Betulinic acid (BA), a lupane-type pentacyclic triterpenoid saponin from tree bark, has the potential to induce the apoptosis of cancer cells without toxicity towards normal cells invitro and invivo. The antitumor pharmacological effects of BA consist of triggering apoptosis via the mitochondrial pathway, regulating the cell cycle and the angiogenic pathway via factors, including specificity protein transcription factors, cyclinD1 and epidermal growth factor receptor, inhibiting the signal transducer and activator of transcription3 and nuclear factor‑κB signaling pathways, preventing the invasion and metastasis of tumor cells, and affecting the expression of topoisomeraseI, p53 and laminB1. In previous years, several studies have shown its antitumor effect, initially applied to malignant melanoma, however, it also has broad efficacies against most solid types of tumor from different regions of the body. There have been few investigations in hematological malignancies, however, this direction may offer potential in such a novel field of research. In this review, the primary pharmacological effects of BA in tumors, particularly in hematological malignancies are discussed.