Cheese whey (CW) is the yellow-green liquid main by-product from cheese manufacturing. Historically, it has been recognized as a major environmental pollutant. Nowadays, it represents a source of high-quality nutrients, such as lactose. Enzymatic bioprocesses, chemical synthetic reactions and microbial bioprocesses use lactose as substrate to obtain relevant derivatives such as lactitol, lactulose, lactosucrose, sialyllactose, kefiran and galacto-oligosaccharides. These lactose derivatives stimulate the growth of indigenous bifidobacteria and lactobacilli improving the intestinal motility, enhancing immunity and promoting the synthesis of vitamins. Also, they have versatile applications in pharmaceutical, biotechnological and food industries. Therefore, this book chapter shows the state of the art focusing on recent uses of CW lactose to produce value-added functional compounds and discusses new insights associated with their human health-promoting effects and well-being.