Drug intelligence / Profile preview

simotaxel

Development stage
Phase 1
Lead developer
Taxolog
Modality
Small Molecules
Administration
Oral
01

Overview

Simotaxel is a semi-synthetic, orally bioavailable, third-generation taxane derivative and microtubule-stabilizing agent with potential antineoplastic activity. It was developed as a small molecule drug for the treatment of cancer, particularly advanced malignant solid tumors. Simotaxel binds to tubulin, promotes microtubule assembly and stabilization, and prevents microtubule depolymerization. This leads to G2/M cell cycle arrest, apoptosis, and inhibition of tumor cell proliferation. Notably, simotaxel is a poor substrate for P-glycoprotein-related drug resistance mechanisms and has shown greater potency than paclitaxel or docetaxel in preclinical models—including overcoming resistance to these agents in certain tumor types. The drug was initially developed by University of Florida and further pursued by Taxolog and Wyeth (later Pfizer). Clinical development reached Phase 1 trials for neoplasms but has since been discontinued[1][2][3][4][5].

Other names
simotaxel (USAN)
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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