Avocado (Persea americana Mill.) has had considerable attention in recent years due to the presence of valuable bioactive compounds with potential health benefits. The bioactive constituents of avocados encompass a diverse range of compounds, including monounsaturated fatty acids (MUFA), polyphenols, vitamins, and minerals. These constituents have been studied for their antioxidant, anti-inflammatory, antimicrobial, and cardioprotective properties. Notably, fatty acid (oleic, linoleic, palmitic, palmitoleic, linolenic), the primary MUFA in avocado, has been linked to improved cardiovascular health and lipid metabolism. Polyphenols, such as flavonoids and phenolic acids (coumaric acid, epicatechin, quercetin), contribute significantly to the antioxidant capacity of avocados. These compounds exhibit potential anticancer properties by modulating cell signaling pathways and inhibiting tumor growth. Moreover, avocado-derived phytosterols (sitosterol, campesterol, avenasterol, stigmasterol) and phytosterols (cycloartenol, sitostanol, campestanol) have shown promising effects in mitigating inflammatory responses and oxidative stress, thereby offering therapeutic potential in inflammatory diseases and age-related disorders. Avocado also serves as a rich source of vitamins, particularly vitamin E and vitamin C, which play crucial roles in immune function and skin health. Additionally, minerals like potassium and magnesium contribute to the regulation of blood pressure and muscle function, highlighting the multifaceted pharmacological benefits of avocado consumption. This review aims to provide a comprehensive exploration of the bioactive components in avocados and their pharmacological prospects.