Drug intelligence / Profile preview

tyroserleutide

Development stage
Phase 3
Lead developer
Shenzhen Kangzhe Pharmaceutical
Modality
Small Molecules, Peptides
Administration
Intravenous
01

Overview

Tyroserleutide is a tripeptide consisting of the amino acids tyrosine, serine, and leucine. It has potential antineoplastic activity and was developed for the treatment of liver cancer. The mechanism of its antitumor activity is not fully elucidated but appears to involve inhibition of ICAM-1 (CD54), a cell adhesion factor important in tumor invasion and metastasis. Tyroserleutide may also influence the Ca²⁺/calmodulin pathway and inhibit phosphatidylinositol 3 kinase (PI3K), which is upregulated in tumor cells and involved in cellular proliferation[2][4]. The drug was initially separated from pig spleen hydrolyzates but can now be synthesized chemically. It has shown antitumor effects on human hepatocarcinoma BEL-7402 both in vitro and in vivo[4]. Tyroserleutide is characterized by low molecular weight, simple structure, nonimmunogenicity, specificity for tumor cells, few side effects, and ease of synthesis[4].

Other names
L-leucineL-tyrosyl-L-seryl-L-tyrosine-L-serine-L-leucineTyr-Ser-LeuN-(N-L-Tyrosyl-L-seryl)-L-leucine
02

Targets

CaM (Calmodulin)ICAM1 (Intercellular Adhesion Molecule 1)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)

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