Pharmacokinetics of Modified Slow-Release Oral Testosterone Over 9 Days in Normal Men With Experimental Hypogonadism

    May 2012 in “ International Journal of Andrology ”
    Ada Lee, Katya B. Rubinow, Richard V. Clark, Ralph B. Caricofe, Mark A. Bush, Hui Zhi, Mara Y. Roth, Stephanie T. Page, William J. Bremner, John K. Amory
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    TLDR The new oral testosterone pill normalized testosterone levels and lowered SHBG in men with low testosterone.
    In 2011, a study involving 12 healthy young men assessed the pharmacokinetics of a novel oral testosterone formulation over 9 days. The men were made hypogonadal using acyline and then given 300 mg of oral testosterone three times daily. Initial serum testosterone levels were under 75 ng/dL, but after treatment, the 24-hour average serum total testosterone decreased from 378 ng/dL on day 1 to 315 ng/dL on day 9, with calculated free testosterone levels remaining similar. SHBG levels significantly dropped from 27 nmol/L to 19 nmol/L, while DHT levels stayed within the reference range, and estradiol was slightly below by day 9. The study concluded that the oral testosterone formulation normalized serum testosterone and significantly suppressed SHBG, indicating potential effectiveness for treating testosterone deficiency.
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