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Cyclocreatine is a small molecule analog of creatine that acts as a substrate for creatine kinase and can enter the brain via alternative transport mechanisms. It is phosphorylated to phosphocyclocreatine inside cells, acting as a high-energy phosphate reservoir. Cyclocreatine serves as a replacement for creatine in tissues where creatine or its transport are deficient, notably in some creatine deficiency syndromes. It has demonstrated preclinical neuroprotective effects, can protect against energy depletion and oxidative injury, and has been studied as a potential therapy in conditions such as creatine transporter deficiency, Huntington's disease, and certain cancers. Cyclocreatine also suppresses creatine metabolism, impairs proliferation in cancer cells (notably prostate cancer), and has shown antitumor, antiviral, cardioprotective, anti-inflammatory, and neuroprotective activities in experimental models. It is not currently an approved pharmaceutical drug, but has received orphan designation for creatine deficiency syndromes and/or ischemic injury prevention in heart transplantation[1][2][3][5][6][7][8][9].
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