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This phase 1 clinical study was an open\u2010label, parallel\u2010design, single\u2010center, single\u2010dose study in older, healthy male subjects. Following injection, teverelix is released into the systemic circulation in a biphasic manner. An initial rapid phase is followed by a slow\u2010release phase thought to be due to the formation of a depot, which limits the diffusion of teverelix into the blood. The release characteristics differ significantly for the subcutaneous (SC) and intramuscular (IM) routes. Teverelix maximum concentration and exposure increased in an approximately dose\u2010proportional manner across the 60 to 120\u00a0mg SC doses. All 3 pharmacodynamic end points (luteinizing hormone, follicle\u2010stimulating hormone, and total testosterone) showed reductions that were more prolonged following the 90\u00a0mg IM administration compared to 90\u00a0mg SC administration.<\/jats:p>","DOI":"10.1002\/cpdd.1008","type":"journal-article","created":{"date-parts":[[2021,8,27]],"date-time":"2021-08-27T04:26:40Z","timestamp":1630038400000},"page":"257-269","update-policy":"http:\/\/dx.doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":8,"title":["Pharmacokinetic, Safety, and Pharmacodynamic Properties of Teverelix Trifluoroacetate, a Novel Gonadotropin\u2010Releasing Hormone Antagonist, in Healthy Adult Subjects"],"prefix":"10.1002","volume":"11","author":[{"given":"Carol M.","family":"MacLean","sequence":"first","affiliation":[{"name":"Antev Ltd  London 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