Guidance on the use of oral testosterone undecanoate: background, clinical considerations, and best practices

Le résumé fourni par la source

The effective use of oral testosterone therapy has long been hindered by first-pass hepatic metabolism, which renders unmodified oral testosterone largely inactive. Early attempts to overcome this involved 17α-methyltestosterone, a formulation that prevented degradation by the liver but carried a significant risk of hepatotoxicity, particularly with chronic use or high doses. Testosterone undecanoate (TU), developed in the 1970s, provided a solution by utilizing lymphatic absorption to bypass hepatic metabolism. The Andriol formulation was the first to use a lipid-based vehicle to promote gut lymphatic uptake. Despite validating the approach, Andriol faced clinical challenges, including variable serum levels, the need for frequent dosing 3-4 times per day, a short shelf life and the need to be taken with a high fat meal. Newer oral TU formulations—Jatenzo (2019), Tlando (2022), and Kyzatrex (2022)—have addressed these limitations by using distinct lipid excipients to enhance the pharmacokinetic profile of the drugs, leading to improved bioavailability and dosing convenience. These formulations differ in their oil vehicles—Jatenzo’s principal oil is seed based, while Tlando and Kyzatrex utilize glyceryl and propylene glycol, respectively.

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