This book examines cardiac glycosides (CGs) as emerging multi-targeted anticancer agents. Beyond their traditional use in cardiology CGs modulate Na⁺/K⁺-ATPase-linked signaling pathways that control cancer cell survival apoptosis autophagy angiogenesis and immune activation. The book highlights key mechanisms including mitochondrial apoptosis ROS generation HIF-1α inhibition and immunogenic cell death that enhances antitumor immunity. It summarizes strong preclinical evidence across major cancer types and outlines synergy with chemotherapy targeted therapy radiotherapy and immunotherapy. Clinical findings are promising but limited by cardiotoxicity narrow therapeutic index pharmacokinetic variability and tumor heterogeneity. The book explores innovative solutions-structure-activity optimization isoform-selective analogues nanoparticle delivery tumor-activated prodrugs AI-guided drug design and biomarker-based patient selection-to improve safety and efficacy. It concludes that CGs hold significant potential as future precision oncology therapeutics.
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