Drug intelligence / Profile preview

elesclomol + docetaxel

Development stage
Preclinical
Lead developer
Madrigal Pharmaceuticals
Modality
Small Molecules
Administration
Intravenous
01

Overview

A combination drug consisting of **elesclomol**, a small-molecule copper ionophore that induces oxidative stress and mitochondrial apoptosis, and **docetaxel**, a microtubule-stabilizing chemotherapeutic agent. Elesclomol elevates intracellular reactive oxygen species (ROS) by shuttling copper into cancer cells, promoting cell death especially in tumors dependent on mitochondrial metabolism. Docetaxel disrupts cell division by stabilizing microtubules, causing cell cycle arrest and apoptosis. Combination of elesclomol with taxanes (such as docetaxel or paclitaxel) has shown synergistic preclinical and clinical anticancer activity, primarily by exploiting different metabolic or cell cycle vulnerabilities in tumor cells, and is under study in solid tumors and advanced/metastatic cancers. Clinical trials and preclinical studies suggest that dual targeting of mitochondrial metabolism and cell division may enhance cytotoxicity compared to monotherapy[1][2][3][4].

02

Targets

MicrotubuleTUBB (Tubulin (alpha and beta subunits))ND1 (Mitochondrial electron transport chain complex I)

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