Pharmacodynamic Activity of the Novel Neurokinin-3 Receptor Antagonist SJX-653 in Healthy Men.

ABSTRACT: SJX-653 is a novel neurokinin 3 receptor (NK3R) antagonist. The NK3 pathway is a central regulator of gonadotropin releasing hormone (GnRH) secretion and has also been implicated in the generation of hot flashes. Therefore, decreases of luteinizing hormone (LH) and testosterone in men serve as sensitive pharmacodynamic (PD) markers of central NK3 antagonism. To characterize the safety, tolerability, pharmacokinetics, and pharmacodynamic activity of SJX-653 in healthy men. A randomized, placebo-controlled, double-blind, single ascending dose study. Phase 1 unit. Seven cohorts of 6 healthy men 18-45 years of age (4:2 randomization to SJX-653/placebo per cohort). Single oral doses of 0.5-90 mg SJX-653. Safety assessments and serial pharmacokinetic (PK)/PD measurements. SJX-653 was well tolera

SUBMITTER: Anderson RA 

PROVIDER: S-EPMC7571451 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature