# US 12,109,218 B2 · Compositions of grapiprant and methods for using the same

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- Number: US 12,109,218 B2
- Document ID: US12109218B2
- Status: Granted
- Kind: B2
- Application number: 17/548,755
- Filed: 2021-12-13
- Published: 2022-03-31
- Granted: 2024-10-08
- Earliest claimed: 2014-12-09
- Assignees: Aratana Therapeutics, Inc.
- Applicants: Aratana Therapeutics, Inc.
- Inventors: Lesley Rausch-Derra; Tamara Newbold; Gopinath Devaraj; Akemi Shiraishi
- Web page: https://patentgrep.com/patent/US12109218B2

## CPC

- A61K 31/64: Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/0056: {Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals}
- A61K 9/2009: {Inorganic compounds}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin}
- A61K 31/437: the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- 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 disclosure provides a method for treating pain or inflammation in a non-human animal in need thereof. The method comprises administering to a non-human animal a pharmaceutical composition comprising a therapeutically effective amount of grapiprant. Also provided herein are pharmaceutical compositions for treating pain or inflammation in a non-human animal in need thereof. The pharmaceutical compositions comprise a therapeutically effective amount of grapiprant and an excipient, including flavorants.

## Claims

### Claim 1

A method for treating pain and inflammation in a cat or a dog, the method comprising administering to the cat or the dog an oral pharmaceutical composition comprising a therapeutically effective amount of grapiprant and one or more excipients;
wherein the therapeutically effective amount of grapiprant is administered at a dosage rate of 2 mg per kilogram bodyweight of the cat or the dog once per day; and
wherein the oral pharmaceutical composition is administered with or without food.

### Claim 2 (depends on 1)

The method of claim 1, wherein the administering achieves a Cmax of grapiprant of 375 ng/ml to 10000 ng/mL at a Tax of 0.4 to 3.4 hours.

### Claim 3 (depends on 2)

The method of claim 2, wherein the administering achieves a Cmax of grapiprant of 750 ng/mL to 4000 ng/mL.

### Claim 4 (depends on 3)

The method of claim 3 wherein the administering achieves a Cmax of grapiprant of 1300 ng/mL to 4000 ng/mL.

### Claim 5 (depends on 2)

The method of claim 2, wherein the administering achieves the Cmax of grapiprant at a Tmax of 0.7 to 1.7 hours.

### Claim 6 (depends on 3)

The method of claim 3, wherein the administering achieves the Cmax of grapiprant at a Tmax of 0.5 to 1.0 hours.

### Claim 7 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition further comprises 1% to 30% flavorant (w/w of the total composition).

### Claim 8 (depends on 7)

The method of claim 7, wherein the pharmaceutical composition comprises 5% to 15% flavorant (w/w of the total composition).

### Claim 9 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition is administered for 6 days to 9 months.

### Claim 10 (depends on 9)

The method of claim 9, wherein the pharmaceutical composition is administered for 9 to 21 days.

### Claim 11 (depends on 10)

The method of claim 10, wherein the pharmaceutical composition is administered for 12 to 14 days.

### Claim 12 (depends on 1)

The method of claim 1, wherein the administering occurs from about 10 hours to about 18 hours before a surgery is performed on the cat or the dog.

### Claim 13 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition comprises sodium lauryl sulfate.

### Claim 14 (depends on 1)

The method of claim 1, wherein the composition after administering causes no clinically significant adverse gastrointestinal event or changes in liver, kidney, and coagulation parameters in the cat or the dog.