Apple pomace (AP) utilised for analysis of triterpenic acids (TTAs) using HPLC-MS/MS. The methanol, ethanol and ethyl acetate extracts showed high phenolic content with significant antioxidant activity compared to chloroform and n-hexane. AP TTAs; ursolic acid, betulinic acid and maslinic acid showed potent antioxidant and enzyme inhibitory effects. The IC50 values were 13.2–30.8 μg/mL (tyrosinase), 19.6–42.5 μg/mL (xanthine oxidase) and 16.6–38.6 μg/mL (urease) for AP extracts and 8.4–25.8 μg/mL (tyrosinase), 12.6–30.2 μg/mL (xanthine oxidase) and 10.1–28.6 μg/mL (urease) for TTAs, compared to the positive controls; kojic acid (10.4 ± 0.06 μg/mL), allopurinol (9.6 ± 0.04 μg/mL) and thiourea (8.9 ± 0.02 μg/mL) towards respective enzymes. UA showed a competitive type of inhibition for tyrosinase, while BA showed a noncompetitive type of inhibition towards xanthine oxidase. In addition, the AP extracts and TTAs exerted significant cytotoxic effects towards the proliferation of cancer cell lines. AP methanol extract (IC50 of 38.5 ± 4.1, 47.1 ± 3.5, 70.6 ± 2.3, and 50.5 ± 3.9 μg/mL) and ursolic acid (IC50 of 6.5 ± 0.7, 15.5 ± 1.4, 20.8 ± 1.3, and 5.6 ± 0.8 μg/mL) showed prominent anticancer activity on Hela, Skov-3, Caski, and NCL cancer cell lines, respectively. Thus, this study shows that the AP & TTAs could be utilized for functional food development and as a potent antioxidant, anticancer, skin whitening, and anti-urolithic agents. Display omitted •Utilization of apple pomace (AP) towards extraction of triterpenic acids.•HPLC-MS/MS analysis showed significant composition of triterpenic acids.•Inhibition of tyrosinase, xanthine oxidase and urease by AP triterpenic acids.•Apple pomace and triterpenic acids revealed significant therapeutic effects.