Malpighia glabra (Malpighiaceae) is a cherry fruit popularly known as acerola or West Indian cherry, with nutraceuticals in each ripening stage. The changes in the phytoconstituents, pigments, sugars, organic acids, and antioxidants were investigated during the fruit ripening and expressed in fresh weight (FW). Gentisic acid was present in the highest concentration in IMGL fruits (11.43 mg/100 g), which was reduced to 0.362 mg/100 g over-ripening. The major flavonoid present was epicatechin, and the concentration increased from 2.11 mg/100 g in immature green large (IMGL) fruits to 19.52 mg/100 g in ripe fruits. Ascorbic acid was the most abundant organic acid present, and the highest concentration was found in the IMGL fruits (2030 mg/100 g). Fructose and galactose were found in the highest concentrations in overripe fruits (2290 mg/100 g and 1460 mg/100 g, respectively). The IMGL fruits showed the highest total antioxidant activity of 5.48% and 5.34% ascorbic acid equivalent in methanolic and aqueous extracts, respectively. Mineral quantification showed that the fruits were rich in potassium and calcium (150.43 and 12.90 mg/100 g, respectively). This study could identify the appropriate stage of acerola fruit for developing functional foods with maximum utilization of phytoconstituents in all stages.