# US 2021/0276948 A1 · Composition and application thereof as antitumor drug

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- Number: US 2021/0276948 A1
- Document ID: US20210276948A1
- Status: Published application
- Kind: A1
- Application number: 17/209,337
- Filed: 2021-03-23
- Published: 2021-09-09
- Earliest claimed: 2018-10-11
- Assignees: Guangdong Zhongerjian Biotechnology Co., Ltd.
- Applicants: Guangdong Zhongerjian Biotechnology Co., Ltd.
- Inventors: Xiaojiang Tang; Xuefeng Ren; Yichen Ge; Zhiyong Zhong
- Web page: https://patentgrep.com/patent/US20210276948A1

## CPC

- C07C 333/04: having nitrogen atoms of thiocarbamic groups bound to hydrogen atoms or to acyclic carbon atoms
- A61K 33/243: Platinum; Compounds thereof
- A61P 35/00: Antineoplastic agents
- C07C 333/20: having nitrogen atoms of dithiocarbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C: ACYCLIC OR CARBOCYCLIC 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

This disclosure relates to a composition and application thereof in antitumor drugs. The composition is prepared from a platinum-based antitumor compound and a novel compound, wherein the novel compound is sodium(S)-2-(dithiocarboxylate ((2S, 3R, 4R, 5R)-2,3,4,5,6-pentahydroxyhexyl)amino)-4-(methylthio)butyrate. The novel compound in the composition could effectively chelate the platinum-based antitumor compound and reduce the various adverse effects exhibited by the platinum-based compound. The dosage of the platinum-based antitumor compound can thus be increased, and the antitumor effect can be optimized. The novel compound itself is low-toxic and it has low chelating activities with essential metals in the human body; it would not impose significant adverse effects on the human body at given doses. The composition and its application as an antitumor drug provided by the present disclosure overcome some technical drawbacks of platinum-based antitumor drugs of the prior art, namely severe adverse effects and the development of drug resistance during administration.

## Claims

### Claim 1

A method of treating solid tumors in a subject suffering from cancer, including:
administrating a drug to the subject, wherein the drug comprises a platinum-based antitumor compound and a novel compound, the novel compound can enter a tumor cell through a glucose transporter GLUP, the glucose transporter GLUP facilitates entry of the platinum-based antitumor compound into the tumor cell; the novel compound can also enter a kidney cell through a sodium-glucose cotransporter SGLT2, the sodium-glucose cotransporter SGLT2 facilitates excretion of the platinum-based antitumor compound accumulated in a kidney.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the novel compound is sodium (S)-2-(dithiocarboxylate ((2S,3R,4R),5R)-2,3,4,5,6-pentahydroxyhexyl)amino)-4-(methylthio)butyrate.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the platinum-based antitumor compound is one or more selected from the group consisting of cisplatin, oxaliplatin, and carboplatin.

### Claim 4 (depends on 3)

The method according to claim 3, wherein the platinum-based antitumor compound is cisplatin.

### Claim 5 (depends on 1)

The method according to claim 1, wherein the drug comprises, in parts by mole, 1-5 parts of the platinum-based antitumor compound and 1-50 parts of the novel compound.

### Claim 6 (depends on 5)

The method according to claim 5, wherein the drug comprises, in parts by mole, 1-3 parts of the platinum-based antitumor compound and 1-20 parts of the novel compound.

### Claim 7 (depends on 6)

The method according to claim 6, wherein the composition comprises, in parts by mole, 1 part of the platinum-based antitumor compound and 20 parts of the novel compound.

### Claim 8 (depends on 1)

The method according to claim 1, wherein the novel compound is administered 2 hours after administration of cisplatin.

### Claim 9 (depends on 1)

The method according to claim 1, wherein the cancer is breast cancer.