Abstract: Octapeptin is a class of cyclic lipopeptides with broad-spectrum antibacterial activity, demonstrating significant potential against multidrug-resistant Gram-negative bacteria. This review provides a comprehensive overview of the sources, structure, synthesis methods, and antibacterial mechanisms of octapeptin, with a focus on the impact of structural modifications on their antibacterial activity. The unique structural features of octapeptin contribute to their strong antibacterial potential, and structural modifications can significantly enhance their activity, offering insights into the development of novel antibiotics.