# US 10,500,285 B2 · Docetaxel and human serum albumin complexes

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- Number: US 10,500,285 B2
- Document ID: US10500285B2
- Status: Granted
- Kind: B2
- Application number: 15/574,057
- Filed: 2016-05-16
- Published: 2018-10-11
- Granted: 2019-12-10
- Earliest claimed: 2015-05-15
- Assignees: Zhuhai Beihai Biotech Co., Ltd.
- Applicants: Zhuhai Beihai Biotech Co., Ltd.
- Inventors: Qun Sun
- Web page: https://patentgrep.com/patent/US10500285B2

## CPC

- A61K 47/42: Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein (oligopeptides having up to five amino acids {A61K47/183}; polyamino acids A61K47/34)
- 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 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 9/19: lyophilised {, i.e. freeze-dried, solutions or dispersions (lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00)}
- A61K 9/5169: {Proteins, e.g. albumin, gelatin}
- A61K 31/337: having four-membered rings, e.g. taxol
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 13/08: of the prostate
- 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 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

This document relates to non-covalently bound complexes including Docetaxel and human serum albumin. This document also relates to compositions comprising non-covalently bound complexes including Docetaxel and human serum albumin. This document also relates to compositions comprising Docetaxel and human serum albumin, wherein the composition is a clear aqueous solution when the composition is dissolved in an aqueous solution, and wherein the composition has a solubility in an aqueous solution of at least 10 mg/ml. This document also relates to compositions comprising Docetaxel and human serum albumin, wherein the Docetaxel and the human serum albumin in the composition have a ratio by weight from about 1:50 to about 1:1000. This document also relates to compositions consisting essentially of Docetaxel and human serum albumin, wherein the Docetaxel and the human serum albumin in the composition have a ratio by weight from about 1:50 to about 1:1000.

## Claims

### Claim 1

A composition comprising Docetaxel and human serum albumin, wherein the Docetaxel and the human serum albumin in the composition have a ratio by weight from about 1:60 to about 1:300, wherein the composition is a clear aqueous solution when the composition is dissolved in an aqueous solvent and after the clear aqueous solution is filtered by a 0.22 micron filter, the amount of Docetaxel in the filtered aqueous solution is at least 96% of the total amount of Docetaxel in the aqueous solution before the filtration; and
wherein the aqueous solution is substantially free of solvent other than water.

### Claim 2 (depends on 1)

The composition of claim 1, wherein the Docetaxel and the human serum albumin in the composition have a ratio by weight from about 1:80 to about 1:200.

### Claim 3 (depends on 1)

The composition of claim 1, wherein the Docetaxel and the human serum albumin in the composition have a ratio by weight from about 1:90 to about 1:120.

### Claim 4 (depends on 1)

The composition of claim 1, wherein the Docetaxel and the human serum albumin in the composition are in a ratio by weight of about 1:90, about 1:100, about 1:110, or about 1:120.

### Claim 5 (depends on 1)

The composition of claim 1, wherein the composition is a clear aqueous solution when the composition is dissolved in an aqueous solution, and wherein the aqueous solution is substantially free of solvent other than water.

### Claim 6 (depends on 1)

The composition of claim 1, wherein the composition is a clear aqueous solution when the composition is dissolved in an aqueous solution, and wherein after the clear aqueous solution is filtered by a 0.22 micron filter, the amount of Docetaxel in the filtered aqueous solution is at least 98% of the total amount of Docetaxel in the aqueous solution before the filtration.

### Claim 7 (depends on 1)

The composition of claim 1, wherein the composition is a clear aqueous solution for at least 3 hours when the composition is dissolved in an aqueous solution.

### Claim 8 (depends on 1)

The composition of claim 1, wherein the composition is a solid formulation.

### Claim 9 (depends on 1)

The composition of claim 1, wherein the composition is an aqueous formulation.

### Claim 10 (depends on 9)

The composition of claim 9, wherein the aqueous formulation is a clear aqueous solution for at least 3 hours, and wherein the aqueous formulation is substantially free of solvent other than water.

### Claim 11 (depends on 9)

The composition of claim 9, wherein the aqueous formulation is a clear aqueous solution for at least 6 hours at a temperature from about 1° C. to about 10° C., and wherein the aqueous formulation is substantially free of solvent other than water.

### Claim 12

A composition comprising Docetaxel and human serum albumin, wherein the molar ratio of Docetaxel and the human serum albumin in the composition is from about 0.2:1 to about 2:1, wherein the composition forms a clear aqueous solution when the composition is dissolved in an aqueous solvent and after the clear aqueous solution is filtered by a 0.22 micron filter, the amount of Docetaxel in the filtered aqueous solution is at least 96% of the total amount of Docetaxel in the aqueous solution before the filtration; wherein the aqueous solution is substantially free of solvent other than water, and wherein the solubility of the composition in the aqueous solution is at least 10 mg/ml.

### Claim 13 (depends on 12)

The composition of claim 12, wherein the molar ratio of the Docetaxel and the human serum albumin is from about 0.5:1 to about 2:1.

### Claim 14 (depends on 12)

The composition of claim 12, wherein the molar ratio of the Docetaxel and the human serum albumin is from about 0.75:1 to about 1.5:1.

### Claim 15 (depends on 12)

The composition of claim 12, wherein the composition has a solubility in an aqueous solution of about 20 mg/ml, about 30 mg/ml, about 40 mg/ml, about 50 mg/ml, 60 mg/ml, about 70 mg/ml, about 80 mg/ml, about 90 mg/ml, or about 100 mg/ml.

### Claim 16 (depends on 12)

The composition of claim 12, wherein the composition is an aqueous formulation, wherein the aqueous formulation is substantially free of solvent other than water, and wherein the aqueous formulation is a clear aqueous solution for at least 3 hours at a temperature from about 10° C. to about 20° C.

### Claim 17 (depends on 12)

The composition of claim 12, wherein the composition is an aqueous formulation, wherein the aqueous formulation is substantially free of solvent other than water, and wherein the aqueous formulation is a clear aqueous solution for at least 6 hours at a temperature from about 1° C. to about 10° C.

### Claim 18 (depends on 1)

A pharmaceutical composition comprising the composition claim 1, and a pharmaceutically acceptable carrier.

### Claim 19 (depends on 18)

A method of treating a cancer, the method comprising the step of administering to a subject in need thereof a therapeutically effective amount of the pharmaceutical composition of claim 18, and wherein the cancer is selected from the group consisting of breast cancer, non-small cell lung cancer, prostate cancer, gastric cancer, head and neck cancer, ovarian cancer, pancreatic cancer, and Kaposi's sarcoma.