The plethora of bio-functional compounds that are present in fermented alcoholic beverages and their “wastes,” including beer and breweries’ by-products, have recently gained attention for their valorization as functional ingredients in several novel bio-functional products of the food, drug, and cosmetic sectors. Within this chapter, the functional compounds present in beer and their biological activities involved in health-promoting benefits of moderate consumption of beer as part of a balanced diet, against inflammation-related chronic disorders, are thoroughly reviewed, while the detrimental effects of abusing alcoholic beer consumption and the potential benefits of alternative nonalcoholic beer products are also discussed. An overview of the natural bioactive compounds that are present in beer and in breweries’ by-products (i.e., pre-/probiotics, bioactive phenolic compounds, bio-functional lipid compounds, vitamins, and valuable fiber and minerals) is also conducted, along with an evaluation of their mechanisms of action and synergism, in which the anti-inflammatory, antithrombotic, and antioxidant benefits are elicited to lower the risk of inflammation-related disorders. Current status and future perspectives on valorizing such beer and brewery by-products’ bioactives in novel foods, supplements, nutraceuticals, and cosmeceuticals and their health-promoting properties are thoroughly evaluated, while the limitations of valorizing breweries’ by-products are also addressed.