# US 11,896,717 B2 · Sustained-release dosage forms of ruxolitinib

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- Number: US 11,896,717 B2
- Document ID: US11896717B2
- Status: Granted
- Kind: B2
- Application number: 18/090,547
- Filed: 2022-12-29
- Published: 2023-05-04
- Granted: 2024-02-13
- Earliest claimed: 2012-11-15
- Assignees: Incyte Holdings Corporation; Incyte Corporation
- Applicants: Incyte Corporation; Incyte Holdings Corporation
- Inventors: Yong Ni; Bhavnish Parikh; Krishnaswamy Yeleswaram; Susan Erickson-Viitanen; William V. Williams
- Web page: https://patentgrep.com/patent/US11896717B2

## CPC

- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/14: Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 3/02: Nutrients, e.g. vitamins, minerals
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 3/14: for calcium homeostasis (vitamin D A61P3/02; parathyroid hormones A61P5/18; calcitonin A61P5/22; osteoporosis A61P19/10; bone metastasis A61P35/04)
- A61P 5/14: of the thyroid hormones, e.g. T3, T4
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 13/08: of the prostate
- A61P 13/12: of the kidneys
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/04: Antipruritics
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/08: for bone diseases, e.g. rachitism, Paget's disease
- A61P 19/10: for osteoporosis
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 21/04: for myasthenia gravis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 27/02: Ophthalmic agents
- A61P 27/14: Decongestants or antiallergics
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/12: Antivirals
- A61P 31/14: for RNA viruses
- A61P 31/18: for HIV
- A61P 31/20: for DNA viruses
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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 invention relates to sustained-release formulations and dosage forms of ruxolitinib, or a pharmaceutically acceptable salt thereof, which are useful in the treatment of Janus kinase-associated diseases such as myeloproliferative disorders.

## Claims

### Claim 1

An oral sustained release dosage form comprising:
ruxolitinib phosphate, and
a means for sustained release of the ruxolitinib phosphate,
wherein the ruxolitinib phosphate is present in the dosage form in an amount ranging from 10 mg to 60 mg on a free base basis,
wherein the dosage form is suitable for oral administration,
wherein the administration of the dosage form results in a ratio of mean peak to plasma concentration (Cmax) to mean 12-hour plasma concentration (C12h) of ruxolitinib of 10 or less, and
wherein the administration of the dosage form to a human results in a mean half-life (t1/2) of from 3.5 hours to 11 hours.

### Claim 2 (depends on 1)

The oral sustained release dosage form of claim 1, wherein the ruxolitinib phosphate is present in the dosage form in an amount of 10 mg on a free base basis.

### Claim 3 (depends on 1)

The oral sustained release dosage form of claim 1, wherein the ruxolitinib phosphate is present in the dosage form in an amount of 12.5 mg on a free base basis.

### Claim 4 (depends on 1)

The oral sustained release dosage form of claim 1, wherein the ruxolitinib phosphate is present in the dosage form in an amount of 20 mg on a free base basis.

### Claim 5 (depends on 1)

The oral sustained release dosage form of claim 1, wherein the ruxolitinib phosphate is present in the dosage form in an amount of 25 mg on a free base basis.

### Claim 6 (depends on 1)

The oral sustained release dosage form of claim 1, wherein the ruxolitinib phosphate is present in the dosage form in an amount of 30 mg on a free base basis.

### Claim 7 (depends on 1)

The oral sustained release dosage form of claim 1, wherein the ruxolitinib phosphate is present in the dosage form in an amount of 37.5 mg on a free base basis.

### Claim 8 (depends on 1)

The oral sustained release dosage form of claim 1, wherein the ruxolitinib phosphate is present in the dosage form in an amount of 40 mg on a free base basis.

### Claim 9 (depends on 1)

The oral sustained release dosage form of claim 1, wherein the ruxolitinib phosphate is present in the dosage form in an amount of 50 mg on a free base basis.

### Claim 10 (depends on 1)

The oral sustained release dosage form of claim 1, wherein the ruxolitinib phosphate is present in the dosage form in an amount of 60 mg on a free base basis.

### Claim 11 (depends on 1)

The oral sustained-release dosage form of claim 1, wherein administration of the dosage form to a human results in a ratio of mean peak plasma concentration (Cmax) to mean 12-hour plasma concentration (C12h) of ruxolitinib of 1 to 10.

### Claim 12 (depends on 1)

The oral sustained-release dosage form of claim 1, wherein administration of the dosage form to a human results in a ratio of mean peak plasma concentration (Cmax) to mean 12-hour plasma concentration (C12h) of ruxolitinib of 2 to 7.

### Claim 13 (depends on 1)

The oral sustained-release dosage form of claim 1, wherein administration of the dosage form to a human results in a mean half-life (t1/2) of from 4 hours to 8 hours.

### Claim 14 (depends on 1)

The oral sustained-release dosage form of claim 1, wherein the sustained-release dosage form has a mean relative bioavailability based on AUC of from 65% to 110% relative to an immediate release formulation comprising the same amount of ruxolitinib phosphate in humans.

### Claim 15 (depends on 1)

The oral sustained-release dosage form of claim 1, wherein the dosage form is a tablet.

### Claim 16 (depends on 1)

The oral sustained-release dosage form of claim 1, wherein the dosage form is a capsule.

### Claim 17 (depends on 1)

The oral sustained-release dosage form of claim 1, wherein administration of the dosage form to a human results in a mean time to peak plasma concentration (tmax) of ruxolitinib of 1.5 hours to 5 hours.

### Claim 18 (depends on 1)

A method of treating a disease selected from myelofibrosis, polycythemia vera, and graft versus host disease in a human patient in need thereof, comprising administering to the patient the oral sustained-release dosage form of claim 1 once per day.

### Claim 19 (depends on 18)

The method of claim 18, wherein the disease is myelofibrosis.

### Claim 20 (depends on 19)

The method of claim 19, wherein the myelofibrosis is primary myelofibrosis (PMF), postpolycythemia vera myelofibrosis (PV-MF), or post-essential thrombocythemia myelofibrosis (post ET-MF).

### Claim 21 (depends on 18)

The method of claim 18, wherein the disease is polycythemia vera.

### Claim 22 (depends on 18)

The method of claim 18, wherein the disease is graft versus host disease.

### Claim 23 (depends on 18)

The method of claim 18, wherein administration of the dosage form to a human patient results in a reduction in thrombocytopenia or anemia relative to an immediate-release dosing regimen.