Sorghum beer (pito) is an indigenous alcoholic beverage peculiar to northern Ghana and parts of other West African countries. It is overwhelmed with calories, essential amino acids (such as lysine, etc.), B-group vitamins, and minerals. In recent years, there has been a growing demand for highly flavoured yet functional pito in Ghana; however, the local producers lack the prerequisite scientific expertise in designing such products. We propose the utilization of Tetrapleura tetraptera (TT) and Hibiscus sabdariffa (HS) as cheap and readily available materials in designing functional flavoured pito. The addition of TT and HS would not alter the fermentation profile but rather augment the starter with nutrients, thus improving the fermentation performance and shelf life of the final pito. In vitro and in vivo studies provide substantive evidence of antioxidant, nephro-and hepato-protective, renal/diuretic effect, anticholesterol, antidiabetic, and antihypertensive effects among others of the TT and HS, hence enriching the pito with health-promoting factors and consequently boosting the health of the consumer. Herein, we summarise the phytochemical, biological, pharmacological, and toxicological aspects of TT and HS as well as the technology involved in brewing the novel bioactive-flavoured pito. In addition, we also report the incidence of heavy metal in conventional pito.