PF-00915275

PF-00915275 is a potent and selective small molecule inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), an enzyme that catalyzes the conversion of inactive cortisone to active cortisol within tissues. By inhibiting 11β-HSD1, PF-00915275 was developed to reduce local glucocorticoid activation, with the aim of improving glucose metabolism and insulin sensitivity in patients with type 2 diabetes mellitus. The drug demonstrated dose-dependent inhibition of its target in clinical studies and was generally well tolerated in healthy volunteers and patients with type 2 diabetes. However, development was discontinued after early-phase clinical trials[1][2][5][7].