Drug intelligence / Profile preview

tesetaxel

Development stage
Discontinued
Lead developer
Odonate Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Tesetaxel is a semi-synthetic, orally bioavailable taxane derivative developed as a chemotherapy agent for various cancers, including breast cancer, gastric cancer, colorectal cancer, melanoma, prostate cancer, and other solid tumors. Unlike traditional taxanes such as paclitaxel and docetaxel that are administered intravenously, tesetaxel is taken orally. Its mechanism of action involves binding to and stabilizing tubulin in microtubules, promoting their assembly and preventing depolymerization. This leads to cell cycle arrest and inhibition of cell proliferation. Tesetaxel may also inhibit pro-angiogenic factors like vascular endothelial growth factor (VEGF), contributing to its antiangiogenic properties. Notably, it is not a substrate for P-glycoprotein-mediated drug resistance mechanisms—a common cause of resistance in standard taxane therapy—making it potentially effective against multi-drug resistant tumors. Clinical studies have shown activity in patients with metastatic breast cancer who progressed after prior therapies[1][3][4][5][6].

Brand names
tesetaxel
Other names
333754-36-2UNII-UG97LO5M8YUNII-UG-97LO5M8YUNII-UG 97LO5M8Y
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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