Efaproxiral (RSR13)

Description: Efaproxiral (RSR13) is a synthetic allosteric modifier of hemoglobin (Hb) and a bezafibrate analog used for brain metastases originating from breast cancer. Efaproxiral has been shown to bind reversibly to hemoglobin, stabilizing the deoxyhemoglobin tetramer conformation to reduce its affinity for oxygen. Efaproxiral plus oxygen breathing reduces the radiobiological hypoxic fraction of EMT6 tumors from the value of 24% found in both air-breathing and oxygen-breathing mice to 9% and improves the response of the tumors to radiation. It also has the potential to be used for the treatment of depression, traumatic brain injury, ischemia, stroke, myocardial infarction, diabetes, hypoxia, sickle cell disease, hypercholesterolemia and as a radio sensitiser.

References: Exp Biol Med (Maywood). 2006 Mar; 231(3):317-21; Radiat Res. 2007 Aug; 168(2):218-25.

Related CAS #: 131179-95-8 (free acid); 170787-99-2 (sodium)