Zinc-α2-glycoprotein (ZAG), a new adipokine, plays an important role in the development of cancer cachexia by decreasing lipid content in body via promoting lipid mobilization and utilization. The lipolytic effect of ZAG is achieved by increasing the activity of hormone sensitive lipase, activating β3 adrenergic receptors,and up-regulating cyclic adenosine monophosphate. In addition, ZAG increases adiponectin expression and decreases leptin expression in adipocytes and adipose tissue. The ZAG expression is regulated by glucocorticoid, peroxisome proliferator-activated receptor gamma agonist rosiglitazone, tumor necrosis factor-α and many other factors.ZAG can potentially be applied as a tumor marker, and may become a new target in the treatment of cancer cachexia.