Purpose: To investigate the phytochemistry, cytotoxicity and acute toxicity of leaf extracts from Annona vepretorum.Methods: The crude extracts were obtained by maceration with hexane and methanol. The crude methanol extract was suspended in a 3:7 (v/v) mixture of methanol (MeOH) and water (H2O) and partitioned with hexane, chloroform (CHCl3) and ethyl acetate (AcOEt) in ascending order of polarity to obtain the respective extracts. In the investigation of phytochemical profile, the extracts were evaluated on thin layer chromatography (TLC) plates of silica gel. Cytotoxicity was tested using 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) and (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) (MTS) assays against tumor cell lines, viz,HCT-116 (colon), SF-295 (brain), HL-60 (leukemic) and Sarcoma-180. Acute toxicity study was performed by administration of a single oral dose of 2 g/kg body weight of the extracts to mice and the animals were observed for 14 days.Results: Phytochemical screening results showed that A. vepretorum extracts contain alkaloids, flavonoids and terpenes. Methanol and chloroform extracts exhibited high cytotoxic activity against HCT-116, HL-60 and Sarcoma-180. Moreover, the extracts displayed low toxicity in mice, as no deaths and pronounced toxic effects were observed.Conclusion: A. vepretorum contains a variety of secondary metabolites which may confer on this species high cytotoxic activity. In addition, the oral administration of the extracts produced low toxicity in mice.Keywords: Annonaceae, Annona vepretorum, Phytochemistry, Tumor cell lines, Acute toxicit