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Efaproxiral is a synthetic small molecule and an analogue of bezafibrate developed primarily as a radiosensitizer for cancer therapy. Its mechanism of action involves binding non-covalently to the hemoglobin tetramer and decreasing hemoglobin's oxygen-binding affinity, which shifts the oxygen dissociation curve to the right. This results in increased release of oxygen from hemoglobin into hypoxic tumor tissues, thereby reducing tumor radioresistance and potentially enhancing the efficacy of radiation therapy. Efaproxiral has also been investigated for other indications including depression, traumatic brain injury, ischemia, stroke, myocardial infarction, diabetes, hypoxia-related conditions such as sickle cell disease and hypercholesterolemia. The drug reached phase III clinical trials but did not demonstrate benefit in pivotal studies for its primary indication.
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