Key result
Calmangafodipir improves Mn binding stability and superoxide dismutase mimetic activity over mangafodipir.
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Reactive oxygen species (ROS) and reactive nitrogen species (RNS) participate in pathological tissue damage. Mitochondrial manganese superoxide dismutase (MnSOD) normally keeps ROS and RNS in check. During development of mangafodipir (MnDPDP) as a magnetic resonance imaging (MRI) contrast agent, it was discovered that MnDPDP and its metabolite manganese pyridoxyl ethyldiamine (MnPLED) possessed SOD mimetic activity. MnDPDP has been tested as a chemotherapy adjunct in cancer patients and as an adjunct to percutaneous coronary intervention in patients with myocardial infarctions, with promising results. Whereas MRI contrast depends on release of Mn(2+), the SOD mimetic activity depends on Mn(2+) that remains bound to DPDP or PLED. Calmangafodipir [Ca4Mn(DPDP)5] is stabilized with respect to Mn(2+) and has superior therapeutic activity. Ca4Mn(DPDP)5 is presently being explored as a chemotherapy adjunct in a clinical multicenter Phase II study in patients with metastatic colorectal cancer.
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Karlsson et al. (2014) conducted a review in Cancer and myocardial infarction. Calmangafodipir [Ca4Mn(DPDP)5], mangafodipir (MnDPDP), and MnPLED was evaluated. Calmangafodipir [Ca4Mn(DPDP)5] exhibits stabilized Mn(2+) binding and superior SOD mimetic therapeutic activity compared to mangafodipir, and is in Phase II testing for metastatic colorectal cancer.
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