Hypericum androsaemum L. is a plant renowned in the Mediterranean basin for diuretic, hepatoprotective, anti-hypertensive, anti-hemorrhoidal, anti-depressant and skin-protective effects. This review makes a critical summary of published pharmacognostical data. H. androasemum contains significant amounts of phenolic compounds, namely chlorogenic acids, flavonoids, triterpenoids, polycyclic polyprenylated acylphloroglucinols (PPAPs) and xanthones. Extracts of the plant have shown radical scavenging activity. The fruits' extracts have shown cytotoxic activity against some cancer cell lines. The plant has some immunomodulatory, DNA-protective, anti-glycation, antidepressant and antiinflammatory effects. Given its effect on fibroblasts proliferation and migration, collagenase and tyrosinase inhibitory action, immunomodulatory effect, UV-protective and lack of phototoxicity, it has potential in skin formulas. It has shown biocidal activity against some bacteria, fungi, nematodes, mollusks and insects. At low concentrations, the extracts were nontoxic on normal cells. However, safety issues may arise with oral administration of high hyperforin H. androasemum preparations.