# US 2021/0330653 A1 · Dosage Regimen for the Treatment of Cancer

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- Number: US 2021/0330653 A1
- Document ID: US20210330653A1
- Status: Published application
- Kind: A1
- Application number: 17/237,112
- Filed: 2021-04-22
- Published: 2021-10-28
- Earliest claimed: 2020-04-24
- Applicants: AstraZeneca AB
- Inventors: Pablo MORENTIN GUTIERREZ; Camila DE ALMEIDA; Eric Todd GANGL
- Web page: https://patentgrep.com/patent/US20210330653A1

## CPC

- A61K 31/444: containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
- A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)}
- A61K 31/436: the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
- A61K 31/4745: condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines (yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48)
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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 present specification relates to AZD9833 for use in the treatment of cancer and methods of treatment of cancer involving administration of AZD9833 wherein, in each case, the AZD9833 is administered orally once daily at a dose between 25 mg and 450 mg. AZD9833 may be administered alone or its use may be in combination with an additional anti-cancer agent such as a CDK inhibitor, everolimus or an AKT inhibitor.

## Claims

### Claim at position 1

-28. (canceled)

### Claim 29

A method of treating cancer in a human or animal patient in need of such treatment, comprising administering to the patient a compound, or a pharmaceutically acceptable salt thereof, once daily at a dose between 25 mg and 450 mg, wherein the compound is N-(1-(3-fluoropropyl)azetidin-3-yl)-6-((6S,8R)-8-methyl-7-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinolin-6-yl)pyridin-3-amine.

### Claim 30 (depends on 29)

The method of claim 29, wherein the dose is selected from 25 mg, 75 mg, 150 mg, 300 mg, and 450 mg.

### Claim 31 (depends on 29)

The method of claim 29, wherein the compound is administered as a single dose unit or as multiple dose units.

### Claim 32 (depends on 31)

The method of claim 31, wherein the compound is administered as a single tablet.

### Claim 33 (depends on 29)

The method of claim 29, wherein the compound is administered in combination with a further anti-cancer therapy.

### Claim 34 (depends on 29)

The method of claim 29, wherein the compound is administered in combination with a CDK inhibitor.

### Claim 35 (depends on 34)

The method of claim 34, wherein the compound is administered in combination with palbociclib, ribociclib, abemaciclib, lerociclib, or trilaciclib.

### Claim 36 (depends on 34)

The method of claim 34, wherein the compound is administered in combination with palbociclib.

### Claim 37 (depends on 29)

The method of claim 29, wherein the compound is administered in combination with an mTOR inhibitor.

### Claim 38 (depends on 37)

The method of claim 37, wherein the compound is administered in combination with everolimus.

### Claim 39 (depends on 29)

The method of claim 29, wherein the cancer is selected from breast cancer and gynaecological cancer.

### Claim 40 (depends on 39)

The method of claim 39, wherein the cancer is ER-positive HER2-negative advanced breast cancer.

### Claim 41 (depends on 29)

The method of claim 29, wherein the compound is administered to a pre- or post-menopausal woman.

### Claim 42 (depends on 29)

The method of claim 29, wherein the cancer has previously been treated with one or more endocrine therapies and no more than two prior chemotherapies for ER-positive HER2-negative advanced breast cancer.

### Claim 43 (depends on 29)

The method of claim 29, wherein the compound is administered to a patient whose cancer is resistant to non-steroidal aromatase inhibitors.

### Claim 44 (depends on 29)

The method of claim 29, wherein the dose achieves a mean peak blood plasma concentration in the patient between 10 ng/mL and 1000 ng/mL.

### Claim 45 (depends on 29)

The method of claim 29, wherein the dose of the compound achieves a median terminal half-life in the patient between 8 hours and 14 hours.

### Claim 46 (depends on 29)

The method of claim 29, wherein the dose achieves a median terminal half-life in the patient of 12 hours.

### Claim 47 (depends on 29)

The method of claim 29, wherein the dose achieves an objective response rate in the patient between 10% and 20%.

### Claim 48 (depends on 29)

The method of claim 29, wherein the dose does not cause any serious side-effects in the patient.

### Claim 49

An oral pharmaceutical composition comprising between 25 mg and 450 mg of a compound, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient; wherein the compound is N-(1-(3-fluoropropyl)azetidin-3-yl)-6-((6S,8R)-8-methyl-7-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinolin-6-yl)pyridin-3-amine.

### Claim 50 (depends on 49)

The composition of claim 49, wherein the composition contains 25 mg, 75 mg, 150 mg, 300 mg, or 450 mg of the compound.

### Claim 51 (depends on 50)

The composition of claim 50, wherein the composition contains 75 mg of the compound.

### Claim 52 (depends on 50)

The composition of claim 50, wherein the composition contains 150 mg of the compound.

### Claim 53 (depends on 49)

The composition of claim 49 in the form of a single tablet.

### Claim 54

A kit comprising:
an oral pharmaceutical composition comprising from 25 mg to 450 mg of N-(1-(3-fluoropropyl)azetidin-3-yl)-6-((6S,8R)-8-methyl-7-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinolin-6-yl)pyridin-3-amine, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient; and
instructions for the use of the composition in the treatment of cancer.

### Claim 55 (depends on 54)

The kit of claim 54, further comprising an additional anti-cancer agent for administration in combination with the composition.