# US 10,369,129 B2 · Long acting pharmaceutical composition of protease inhibitor

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- Number: US 10,369,129 B2
- Document ID: US10369129B2
- Status: Granted
- Kind: B2
- Application number: 15/168,864
- Filed: 2016-05-31
- Published: 2017-11-30
- Granted: 2019-08-06
- Earliest claimed: 2016-05-31
- Assignees: TaiMed Biologics, Inc.
- Applicants: TaiMed Biologics, Inc.
- Inventors: James Nienyuan Chang; Hsiang-Fa Liang; Meng-Hsin Chen; Kuei-Ling Kuo; An-Chieh Li
- Web page: https://patentgrep.com/patent/US10369129B2

## CPC

- A61K 31/325: Carbamic acids; Thiocarbamic acids; Anhydrides or salts thereof (thiurams A61K31/145)
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/10: Dispersions; Emulsions
- A61K 9/146: {with organic macromolecular compounds}
- 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)

## Abstract

Disclosed herein is a long acting pharmaceutical composition for treating or preventing human immunodeficiency virus (HIV) infection. The pharmaceutical composition comprises a suspension of a lysine-based aspartyl protease inhibitor or salt thereof, a surface modifier, and a pharmaceutically acceptable carrier; wherein the lysine-based aspartyl protease inhibitor or salt thereof has an average effective particle size of less than about 500 nm. A method for treating or preventing HIV infection with the pharmaceutical composition is also disclosed.

## Claims

### Claim 1

A long acting pharmaceutical composition for treating human immunodeficiency virus (HIV) infection, which consists of a suspension of a lysine-based aspartyl protease inhibitor or salt thereof, a surface modifier, wherein the surface modifier is selected from the group consisting of poloxamer 188, poloxamer 407, d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS or Vitamin E TPGS), Polysorbate 80 (Tween 80), and distearoyl phosphatidyl-ethanolamine-poly(ethylene glycol) (DSPE-PEG), and a pharmaceutically acceptable carrier; wherein the lysine-based aspartyl protease inhibitor is TMB-607 having the structure of formula IIb:
and
wherein the average effective particle size of the lysine-based aspartyl protease inhibitor or salt thereof is 300 nm or less.

### Claim 2 (depends on 1)

The pharmaceutical composition of claim 1, wherein the composition is formulated for intramuscular or subcutaneous injection.

### Claim 3

A method of treating HIV infection for a long term comprising administering to a subject in need thereof by intramuscular or subcutaneous injection once a week to once a month a therapeutically effective amount of a pharmaceutical composition consisting of a suspension of a lysine-based aspartyl protease inhibitor or salt thereof, a surface modifier, and a pharmaceutically acceptable carrier; wherein the lysine-based aspartyl protease inhibitor or salt thereof has an average effective particle size of less than 300 nm, and wherein the lysine-based aspartyl protease inhibitor is TMB-607 having the structure of formula IIb:

### Claim 4 (depends on 3)

The method of claim 3, wherein a dose of the pharmaceutical composition of about 5 to about 65 mg/kg of the subject's body weight is administered.

### Claim 5 (depends on 3)

The method of claim 3, wherein the administering is by intramuscular injection.

### Claim 6 (depends on 3)

The method of claim 3, wherein the administering is by subcutaneous injection.

### Claim 7 (depends on 1)

The method of claim 1, wherein the average effective particle size of the lysine-based aspartyl protease inhibitor or salt thereof is 240 nm or less.

### Claim 8 (depends on 3)

The method of claim 3, wherein the lysine-based aspartyl protease inhibitor or salt thereof has an average effective particle size of less than 240 nm.