Abstract Cyclolinopeptides (CLs) are active ingredients with significant edible and medicinal value, that have been isolated from Linum usitatissimum L. in recent years. CLs can also be extracted from flaxseed oil, but there is currently no quality control or standardization of their content in flaxseed oil. CLs exhibit elevated efficiency, low toxicity, and a variety of pharmacological activities such as immunomodulation, anti‐osteoporosis, anticancer, antimalarial, and antibacterial effects, among others. Despite the broad application prospects of CLs, the specific mechanism by which they function remains unknown. Although research on CLs is still primarily in the preclinical phase, advancements in separation technology and the increase in flaxseed oil production have significantly reduced extraction costs. This has led to further research into understanding the diverse biological and pharmacological properties of CLs. The aim of this review is to provide a comprehensive overview of recent advancements in understanding the multifaceted biological and pharmacological properties of CLs.