In the present study, the safety and toxicity of Dendrophthoe pentandra (DP) extracted using ethyl acetate were investigated. DP ethyl acetate (DPEA) extract was screened for its phytochemical constituents using standard procedure and active compounds present in DPEA extract were determined using gas chromatographymass spectrometry (GC-MS), the toxicity of DPEA extract was investigated using brine shrimp lethality assay (BSLA) while the heavy metal content of DP plant was detected using atomic absorption spectrophotometer (AAS) and the cytotoxicity effect of DPEA extract on selected cell lines (HeLa, L929, Glioma, MD-AMB 231, Hep G2 and MCF-7) was determined through MTT assay. The results showed that DPEA extract consist of wide range of bioactive compounds including tannins, saponins, flavonoids and alkaloids. The crude extract contained 1.33% alkaloid, 2.67% flavonoid and 14.87±0.2µg/g total phenolic content. Heavy metals such as copper, zinc and manganese were present below the maximum permissible level. GC-MS result revealed the presence of 39 compounds and out of that, only decanoic acid, palmitic acid, linolenic acid and betasitosterol were suggested to contribute to the medicinal use of DP. The LC 50 of DPEA extract was underdetermined and was predicted above 1000 ppm and DPEA extract showed antiproliferative activity on MCF-7 and L929 with IC 50 of 4.72±0.52µg/ml and 18.12±3.46µg/ml respectively. Thus, the result of the present study revealed that DP plant is relatively safe and can be considered as possible candidates with promising potency to be developed as new chemotherapeutic agent.