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Importance of measuring testosterone in enzyme-inhibited plasma for oral testosterone undecanoate androgen replacement therapy clinical trials

AIM: Testosterone undecanoate (TU) is metabolized by nonspecific esterases in blood to testosterone (T). Typical clinical practice has been to analyze testosterone in human serum. The degradation of TU to testosterone was evaluated in conditions typically used in clinical studies. METHODS & RESU...

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Detalles Bibliográficos
Autores principales: Lachance, Sylvain, Dhingra, Om, Bernstein, James, Gagnon, Stéphanie, Savard, Caroline, Pelletier, Nathalie, Boudreau, Nadine, Lévesque, Ann
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Future Science Ltd 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5137954/
https://www.ncbi.nlm.nih.gov/pubmed/28031910
http://dx.doi.org/10.4155/fso.15.55
Descripción
Sumario:AIM: Testosterone undecanoate (TU) is metabolized by nonspecific esterases in blood to testosterone (T). Typical clinical practice has been to analyze testosterone in human serum. The degradation of TU to testosterone was evaluated in conditions typically used in clinical studies. METHODS & RESULTS: Freshly collected whole blood was fortified with TU at known concentration. Serum was prepared and T concentration was determined by LC–MS/MS. It was observed that TU degrades extensively to T in human blood under conditions typical of harvesting serum causing overestimation of T concentration of up to 243%. These results were confirmed in a clinical study in which serum and plasma samples were compared. CONCLUSION: It was demonstrated that T must be analyzed in enzyme-inhibited plasma when TU is the administered medication.