TYROSERLEUTIDE

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C18H27N3O6
Molecular Weight	381.4235
Optical Activity	UNSPECIFIED
Defined Stereocenters	3 / 3
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC1=CC=C(O)C=C1)C(O)=O

InChI

InChIKey=MQGGXGKQSVEQHR-KKUMJFAQSA-N

InChI=1S/C18H27N3O6/c1-10(2)7-14(18(26)27)20-17(25)15(9-22)21-16(24)13(19)8-11-3-5-12(23)6-4-11/h3-6,10,13-15,22-23H,7-9,19H2,1-2H3,(H,20,25)(H,21,24)(H,26,27)/t13-,14-,15-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C18H27N3O6
Molecular Weight	381.4235
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	3 / 3
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://adisinsight.springer.com/drugs/800027782 | https://www.ncbi.nlm.nih.gov/pubmed/17515953 | https://www.ncbi.nlm.nih.gov/pubmed/16091933 | http://en.cms.net.cn/CmsNewWebEn/product/content.html

Tyroserleutide (YSL) is a tripeptide treatment being developed by Shenzhen Kangzhe Pharmaceutical Co Ltd, a subsidary of China Medical System Holdings (CMS), for the treatment of liver cancer. It is initially separated and purified from the hydrolyzates of pig’s spleen, but now can be obtained by chemical synthesis, its chemical name is L-tyrosine-L-serine-L-leucine. Tyroserleutide is an active, low-molecular-weight polypeptide, comprised of three amino acids, that has shown antitumor effects on human hepatocarcinoma BEL-7402 in vitro and in vivo. Tyroserleutide has various advantages over the other bioactive peptides such as its low molecular weight, simple construction, nonimmunogenicity, specificity, few side effects, and ease of synthesis. Tyroserleutide is in Phase-III clinical trials for the treatment of liver cancer.

Originator

Approval Year

PubMed

Title	Date	PubMed
Therapeutic effects of tyroserleutide on lung metastasis of human hepatocellular carcinoma SK-HEP-1 and its mechanism affecting ICAM-1 and MMP-2 and -9.	2018	30349190
Effects of Tyroserleutide on phosphatidylinositol 3'-kinase/AKT pathway in human hepatocellular carcinoma cell.	2014-02	24147456
Effects of a novel tripeptide, tyroserleutide (YSL), on cell cycle progression of human hepatocellular carcinoma.	2009-08	19491661
The effect of tripeptide tyroserleutide (YSL) on animal models of hepatocarcinoma.	2006-06	16129512

Sample Use Guides

In Vivo Use Guide

Hepatocellular carcinoma: continuous administration of Tyroserleutide (YSL) by a portable infusion pump; forty patients (12 in stage 1, 28 in stage 2, total 10 treated in each dose cohort) were treated with Tyroserleutide 6, 12, 18, or 24 mg/day lasting for 5 days.

Route of Administration: Intravenous

In Vitro Use Guide

When B16-F10 cells were treated with Tyroserleutide (0.01, 0.1, 1, 10, or 100 ug/mL) in vitro, it inhibited the proliferation of B16-F10 cells with a 28.11% rate of inhibition.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 21:37:47 GMT 2025` Edited by `admin` on `Mon Mar 31 21:37:47 GMT 2025`
Record UNII	L9TIM50J8N
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TYROSERLEUTIDE

Common Name

English

CMS-024

Preferred Name

English

Tyroserleutide [WHO-DD]

Common Name

English

L-LEUCINE, L-TYROSYL-L-SERYL-

Systematic Name

English

L-TYROSINE-L-SERINE-L-LEUCINE

Systematic Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

190604