Abstract: Mesothelin is a glycoprotein expressed mainly on some normal mesothelial cells lining the pleura, pericardium and peritoneum with limited expression on other normal tissues. Many studies in recent years have found that it is overexpressed in multiple cancers including ovarian cancers, lung cancers, pancreatic cancers and mesothelioma, so mesothelin is a promising candidate target for tumor-specific therapy. Macromolecular drugs have broader prospect of application with their superiority in safety in comparison with traditional small molecular drugs. Main types of macromolecular drugs include immune toxins, mono-antibody and antibody drug conjugates. This paper briefly reviews the target expression and function of mesothelin as well as the development progress of some mesothelin targeted biologics.