Marine-derived bioactive peptides show significant promise as candidates for cardiovascular drug discovery because of their diverse biological activities and ACE-inhibitory activity. This review outlines the current state of knowledge on marine-derived ACE-inhibitory peptides as potential therapeutic targets for cardiovascular drug discovery. This narrative review was conducted using Scopus, PubMed, and Web of Science databases with a focus on eligible studies on ACE inhibition; peptide sequence and structural characteristics; hydrolysis and purification approaches; molecular docking; pharmacokinetic strategies; drug discovery; drug-delivery approaches; and clinical studies. This review shows that ACE-inhibitory peptides are derived from marine organisms. The reviewed studies report peptide activity determined by amino acid composition, peptide length, hydrophobicity, hydrolysis method, fractionation, chromatographic purification, and characterization techniques. Computer-based molecular mechanism studies further demonstrate that marine peptides interact with ACE through hydrogen bonding, hydrophobic interactions, and interactions at the catalytic subsite surrounding the Zn ion center. Most of the peptides have demonstrated antihypertensive effects in animal models, while limited clinical evidence suggests potential for further development. This review concludes that marine-derived ACE-inhibitory peptides are promising targets for cardiovascular drug discovery. Clinical translational barriers, industrial-scale production, clinical validation, and regulatory approval are essential to address in future work. Integration of molecular docking, advanced delivery approaches, medicinal chemistry, AI-assisted peptide design, sustainable green extraction, and clinical research could expedite their translation into pharmaceutical approaches for further drug development.