As one-electron reduced molecule of nitric oxide (NO), nitroxyl (HNO) has gained enormous attention because its novel physiological or pharmacological properties, ranging from cardiovascular protective actions to anti-tumoricidal effects. Recent Advances: HNO is emerging as a new entity with therapeutic advantages over its redox sibling, NO. The interests in the chemical, pharmacological and biological characteristics of HNO have broadened our current understanding of its role in physiology and pathophysiology.In particular, the experimental evidence suggests the therapeutic potential of HNO in tumor pharmacology, such as neuroblastoma, gastrointestinal tumor, ovarian, lung and breast cancers. Indeed, HNO donors have been demonstrated to attenuate tumor proliferation and angiogenesis.In this review, the generation and detection of HNO are outlined, and the roles of HNO in cancer progression are further discussed. We anticipate that the completion of this review might give novel insights into the roles of HNO in cancer pharmacology and open up a novel field of cancer therapy based on HNO. Key words: nitroxyl, nitric oxide; hydrogen sulfide; anti-cancer; cancer therapy.