Sustained Exposure to the Investigational Kisspeptin Analog, TAK-448, Down-Regulates Testosterone into the Castration Range in Healthy Males and in Patients With Prostate Cancer: Results From Two Phase 1 Studies

摘要

Background/Objective:Kisspeptin-54, an endogenous naturally occurring ligand of the G protein-coupled receptor-54, stimulates GnRH-gonadotropin secretion and suppresses metastases in animal models of cancer but is subject to rapid degradation and inactivation. TAK-448 is an investigational oligopeptide analog of the fully active 10-amino acid C terminus of kisspeptin-54. This phase 1 study evaluated the safety, pharmacokinetics, and pharmacodynamics of TAK-448 in healthy subjects and patients with prostate cancer (PC).