Globularia alypum L. (Plantaginaceae) is widespread in the Mediterranean region and traditionally used against diabetes, digestive disorders, infections, and skin problems. This review summarizes its botanical features, ethnobotanical uses, phytochemistry, pharmacological effects, and toxicological profile. Relevant studies published between 1991 and 2024 were retrieved from Web of Science, Scopus, PubMed, and other relevant databases using targeted keywords in English and French. Extracts of G. alypum have shown significant antidiabetic, antioxidant, anticancer, antibacterial, anti-inflammatory, anticoagulant, nephroprotective, and wound-healing activities in vitro and in vivo, which were largely attributed to its diverse secondary metabolites such as phenolics, flavonoids, and iridoids. Toxicological studies indicate generally low risk at tested doses. However, further research is needed to elucidate the molecular mechanisms underlying these activities, validate its efficacy through clinical trials, and evaluate long-term safety, thereby bridging traditional knowledge with modern pharmacological evidence.