ArticleEuropean journal of drug metabolism and pharmacokinetics2026
Clinical Pharmacokinetics, Mass Balance and Metabolism of Fezolinetant in Postmenopausal Women.
Article in European journal of drug metabolism and pharmacokinetics, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
backgroundFezolinetant is a non-hormonal selective neurokinin-3 receptor antagonist for the treatment of moderate to severe vasomotor symptoms associated with menopause. The objective of this study was to characterize the pharmacokinetics, mass balance, and metabolism of fezolinetant in postmenopausal women.
methodsA single dose of 180 mg
resultsFollowing a single administration of
conclusionThis study successfully characterized the overall pathways of metabolism and excretion of fezolinetant, identified the circulating metabolites, and provided key data to support the development of fezolinetant. Fezolinetant is mainly metabolized to yield ES259564, and primarily excreted into urine as ES259564. In plasma, only fezolinetant and ES259564 were detected, accounting for approximately 81% of total radioactivity, indicating that the majority of circulating drug-related material was quantitatively characterized, with the remaining radioactivity attributable to multiple low-abundance components below the threshold for a major circulating metabolite. TRIAL REGISTRATION NUMBER: EudraCT Number 2017-004911-38.
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