リュープリン (高活性LH-RH誘導体) の研究開発

抄録

Biologically active peptide have potential therapeutic applications in the treatment of diseases caused by peptide deficiency. However, there are only a few peptide drugs, Elcitonin (a calcitonin derivatives for osteoporosis, Asahikasei), Hirutonin (TRH tartrate for prolonged disturbance of consciousness, Takeda) and Leuplin (a highly potent LH-RH derivative for prostate cancer/endometriosis, Takeda) There are two serious drawbacks to using peptide derivatives as drugs : their poor oral bioavailability and their short duration of activity. Although the latter can be overcome by studing various derivatives, the development of orally active peptide derivatives is almost impossible. I would like to describe briefly the process of the research and development of “Leuplin Depot”, once-a-month depot type formulation of super agonist of LH-RH.