Pink rock-rose (C. creticus), among the Cistaceae family, is an herb highly distributed along the coasts of Central-South-East Mediterranean, while the subspecies C. creticus subsp. creticus and C. creticus subsp. eriocephalus are endemic mostly in the Greek island of Crete. The scope of this comprehensive research is the gathering of published literature on the historical and ethnopharmacological uses as well as on the phytochemical profile (aerial part, flower, resin, and essential oil extracts) and the different pharmacological, non-clinical and clinical, activities. Antimicrobial activities, including in vitro and in vivo antibacterial, antifungal, and antiviral data, and clinical studies, using different extracts and/or isolated compounds of the plant as single herbal substance or in combinations, were extensively reviewed. Potential mechanisms of action and safety parameters were investigated. Through this review, an increased interest in pink rock-rose was found, while the need of quality standards (mostly phenolic content) and appropriate analyses to promote its proper and safer use for future applications is highlighted.