# US 12,005,055 B2 · Methods for shrinking pituitary tumors

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- Number: US 12,005,055 B2
- Document ID: US12005055B2
- Status: Granted
- Kind: B2
- Application number: 17/185,133
- Filed: 2021-02-25
- Published: 2021-06-17
- Granted: 2024-06-11
- Earliest claimed: 2018-11-09
- Assignees: Corcept Therapeutics, Inc.
- Applicants: Corcept Therapeutics Incorporated
- Inventors: Andreas Moraitis
- Web page: https://patentgrep.com/patent/US12005055B2

## CPC

- A61K 31/444: containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
- A61P 35/00: Antineoplastic agents
- A61B 17/3205: Excision instruments
- A61N 5/10: X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy (A61N5/01 takes precedence)
- 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
- A61B: DIAGNOSIS; SURGERY; IDENTIFICATION (usefulness limited to only animals A61D)
- A61N: ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY (measurement of bioelectric currents A61B; surgical instruments, devices or methods for transferring non-mechanical forms of energy to or from the body A61B18/00; anaesthetic apparatus in general A61M; incandescent lamps H01K; infrared radiators for heating H05B)

## Abstract

Pituitary tumors may be reduced in size by administration of relacorilant. Pituitary tumors include, without limitation, non-secreting tumors, hormone-secreting tumors, adenomas, and carcinomas. Relacorilant administration may be effective to reduce hormone secretion from a hormone-secreting pituitary tumor, e.g., to reduce adrenocorticotrophic hormone (ACTH) secretion. A pituitary tumor may be imaged before and/or after relacorilant administration. Relacorilant may be administered independent of surgery, and before, during, or after surgery to treat a pituitary tumor. Relacorilant may aid or improve surgical outcomes, and may reduce the size or growth of pituitary tumor tissue before surgery, and any tumor tissue remaining following surgical treatment. Relacorilant may be orally administered for the treatment of pituitary tumors. Relacorilant may be orally administered to a fasted patient, or to a fed patient. Relacorilant may be administered in conjunction with other pituitary tumor targeting treatments, including surgical treatments, radiation treatments, chemotherapy for carcinomas, and other pharmaceutical treatments.

## Claims

### Claim 1

A method of reducing the size of a visible pituitary macroadenoma tumor in a patient who had not received radiation treatment for said visible pituitary macroadenoma tumor, said visible pituitary macroadenoma tumor having a visible size, the method comprising:
measuring said visible size of said visible pituitary macroadenoma tumor, wherein said measuring comprises a first imaging of the visible pituitary macroadenoma tumor effective to determine that the tumor is a visible pituitary macroadenoma tumor and to determine a first visible size of the visible pituitary macroadenoma tumor, and then, for three months,
administering to said patient an effective amount of relacorilant, where relacorilant is ((R)-(1-(4-fluorophenyl)-64(1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone), which has the following structure:
effective to reduce the size of the visible pituitary macroadenoma tumor from said first visible size of the visible pituitary macroadenoma tumor to a second visible size of the visible pituitary macroadenoma tumor, wherein said second visible size is at least about 27% smaller than the first visible size of the visible pituitary macroadenoma tumor,
wherein the size of the visible pituitary macroadenoma tumor is reduced in the patient who had not received radiation treatment for the visible pituitary macroadenoma tumor.

### Claim 2 (depends on 1)

The method of claim 1, wherein said selecting further comprises determining that said patient suffers from a symptom of Cushing's syndrome.

### Claim 3 (depends on 1)

The method of claim 1, wherein said patient suffers from Cushing's Disease.

### Claim 4 (depends on 1)

The method of claim 1, further comprising measuring the visible size of the visible pituitary macroadenoma tumor following relacorilant administration, wherein said measuring comprises a second imaging of the visible pituitary macroadenoma tumor effective to determine said second visible size of the visible pituitary macroadenoma tumor.

### Claim 5 (depends on 4)

The method of claim 4, further comprising application of a further treatment targeting said visible pituitary macroadenoma tumor following said second imaging of the visible pituitary macroadenoma tumor.

### Claim 6 (depends on 5)

The method of claim 5, wherein said further treatment targeting said visible pituitary macroadenoma tumor comprises surgical treatment, radiation treatment, or both surgical treatment and radiation treatment.

### Claim 7 (depends on 1)

The method of claim 1, wherein said relacorilant administration comprises oral administration of relacorilant to the selected patient.

### Claim 8 (depends on 1)

The method of claim 1, wherein the visible pituitary macroadenoma tumor is a non-secreting pituitary tumor.

### Claim 9 (depends on 1)

The method of claim 1, wherein the visible pituitary macroadenoma tumor is a hormone-secreting tumor, and said treatment is effective to reduce hormone secretion from the visible pituitary macroadenoma tumor.

### Claim 10 (depends on 9)

The method of claim 9, wherein the visible pituitary macroadenoma tumor is hormone-secreting tumor, and the visible pituitary macroadenoma tumor secretes a hormone selected from adrenocorticotrophic hormone, prolactin, growth hormone, thyroid stimulating hormone, follicle stimulating hormone, luteinizing hormone, melanocyte stimulating hormone, β-lipotropin, oxytocin, and vasopressin.

### Claim 11 (depends on 1)

The method of claim 1, wherein said relacorilant administration comprises daily administration of between about 20 milligrams (mg) to about 800 mg of relacorilant.

### Claim 12 (depends on 1)

The method of claim 1, wherein said relacorilant administration comprises daily administration of relacorilant in single unit dosage forms each containing an amount of relacorilant selected from 50 milligrams (mg), 100 mg, 150 mg, 200 mg, 250 mg, 300 mg, 350 mg, 400 mg, 450 mg, and 500 mg of relacorilant.

### Claim 13 (depends on 1)

The method of claim 1, wherein said administration of relacorilant comprises relacorilant administration prior to surgery for resection of the visible pituitary macroadenoma tumor.

### Claim 14 (depends on 1)

The method of claim 1, wherein said administration of relacorilant comprises relacorilant administration following surgery for resection of the visible pituitary macroadenoma tumor.

### Claim 15 (depends on 14)

The method of claim 14, wherein some tumor tissue remains visible in the patient following said surgery, wherein said relacorilant administration following surgery for resection of the visible pituitary macroadenoma tumor is effective to reduce the visible size of tumor tissue remaining in the patient following said surgical treatment.

### Claim 16 (depends on 15)

The method of claim 15, further comprising administration of radiation treatment or cancer chemotherapy treatment, or both, to said patient receiving relacorilant administration following surgery for resection of the visible pituitary macroadenoma tumor.

### Claim 17 (depends on 1)

The method of claim 1, wherein said administration of relacorilant to the selected patient comprises relacorilant administration to a patient who has been administered another pharmaceutical or medical treatment prior to, or at the same time as, said relacorilant administration.

### Claim 18 (depends on 1)

The method of claim 1, wherein said administration of relacorilant to the selected patient comprises relacorilant administration to the selected patient, followed by surgical treatment to resect the visible pituitary macroadenoma tumor, then followed by further relacorilant administration.

### Claim 19 (depends on 1)

The method of claim 1, wherein said administration of relacorilant to the selected patient comprises relacorilant administration to the patient, followed by surgical treatment to resect the visible pituitary macroadenoma tumor, then followed by radiation treatment targeting the visible pituitary macroadenoma tumor and/or regions near the location previously occupied by the visible pituitary macroadenoma tumor.

### Claim 20 (depends on 1)

The method of claim 1, wherein the visible pituitary macroadenoma tumor is hormone-secreting tumor, and the visible pituitary macroadenoma tumor secretes a hormone selected from adrenocorticotrophic hormone, prolactin, growth hormone, thyroid stimulating hormone, follicle stimulating hormone, luteinizing hormone, melanocyte stimulating hormone, β-lipotropin, oxytocin, and vasopressin.