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Amplimexon Uses, Dosage, Side Effects and more

Amplimexon is currently being studied for the treatment of pancreatic, lung, breast, prostate, melanoma, and multiple myeloma cancers. It belongs to the family of drugs called cyanoaziridine derivatives. Also called Amplimexon. Amplimexon is a cyanoaziridine derivative.Amplimexon is a thiol-binding small molecule which induces mitochondrial oxidation, a loss of membrane potential and cytochrome C, leading to apoptosis.

Attribute Details
Trade Name Amplimexon
Generic Imexon
Imexon Other Names Imexon
Type
Formula C4H5N3O
Weight Average: 111.102
Monoisotopic: 111.043261797
Groups Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: January 7, 2025 at 1:49 am
   

Uses

Investigated for use/treatment in melanoma, multiple myeloma, ovarian cancer, pancreatic cancer, and solid tumors.

How Amplimexon works

Amplimexon enters the cell and binds to glutathione and other sulfhydryl compounds, effectively preventing them from scavenging the toxic free radicals. So, particularly in the rapidly dividing cancer cell, free radical build-up in the presence of imexon leads to changes in mitochondrial membrane potential and ultimately to the mitochondria swelling and bursting. Mitochondrial proteins, in particular cytochrome c, are released into the cytoplasm and this activates caspase-mediated apoptosis resulting in cancer cell death. This sequence of events has been well characterized and published in several papers in leading cancer journals. Amplimexon is probably the only cancer drug under development at this time which exploits this mechanism of action. Amplimexon is an inhibitor of ribonucleotide reductase, a key enzyme in DNA synthesis that is also a target for gemcitabine. Amplimexon is also a cell cycle inhibitor and in the presence of the drug cells accumulate in S phase.

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