Drug intelligence / Profile preview

tetrathiomolybdate

Development stage
Phase 3
Lead developer
Theriva Biologics
Modality
Small Molecules
Administration
Oral
01

Overview

Tetrathiomolybdate is an orally bioavailable, small-molecule copper chelator developed primarily as an anticopper agent. Its main mechanism involves binding to copper in the gastrointestinal tract and bloodstream, forming stable complexes that prevent copper absorption and reabsorption. This results in a significant reduction of free serum copper levels. Tetrathiomolybdate has been investigated for the treatment of neurologic Wilson's disease, where it demonstrated efficacy in lowering toxic copper accumulation. Beyond Wilson's disease, it has shown potential antiangiogenic, antifibrotic, anti-inflammatory, antimetastatic, and antitumor activities by inhibiting multiple copper-dependent enzymes and cytokines (such as VEGF, bFGF, NF-kB), thereby interfering with angiogenesis and tumor progression. It also inhibits fibrotic processes by targeting key cytokines involved in fibrosis (e.g., SPARC, TGF-beta). The drug was originally developed at the University of Michigan and further advanced by Theriva Biologics[1][2][3][4][5].

Brand names
Coprexa
Other names
thiomolybdatetiomolibdate ioncholine tetrathiomolybdate
02

Targets

FGF2Misfolded SOD1NF-κBVEGFR (VEGFR family)TGFB (GARP–latent transforming growth factor beta 1 complex)

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