Drug intelligence / Profile preview

tetraiodothyroacetic acid

Development stage
Unknown
Lead developer
Cleveland Clinic
Modality
Small Molecules
Administration
Intravenous
01

Overview

Tetraiodothyroacetic acid (tetrac) is a deaminated analogue of the thyroid hormone L-thyroxine (T4). Unlike the parental hormone, tetrac acts as an antagonist at the cell surface receptor for thyroid hormone located on the extracellular domain of integrin $\alpha_v\beta_3$. This integrin is frequently overexpressed in cancer cells and actively dividing endothelial cells. By binding to this site, tetrac inhibits the pro-angiogenic and pro-proliferative effects of T4 and triiodothyronine (T3). It has demonstrated the ability to induce apoptosis, arrest the cell cycle, and act as a radiosensitizer by inhibiting the repair of DNA double-strand breaks. A nanoparticulate formulation, often referred to as Nanotetrac or NDAT (nanoparticulate diamino-tetrac), has been developed to restrict the drug's action to the cell surface integrin receptor and prevent its entry into the cell nucleus, thereby enhancing its anti-cancer profile.

Other names
3,3',5,5'-tetraiodothyroacetic acidT4acT-4acT 4acNanotetrac
02

Targets

αVβ3 (Integrin αVβ3)

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