Drug intelligence / Profile preview

ferumoxytol-cleavable valine-citrulline-monomethyl auristatin E

Development stage
Preclinical
Lead developer
Stanford University
Modality
Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

Ferumoxytol-cleavable valine-citrulline-monomethyl auristatin E (also referred to as FCM or TNP) is an investigational theranostic nanoparticle conjugate developed by researchers at Stanford University for the treatment and magnetic resonance imaging (MRI) of glioblastoma. The agent consists of a superparamagnetic iron oxide nanoparticle core (ferumoxytol) conjugated via a cathepsin B-cleavable valine-citrulline dipeptide linker to the potent antimitotic toxin monomethyl auristatin E (MMAE). The ferumoxytol core acts as an MRI contrast agent, allowing non-invasive in vivo tracking of nanoparticle accumulation in the tumor. Upon internalization into glioblastoma cells, the linker is selectively cleaved by lysosomal cathepsin B, which is highly expressed in glioblastoma, releasing active MMAE to inhibit tubulin polymerization and induce tumor cell death while minimizing off-target systemic toxicity.

Other names
ferumoxytol-cleavable MMAEferumoxytol-valine-citrulline-monomethyl auristatin Etheranostic nanoparticlesTNP

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