Drug intelligence / Profile preview

Second-generation TASIN

Development stage
Preclinical
Lead developer
Barricade Therapeutics
Modality
Small Molecules
01

Overview

Second-generation TASIN (Truncated APC Selective Inhibitor) is a small molecule drug program being developed by Barricade Therapeutics for the treatment of multiple sclerosis and other demyelinating diseases. These compounds target the emopamil binding protein (EBP), an enzyme within the cholesterol biosynthesis pathway. By inhibiting EBP, TASINs induce the accumulation of specific sterol intermediates that promote oligodendrocyte formation and subsequent remyelination. Originally discovered at the University of Texas Southwestern Medical Center for their ability to selectively kill cells with APC mutations (such as in colorectal cancer), these second-generation derivatives are being chemically optimized for their pro-myelinating properties and CNS penetration. The program is currently in preclinical development, with the company aiming to advance specific candidates into further development for demyelinating diseases.

Other names
Truncated APC Selective InhibitorTASINs
02

Targets

DHCR24 (3β-hydroxysterol Δ24-reductase)DHCR7 (7-dehydrocholesterol reductase)EBP (Sterol isomerase (emopamil-binding protein))

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