Drug intelligence / Profile preview

mito-lonidamine

Development stage
Preclinical
Lead developer
Medical College of Wisconsin
Modality
Small Molecules
Administration
Oral
01

Overview

**Mito-lonidamine** is a mitochondria-targeted small molecule anticancer agent derived from lonidamine. It is created by conjugating lonidamine with a mitochondria-targeting triphenylphosphonium moiety, markedly increasing its potency and mitochondrial selectivity compared to the parent compound. Mito-lonidamine potently inhibits mitochondrial bioenergetics, causing tumor-selective suppression of oxidative phosphorylation. Its mechanism involves inhibition of mitochondrial respiration, increased generation of reactive oxygen species (ROS), and alteration of redox homeostasis, ultimately leading to autophagic cell death in cancer cells. Preclinical studies have shown substantial efficacy against lung cancer progression and brain metastasis, as well as a radiosensitizer effect in prostate cancer models. Mito-lonidamine is being explored primarily for the treatment of lung and prostate cancers, with evidence suggesting it can enhance chemotherapy and radiotherapy responses and decrease tumor hypoxia[2][4][5].

Other names
mito-lonidaminemitochondria-targeted lonidamine
02

Targets

ND1 (Mitochondrial electron transport chain complex I)

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