Drug intelligence / Profile preview

tetramethoxystilbene

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Ex Vivo Vascular Exposure, Liposomal Formulation (preclinical)
01

Overview

**Tetramethoxystilbene** is a synthetic methylated derivative of resveratrol classified as a small molecule polyphenol. It displays potent **antioxidant** properties and acts as a selective and competitive inhibitor of cytochrome P450 1B1 (CYP1B1)[3][7]. In preclinical studies, TMS has shown ability to reduce blood pressure, cardiac fibrosis, vascular hypertrophy, and oxidative stress, mainly by inhibition of CYP1B1 and reduction of NADPH-oxidase-derived reactive oxygen species[1][3][9]. TMS also demonstrated anti-cancer activity, especially notable in gefitinib-resistant non-small-cell lung cancer (NSCLC), via selective elevation of intracellular calcium, direct inhibition of SERCA (sarco/endoplasmic reticulum Ca2+-ATPase), induction of endoplasmic reticulum stress, and activation of autophagy and apoptosis[5]. TMS is of interest for hypertension, cardiovascular, and cancer indications, but is investigational and not approved for clinical use.

Other names
2,3',4,5'-tetramethoxystilbeneTMS(E)-3,3',4,5'-tetramethoxystilbenetrans-3,4,5,4'-tetramethoxystilbene2,4,3',5'-tetramethoxystilbene
02

Targets

CYP1B1 (Cytochrome P450 1B1)

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