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R-CP201 is the purified R-enantiomer of edelfosine, an alkylphospholipid anticancer agent. Developed by RDP Pharma, it acts by integrating into lipid rafts within cell membranes, including the endoplasmic reticulum and mitochondria. Its mechanism of action involves inducing CD95-mediated apoptosis and inhibiting signaling pathways such as AKT3/PI3K, phospholipase C, and protein kinase C. It also disrupts cholesterol and phosphatidylcholine metabolism. While edelfosine has been studied as a racemic mixture, RDP Pharma is evaluating the individual enantiomers (R-CP201 and S-CP201) for improved pharmacokinetic and pharmacodynamic profiles. In preclinical studies for pancreatic cancer, R-CP201 demonstrated tumor growth inhibition, though it generally showed lower systemic exposure and efficacy compared to the S-enantiomer (S-CP201).
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