Drug intelligence / Profile preview

RGD-temozolomide

Development stage
Preclinical
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Intravenous
01

Overview

RGD-temozolomide is a **nanostructured lipid carrier (NLC) delivery system for temozolomide** that is surface-modified with RGD (arginine-glycine-aspartic acid) peptide, designed to enhance targeted drug delivery to tumor cells expressing integrin receptors such as those found in glioblastoma multiforme (GBM)[4][15]. Temozolomide, the active pharmaceutical agent, is an alkylating agent that methylates DNA at the O6 and N7 positions of guanine, leading to DNA damage and apoptosis in rapidly dividing cancer cells[1][5]. The **RGD modification** improves selective uptake by tumor cells through binding to integrin αvβ3 receptors, facilitating enhanced delivery of temozolomide into glioma cells[4][15]. This approach aims to improve the cytotoxic efficacy and tumor selectivity of temozolomide while reducing off-target effects. Preclinical studies have demonstrated improved inhibition of glioma cell lines and antitumor activity in mouse models compared to regular temozolomide[4][15]. The system is primarily under investigation for malignant gliomas such as glioblastoma multiforme and gliomatosis cerebri.

Other names
RGD-TMZRGD-TMZ/NLCs
02

Targets

αVβ3 (Integrin αVβ3)DNA

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