Saussurea heteromalla is the one of specie of Saussurea plant belonging to family Asteraceae. The Saussurea heteromalla found extensively in Pakistan. The literature review highlights numerous biological aspects of Saussurea heteromalla. This research therefore aims to assess its potential anti-inflammatory, antioxidant, anti-cancer. Carrageenan induced rat paw edema model was used for the evaluation of anti-inflammatory activity. DPPH method was used to evaluate anti-oxidant activity. The MTT (3- [4, 5-dimethylthiazol-2-yl]-2, 5 diphenyl tetrazolium bromide) test was used to assess the viability of the cells for the assessment of the cytotoxic effect of the extract. Methanolic Saussurea heteromalla flowers extract analysis carried by GC-MS, result 19 different peaks. The methanolic extract of Saussurea heteromalla at 400mg/kg dose have equal anti-inflammatory action when compare with standard that is diclofenac sodium. Anti-oxidant activity of methanolic extract is also very good. IC50 value of methanol extract was 25µg/ml. 18.72% cell survive out of 100 when methanolic flower extract of Saussurea heteromalla was given at the dose of 400mg, which shows the cytotoxic effect. This activity shows that plant Saussurea heteromalla methanolic flowers extract have anti-inflammatory, anti-oxidant, cytotoxic effect. The isolation and characterization-based investigations proclaiming the biologically leading active molecule are worthy for further study in this regard.