim 90, wherein the maintenance dose of degarelix is administered at a concentration of 20 mg/mL.

### Claim 106 (depends on 94)

The method of claim 94, wherein the treated subject has at least about a 60% decrease in PSA by day 28 of treatment.

### Claim 107 (depends on 94)

The method of claim 94, wherein the treated subject has at least about a 75% decrease in PSA by day 28 of treatment.