# US 11,298,355 B2 · Inhalable imatinib formulations, manufacture, and uses thereof

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- Number: US 11,298,355 B2
- Document ID: US11298355B2
- Status: Granted
- Kind: B2
- Application number: 16/874,118
- Filed: 2020-05-14
- Published: 2020-11-19
- Granted: 2022-04-12
- Earliest claimed: 2019-05-16
- Assignees: Aerovate Therapeutics, Inc.
- Applicants: Aerovate Therapeutics, Inc.
- Inventors: Ben Dake; Ralph Niven; Andrew D. Levin
- Web page: https://patentgrep.com/patent/US11298355B2

## CPC

- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 9/0073: {Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy; (nasal sprays A61K9/0043; inhalation of vapours of volatile or heated drugs, e.g. essential oils or nicotine, A61K9/007; devices A61M)}
- A61K 9/0075: {for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles}
- A61K 9/0078: {for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions}
- A61K 31/501: not condensed and containing further heterocyclic rings
- A61K 38/1858: {Platelet-derived growth factor [PDGF]}
- A61K 38/193: {Colony stimulating factors [CSF]}
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61P 9/12: Antihypertensives
- A61P 11/00: Drugs for disorders of the respiratory system
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- 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
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

The invention relates to inhalable imatinib formulations, manufacture, and uses thereof.

## Claims

### Claim 1

An inhalable formulation comprising micronized particles of imatinib freebase having a type A crystal structure, the micronized particles having a mass median aerodynamic diameter in the range of about 0.5 μm to about 5 μm and the inhalable formulation comprising less than 5% amorphous imatinib particles and less than 5% water, wherein imatinib freebase is the only active pharmaceutical ingredient in the inhalable formulation.

### Claim 2 (depends on 1)

The inhalable formulation of claim 1, wherein the inhalable formulation further comprises one or more carrier agents.

### Claim 3 (depends on 2)

The inhalable formulation of claim 2, wherein one or more carrier agents is lactose.

### Claim 4 (depends on 1)

The inhalable formulation of claim 1, wherein the imatinib is present in a therapeutically effective amount to treat a condition of the pulmonary cardiovascular system.

### Claim 5 (depends on 4)

The inhalable formulation of claim 4, wherein the condition of the pulmonary cardiovascular system is pulmonary arterial hypertension (PAH).

### Claim 6 (depends on 1)

The inhalable formulation of claim 1, wherein inhalable formulation comprises less than 3% amorphous imatinib particles.

### Claim 7 (depends on 1)

The inhalable formulation of claim 1, wherein inhalable formulation comprises less than 1% amorphous imatinib particles.

### Claim 8 (depends on 1)

The inhalable formulation of claim 1, wherein the inhalable formulation comprises less than 1% water.

### Claim 9

A method of treating pulmonary arterial hypertension (PAH), the method comprising providing to a subject an inhalable formulation comprising micronized particles of imatinib freebase having a type A crystal structure, the micronized particles having a mass median aerodynamic diameter in the range of about 0.5 μm to about 5 μm and the inhalable formulation comprising less than 5% amorphous imatinib particles and less than 5% water, wherein imatinib freebase is the only active pharmaceutical ingredient in the inhalable formulation.

### Claim 10 (depends on 9)

The method of claim 9, wherein the inhalable formulation further comprises one or more carrier agents.

### Claim 11 (depends on 10)

The method of claim 10, wherein the one or more carrier agents is lactose.

### Claim 12 (depends on 9)

The method of claim 9, wherein the subject is a human.

### Claim 13 (depends on 9)

The method of claim 9, wherein inhalable formulation comprises less than 3% amorphous imatinib particles.

### Claim 14 (depends on 9)

The method of claim 9, wherein inhalable formulation comprises less than 1% amorphous imatinib particles.

### Claim 15 (depends on 9)

The method of claim 9, wherein the inhalable formulation comprises less than 1% water.