Drug intelligence / Profile preview

trodusquemine

Development stage
Phase 1
Lead developer
DepYmed
Modality
Small Molecules
Administration
Intravenous, Subcutaneous
01

Overview

Trodusquemine is a naturally occurring aminosterol and cholestane originally isolated from the liver of the dogfish shark (*Squalus acanthias*), but now also synthesized in laboratories. It acts as a non-competitive allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B), which plays a key role in insulin and leptin signaling pathways. By inhibiting PTP1B centrally and peripherally, trodusquemine enhances insulin sensitivity and glycemic control. It also suppresses feeding behavior by acting on the hypothalamus’s paraventricular nucleus and modulates neuropeptide expression associated with weight loss. In addition to its metabolic effects, trodusquemine has demonstrated regenerative properties in animal models (e.g., heart regeneration), anti-atherosclerotic activity by preventing macrophage foam cell formation, broad-spectrum antimicrobial activity, neuroprotective effects (including reduction of toxic protein aggregates relevant to neurodegenerative diseases), antitumor activity through inhibition of tumor cell proliferation via PTP1B inhibition or other mechanisms such as dopamine/norepinephrine reuptake inhibition[2][5][9].

Other names
Trodusquemine [USAN]TrodusqueminaProdulestan3-N-1(spermine)-7,24-dihydroxy-5-cholestane 24-sulfate3beta-N-1(spermine)-7alpha,24R-dihydroxy-5alpha-cholestane 24-sulfate
02

Targets

PTPN1 (Protein tyrosine phosphatase 1B)

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