This review aims to analyze Mentha piperita L. as a potential raw material for the development of new health-promoting products (nutraceuticals, cosmetics, and pharmaceutical products). A lot of scientific publications were retrieved from the Scopus, PubMed, and Google Scholar databases which enable the study and generalization of the extraction procedures, key biologically active compounds of essential oil and extracts, biological properties, and therapeutic potential of M. piperita, along with perspectives on the development of its dosage forms, including combinations of synthetic active substances and herbal preparations of M. piperita. The results of this review indicate that M. piperita is a source rich in phytoconstituents of different chemical nature and can be regarded as a source of active substances to enhance health and to develop medicinal products for complementary therapy of various conditions, especially those related with oxidant stress, inflammation, and moderate infections. Essential oil has a broad spectrum of activities. Depending on the test and concentration, this essential oil has both anti- and prooxidant properties. Gram-positive bacteria are more sensitive to the essential oil of M. piperita than Gram-negative ones. This review also considered some facets of the standardization of essential oil and extracts of M. piperita. Among the identified phenolics of extracts were caffeic acid, rosmarinic acid, eriocitrin, luteolin derivates (luteolin-7-O-rutinoside, luteolin-7-O-glucoronide), and hesperidin. The concentration of these phenolics depends on the solvent used. This review also considered the relationships between the chemical component and biological activity. The results showed that the essential oil and extracts reduced inflammation in vitro by inhibiting the production of pro-inflammatory cytokines, such as tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6), and in vivo by reducing the paw edema induced using carrageenan injection in rats. Therefore, herbal preparations of M. piperita are promising medicinal and cosmetic preparations for their usage in skincare and oral cavity care products with antimicrobial, anti-inflammatory, and wound-healing properties. This plant can also be regarded as a platform for the development of antibacterial preparations and combined anti-inflammatory and cardioprotective medicinal products (synthetic active substances plus herbal preparations). This review could be considered for the justification of the composition of some medicinal products during their pharmaceutical development for writing a registration dossier in the format of Common Technical Document.