Английская Википедия:EC586
Шаблон:Short description Шаблон:Drugbox
EC586, also known as testosterone 17β-(1-((5-(aminosulfonyl)-2-pyridinyl)carbonyl)-Шаблон:Small-proline), is an androgen and anabolic steroid which is under development by Evestra for use in androgen replacement therapy in men.[1][2] It is an orally active androgen ester – specifically, a C17β sulfonamide–proline ester of the natural and bioidentical androgen testosterone – and acts as a prodrug of testosterone in the body.[2] However, unlike oral testosterone and conventional oral testosterone esters such as testosterone undecanoate, EC586 has high oral potency, may undergo little or no first-pass metabolism, and may not have disproportionate androgenic effects in the liver.[2][3] As such, it may have a variety of desirable advantages over oral testosterone, similarly to parenteral testosterone, but with the convenience of oral administration.[2][3] Evestra intends to seek Investigational New Drug status for EC586 in the fourth quarter of 2018.Шаблон:Update inline[1]
The pharmacokinetics of oral EC586 have been briefly assessed in rats in a small pilot study.[2] Oral EC586 showed area-under-the-curve (AUC) levels that were more than 100-fold greater than those of oral testosterone propionate, the C17β propionate ester of testosterone (AUC0-3h = 330 ng/mL and 2.5 ng/mL, respectively, for doses of 3.0 mg/rat each).[2] As such, EC586 would appear to possess strongly increased oral bioavailability, potency, and systemic exposure relative to testosterone propionate.[2] Additional research and details on the pharmacokinetics and properties of EC586 are to be published "soon".[2]
The mechanism for the absence of first-pass metabolism and lack of disproportionate liver exposure with oral administration has been elucidated for a closely related sulfonamide–proline estradiol ester known as EC508, which shows the same properties as EC586.[2][3]
Clinical trials for EC586 and EC508 are undergoing as of 2023.[4]
See also
- List of androgen esters § Testosterone esters
- List of investigational sex-hormonal agents § Androgenics
References
External links
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