Key result
The semi-synthetic flavonoid monoHER demonstrated protective effects against doxorubicin-induced cardiotoxicity in preclinical models and was found to be safe and feasible at an intravenous dose of 1,500 mg/m2 in a phase I clinical study.
Why the study?
Does 7-monohydroxyethylrutoside (monoHER) prevent doxorubicin-induced cardiotoxicity in preclinical models and is it safe in humans?
Does 7-monohydroxyethylrutoside (monoHER) prevent doxorubicin-induced cardiotoxicity in preclinical models and is it safe in humans?
Answers are grounded in this paper and cite their sources.
MonoHER is a promising flavonoid that protects against doxorubicin-induced cardiotoxicity in preclinical models without compromising antitumor efficacy, and has demonstrated safety in a phase I human trial.
Cardiotoxic side-effects of doxorubicin limit the clinical use of this anti-cancer agent. Iron chelators have been studied as protectors against doxorubicin-induced cardiotoxicity. These iron chelators do not provide optimal protection and have certain drawbacks. We therefore looked for new protectors and decided that these new compounds should combine iron chelating and antioxidant activity. Flavonoids appeared to possess those combined iron chelating and antioxidant properties. Quantum chemical evaluation of radical stabilization and determination of physico-chemical properties of a series of flavonoids brought our attention to the semi-synthetic flavonoid 7-monohydroxyetylrutoside (monoHER). Both in vitro (using an electrically paced mouse left atrium model) and in vivo (using a mouse ECG telemetry model) experiments corroborated the protective effect of monoHER. MonoHER also showed anti-inflammatory properties. A subsequent clinical phase I study showed that an i.v. dose of 1,500mg/m2 is a feasible and safe dose to be evaluated in a phase II study to investigate the protective properties of monoHER against doxorubicin-induced cardiotoxicity in cancer patients.
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Bast et al. (2007) conducted a review in Doxorubicin-induced cardiotoxicity. 7-monohydroxyethylrutoside (monoHER) vs. Placebo was evaluated. The semi-synthetic flavonoid monoHER demonstrated protective effects against doxorubicin-induced cardiotoxicity in preclinical models and was found to be safe and feasible at an intravenous dose of 1,500 mg/m2 in a phase I clinical study.
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