Premna tomentosa is one of the medicinal plants that have high therapeutic versatility and the possibility of being a sustainable source of bioactive phytochemicals for use in pharmaceutical industry and environmental management. This paper evaluates the phytochemical composition of P. tomentosa leaf extracts using solvents of varying polarity (n-hexane, acetone, ethanol, and methanol) based on qualitative and quantitative phytochemical analysis, Fourier Transform Infrared (FTIR) spectroscopy and Gas Chromatography–Mass Spectrometry (GC–MS). Qualitative screening revealed that the methanolic extract had the richest phytochemical composition, having very strong (+++) presence of alkaloids, flavonoids, phenolics, tannins, saponins, glycosides and coumarins. Quantitative analysis indicated that the methanol extract had significantly high levels (p<0.001) of total phenolics (151.89±3.02 mg GAE/g), carbohydrates (134.58±2.89 mg GE/g), alkaloids (132.64±2.67 mg AE/g), flavonoids (128.67±2.81 mg QE/g), tannins (82.73±2.46 mg GAE/g), saponins (67.49±2.13 mg DE/g), proteins (61.82±1.86 mg BSAE/g), steroids (58.36±1.89 mg CE/g), glycosides (53.28±1.67 mg DTE/g), and reducing sugars (48.92±1.42 mg GE/g) compared to extracts prepared using other solvents. FTIR spectroscopic analysis confirmed the presence of hydroxyl, carbonyl, aromatic, ether and amine functional groups. GC-MS analysis revealed 25 major bioactive compounds, which included phytol, squalene, campesterol, stigmasterol, β-sitosterol, lupeol and α-tocopherol, compounds known to possess phytoremedationantimicrobial and anti-inflammatory properties. The presence of high amounts of phenolics, flavonoids, terpenoids and phytosterols also implies that P. tomentosa has significant phytoremediation potential since these phytochemicals are responsible for increasing the resistance of plants to oxidative stress due to exposure to heavy metals and organic contaminants. Therefore, methanol was found to be the best solvent for the extraction process, and phytochemical profile shows that Premna tomentosa is a valuable natural resource.