WAY-138451

WAY-138451 is a small molecule inhibitor of protein tyrosine phosphatase 1B (PTP1B), originally developed by Wyeth (now Pfizer) for the treatment of type 2 diabetes and obesity. PTP1B is a key negative regulator of the insulin and leptin signaling pathways; its inhibition is intended to enhance insulin sensitivity and promote weight loss by increasing leptin signaling. While WAY-138451 demonstrated efficacy in preclinical models, including improvements in glucose tolerance and reduction in body weight, the development of PTP1B inhibitors has been historically hindered by challenges in achieving sufficient selectivity over other phosphatases and optimal pharmacokinetic properties. The program appears to have been discontinued during the early stages of development.