Diabetes and Obesity are the major health problems in the modern world. Although a no. of drugs are available to control both of these problems but due to limitations of their side effects, there is need of search for the novel targets for the treatment of these problems. Protein tyrosine phosphatase -1B (PTP-1B) is a novel target of such type. It is implicated in both insulin and leptin signaling and is found to be negative regulator of both. Therefore it is an emerging therapeutic target to treat both diabetes and obesity. But due to some important issues like less selectivity and low bioavailability, the inhibitor development is a challenging job and therefore a safe, selective and efficacious PTP-1B inhibitor has yet to be identified. So many researches are currently in progress related to this aspect and attempts are made to avoid the problems associated with the safety and efficacy of PTP-1B inhibitors. Along with diabetes and obesity, PTP-1B is also implicated in some non-metabolic diseases like cancer. Therefore PTP-1B is an interesting novel therapeutic target that has attracted the interest of many researches toward itself.