Drug intelligence / Profile preview

recombinant human endostatin + cisplatin

Development stage
Unknown
Lead developer
Simcere Pharmaceutical Group
Modality
Small Molecules, Recombinant Proteins and Enzymes
Administration
Intra-arterial, Intraperitoneal, Intratumoral, Intravenous
01

Overview

Recombinant human endostatin + cisplatin is a combination regimen consisting of recombinant human endostatin (rh-endostatin, marketed in China as Endostar) and the platinum-based chemotherapy drug cisplatin. Recombinant human endostatin is a purified, modified form of the endogenous angiogenesis inhibitor endostatin, featuring an additional nine-amino-acid sequence at the N-terminus that improves its solubility and stability. It acts as an anti-angiogenic agent by binding to vascular endothelial growth factor receptor 2 (VEGFR-2), integrin alpha-5 beta-1, and nucleolin, thereby inhibiting endothelial cell proliferation, migration, and tube formation. Cisplatin is a small-molecule cytotoxic agent that binds to DNA, forming intra-strand and inter-strand crosslinks that inhibit DNA replication and transcription, leading to cell cycle arrest and apoptosis. In combination, recombinant human endostatin normalizes tumor vasculature, which enhances the intratumoral delivery and therapeutic efficacy of cisplatin. This combination regimen is primarily investigated and utilized in China for the treatment of non-small cell lung cancer (NSCLC), malignant pleural effusion, malignant ascites, and other solid tumors.

Other names
Endostar + cisplatinEndostar plus cisplatinYH-16 + cisplatincisplatin + Endostarcisplatin + recombinant human endostatincisplatin + rh-endostatincisplatin plus Endostarcisplatin plus recombinant human endostatincisplatin plus rh-endostatinrecombinant human endostatin plus cisplatinrh-endostatin + cisplatinrh-endostatin plus cisplatin
02

Targets

DNAITGA5:ITGB1 (Integrin α5β1)NCL (Nucleolin)VEGFR2 (Vascular endothelial growth factor receptor 2)

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