Tumor　formation　and　growth　depend　on　various　biological　metabolism　processes　that　are　distinctly　different　with　normal　tissues.　Abnormal　energy　metabolism　is　one　of　the　typical　characteristics　of　tumors.　It　has　been　proven　that　most　tumor　cells　highly　rely　on　aerobic　glycolysis　to　obtain　energy　rather　than　mitochondrial　oxidative　phosphorylation　(OXPHOS)　even　in　the　presence　of　oxygen,　a　phenomenon　called　“Warburg　effect”.　Thus,　inhibition　of　aerobic　glycolysis　becomes　an　attractive　strategy　to　specifically　kill　tumor　cells,　while　normal　cells　remain　unaffected.　In　recent　years,　a　small　molecule　alkylating　agent,　3-bromopyruvate　(3-BrPA),　being　an　effective　glycolytic　inhibitor,　has　shown　great　potential　as　a　promising　antitumor　drug.　Not　only　it　targets　glycolysis　process,　but　also　inhibits　mitochondrial　OXPHOS　in　tumor　cells.　Excellent　antitumor　effects　of　3-BrPA　were　observed　in　cultured　cells　and　tumor-bearing　animal　models.　In　this　review,　we　described　the　energy　metabolic　pathways　of　tumor　cells,　mechanism　of　action　and　cellular　targets　of　3-BrPA,　antitumor　effects,　and　the　underlying　mechanism　of　3-BrPA　alone　or　in　combination　with　other　antitumor　drugs　(e.g.,　cisplatin,　doxorubicin,　daunorubicin,　5-fluorouracil,　etc.)　in　vitro　and　in　vivo.　In　addition,　few　human　case　studies　of　3-BrPA　were　also　involved.　Finally,　the　novel　chemotherapeutic　strategies　of　3-BrPA,　including　wafer,　liposomal　nanoparticle,　aerosol,　and　conjugate　formulations,　were　also　discussed　for　future　clinical　application.　©　2019　by　the　authors.　Licensee　MDPI,　Basel,　Switzerland.