Pomelo (Citrus maxima) is one of the citrus species that is widely consumed. Consumption of pomelo oranges produces fruit peels that tend to be underutilized, so it may produce some waste. Most of the reported research has been extensively studied for its phytochemical and pharmacological properties. The objective of this review article is to provide a comprehensive overview of the chemical compounds and pharmacological activity of the pomelo peel as an introduction to further research related to structure determination and activity testing. Several phytochemicals have been reported from Citrus maxima fruit peel including flavonoids, coumarins, phenylpropanoids, phenolics, steroids, and essential oils. These phytochemicals also exhibit some pharmacological activities, including antioxidant, antimicrobial, anti-inflammation, insecticidal, antialzheimer, and antidiabetic. Further research is needed to explore the fruit peel extract’s activities and compounds in more detail for drug design, herbal products, and or functional foods. Proposed development based on pharmacological activities such as external remedies, internal remedies, dietary supplements, and pesticides.