# US 10,441,582 B2 · Injectable anticancer composition for local administration containing suspension of quinine salt

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- Number: US 10,441,582 B2
- Document ID: US10441582B2
- Status: Granted
- Kind: B2
- Application number: 15/498,212
- Filed: 2017-04-26
- Published: 2017-12-21
- Granted: 2019-10-15
- Earliest claimed: 2016-06-20
- Applicants: Oh Young Yeo
- Inventors: Oh Young Yeo
- Web page: https://patentgrep.com/patent/US10441582B2

## CPC

- A61K 31/4709: Non-condensed quinolines and containing further heterocyclic rings
- 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 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- A61K 31/49: Cinchonan derivatives, e.g. quinine
- A61K 31/525: Isoalloxazines, e.g. riboflavins, vitamin B2
- A61K 47/02: Inorganic compounds
- A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
- A61K 49/0438: {Organic X-ray contrast-enhancing agent comprising an iodinated group or an iodine atom, e.g. iopamidol}
- A61P 35/00: Antineoplastic agents
- 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

Disclosed herein is an injectable anticancer composition for local administration, which contains a suspension of quinine hydrochloride. The anticancer composition for local administration according to the present invention shows an IC50 value against MKN-45 cells, which is about 10 times lower than Paclitaxel, as determined by an MTT assay in vitro, suggesting that the anticancer composition has an excellent cytotoxic effect. The anticancer composition can be administered as a safe anticancer agent in clinical applications, and also shows an anticancer effect by inducing the necrosis and detachment of solid cancer cells. Particularly, the anticancer composition has an anticancer mechanism by which the composition acts locally in a tumor tissue administered with the composition and shows a rapid antitumor effect (1-2 weeks after administration).

## Claims

### Claim 1

An injectable composition for local administration for cancer treatment, comprising, based on 100% (w/w) of the composition: 30-60 (w/w) of a quinine chloride; 1-2% (w/w) of lidocaine as a local anesthetic; 0.1-0.55% (w/w) of riboflavin as an antioxidant; 0.01-0.2% (w/w) of Ioversol as a contrast agent; and the remainder saline; wherein the injectable composition is to be injected into cancer cells in a solution state by heating to a temperature of 40° C. or higher, the temperature being predetermined according to the w/w percent of the quinine chloride, and wherein the quinine chloride has a structure according to formula 1:

### Claim 2 (depends on 1)

The injectable suspension composition of claim 1, wherein the content of the quinine hydrochloride in the composition is 30-50% (w/w).

### Claim 3

A method of treating cancer in a patient in need thereof comprising: changing a suspension composition comprising quinine hydrochloride and saline into an injectable solution by heating the suspension to a temperature of 40° C. or higher so as to enable the quinine hydrochloride to be administered at high concentrations and act locally, the temperature being predetermined according to the w/w percent of the quinine chloride, and injecting the heated solution directly into cancer cells wherein the solution is solidified within the cancer cells as the solution cools down below a crystallization temperature of the solution by a body temperature of a cancer patient, thereby minimizing migration of the quinine hydrochloride to normal cells.