Drug intelligence / Profile preview

imexon

Development stage
Phase 2
Lead developer
Eddingpharm
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Imexon is a small molecule antineoplastic agent classified as a 2-cyanoaziridine derivative. It exerts its anticancer effects primarily by increasing oxidative stress within cancer cells. Imexon binds to glutathione and other cellular thiols, depleting these antioxidants and leading to the accumulation of reactive oxygen species (ROS). This oxidative stress disrupts mitochondrial membrane potential, resulting in the release of cytochrome c and activation of caspase-mediated apoptosis. Additionally, imexon inhibits ribonucleotide reductase—a key enzyme in DNA synthesis—and acts as a cell cycle inhibitor, causing S-phase arrest. Imexon's unique mechanism has been investigated for multiple cancers including pancreatic cancer, lung cancer, breast cancer, prostate cancer, melanoma, multiple myeloma, ovarian cancer, solid tumors, and B-cell non-Hodgkin lymphoma[1][3][5][10].

Brand names
Amplimexon
Other names
2-cyanoaziridine derivativecyanoaziridine compound
02

Targets

RNR (Ribonucleotide reductase)

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