# US 10,946,005 B2 · Methods for shrinking pituitary tumors

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- Number: US 10,946,005 B2
- Document ID: US10946005B2
- Status: Granted
- Kind: B2
- Application number: 16/678,988
- Filed: 2019-11-08
- Published: 2020-05-14
- Granted: 2021-03-16
- Earliest claimed: 2018-11-09
- Assignees: Corcept Therapeutics, Inc.
- Applicants: Corcept Therapeutics Incorporated
- Inventors: Andreas Moraitis
- Web page: https://patentgrep.com/patent/US10946005B2

## 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 tumor in a patient, the method comprising selecting a patient suffering from a visible pituitary macroadenoma tumor who has not been treated with radiation, said pituitary tumor occupying a location within said patient, said selecting comprising imaging the pituitary tumor effective to determine that the pituitary tumor is a visible macroadenoma and to determine a first size of the pituitary tumor, and then, for three months, administering to the selected patient an effective amount of relacorilant, where relacorilant is ((R)-(1-(4-fluorophenyl)-6-((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 pituitary tumor from said first size to a second size, wherein said second size is smaller than said first size following said three months of relacorilant administration.

### 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 said pituitary tumor following relacorilant administration, wherein said measuring comprises a second imaging of the pituitary tumor, and wherein said size is reduced by at least about 27%.

### Claim 5 (depends on 1)

The method of claim 1, wherein said relacorilant administration comprises oral administration of relacorilant.

### Claim 6 (depends on 1)

The method of claim 1, wherein said pituitary tumor is a non-secreting pituitary tumor.

### Claim 7 (depends on 1)

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

### Claim 8 (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 9 (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 10 (depends on 4)

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

### Claim 11 (depends on 10)

The method of claim 10, wherein said pituitary tumor targeting treatment comprises surgical treatment.

### Claim 12 (depends on 5)

The method of claim 5, wherein said administration of relacorilant comprises oral administration of relacorilant to a fasted patient.

### Claim 13 (depends on 12)

The method of claim 12, wherein said fasted patient is a patient who has not eaten a meal or otherwise ingested food for at least two hours prior to the administration of relacorilant.

### Claim 14 (depends on 5)

The method of claim 5, wherein said administration of relacorilant comprises oral administration of relacorilant to a fed patient.

### Claim 15 (depends on 14)

The method of claim 14, wherein said fed patient is a patient who has begun eating a meal about 30 minutes or less prior to the administration of relacorilant.

### Claim 16 (depends on 14)

The method of claim 14, wherein a fed patient is a patient who has begun eating a meal about one hour or less prior to the administration of relacorilant.

### Claim 17 (depends on 1)

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

### Claim 18 (depends on 1)

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

### Claim 19 (depends on 18)

The method of claim 18, wherein said relacorilant administration following surgery for resection of the tumor is effective to reduce the size of, or growth of, tumor tissue remaining in the patient following said surgical treatment.

### Claim 20 (depends on 19)

The method of claim 19, further comprising administration of radiation treatment or cancer chemotherapy treatment, or both, to said patient receiving relacorilant administration following surgery for resection of the tumor.

### Claim 21 (depends on 1)

The method of claim 1, wherein said administration of relacorilant 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 22 (depends on 1)

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

### Claim 23 (depends on 1)

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

### Claim 24 (depends on 5)

The method of claim 5, wherein said administration of relacorilant comprises relacorilant administration to a patient, followed by surgical treatment to resect said pituitary tumor, then followed by further relacorilant administration.

### Claim 25 (depends on 5)

The method of claim 5, wherein said administration of relacorilant comprises relacorilant administration to a patient, followed by surgical treatment to resect said pituitary tumor, then followed by radiation treatment targeting the pituitary tumor and/or regions near said location previously occupied by said pituitary tumor.

### Claim 26 (depends on 14)

The method of claim 14, wherein said administration of relacorilant comprises relacorilant administration to a patient, followed by surgical treatment to resect said pituitary tumor, then followed by further relacorilant administration.

### Claim 27 (depends on 14)

The method of claim 14, wherein said administration of relacorilant comprises relacorilant administration to a patient, followed by surgical treatment to resect said pituitary tumor, then followed by radiation treatment targeting the pituitary tumor and/or regions near said location previously occupied by said pituitary tumor.

### Claim 28 (depends on 1)

The method of claim 1, wherein said pituitary tumor is hormone-secreting tumor, and said 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 29 (depends on 5)

The method of claim 5, wherein said pituitary tumor is hormone-secreting tumor, and said 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 30 (depends on 7)

The method of claim 7, wherein said pituitary tumor is hormone-secreting tumor, and said 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.