Summary

TAK-488 is an oligopeptide analog of kisspeptin, which is a hypothalmic protein that activates the G-protein-coupled receptor GPR54 [Navarro VM, Tena-Sempere M. Nat Rev Endocrinol 2011]. A randomized, placebo-controlled Phase 1 study that used various, continuously administered doses of TAK-488 has demonstrated its safety, tolerability, and effectiveness in suppressing pituitary secretion of luteinizing hormone and follicular-stimulating hormone, which are key in the regulation of testosterone synthesis. Accordingly, serum testosterone declined to below castrate levels in most of the healthy male volunteers.