chapter  23
14 Pages

Depot Injectable Microcapsules of Leuprorelin Acetate (Lupron Depot)

INTRODUCTION Leuprorelin acetate (leuprolide acetate), Des-Gly10-(D-Leu6)-LH-RH ethylamide, is a synthetic nonapeptide analogue of a naturally occurring gonadotropinreleasing hormone called luteinizing hormone-releasing hormone (LH-RH) (Fig. 1). This analogue, originally synthesized by Fujino et al. at Takeda Pharmaceutical Co. (1), is the first superactive agonist to exhibit more than 10 times the biological activity of natural LH-RH.