Testosterone 17β-(1-((5-(aminosulfonyl)-2-pyridinyl)carbonyl)-L-proline)
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Testosterone 17β-(1-((5-(aminosulfonyl)-2-pyridinyl)carbonyl)-L-proline)
EC586, also known as testosterone 17β-(1-((5-(aminosulfonyl)-2-pyridinyl)carbonyl)--proline), is an androgen and anabolic steroid which is under development by Evestra for use in androgen replacement therapy in men. 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. 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. As such, it may have a variety of desirable advantages over oral testosterone, similarly to parenteral testosterone, but with the convenience of oral administration. Evestra intends to seek Investigational New Drug status for EC586 in the fourth quarter of 2018. Relative to parenteral routes of testosterone like ...
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Androgen
An androgen (from Greek ''andr-'', the stem of the word meaning "man") is any natural or synthetic steroid hormone that regulates the development and maintenance of male characteristics in vertebrates by binding to androgen receptors. This includes the embryological development of the primary male sex organs, and the development of male secondary sex characteristics at puberty. Androgens are synthesized in the testes, the ovaries, and the adrenal glands. Androgens increase in both males and females during puberty. The major androgen in males is testosterone. Dihydrotestosterone (DHT) and androstenedione are of equal importance in male development. DHT ''in utero'' causes differentiation of the penis, scrotum and prostate. In adulthood, DHT contributes to balding, prostate growth, and sebaceous gland activity. Although androgens are commonly thought of only as male sex hormones, females also have them, but at lower levels: they function in libido and sexual arousal. Also, an ...
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Anabolic Steroid
Anabolic steroids, also known more properly as anabolic–androgenic steroids (AAS), are steroidal androgens that include natural androgens like testosterone (medication), testosterone as well as synthetic androgens that are structurally related and have similar effects to testosterone. They increase protein within cell (biology), cells, especially in skeletal muscles, and also have varying degrees of virilization, virilizing effects, including induction of the development and maintenance of male, masculine secondary sexual characteristics such as the growth of facial hair, facial and body hair. The word ''anabolic'', referring to anabolism, comes from the Greek ἀναβολή ''anabole'', "that which is thrown up, mound". Androgens or AAS are one of three types of sex hormone agonists, the others being estrogen (medication), estrogens like estradiol (medication), estradiol and progestogens like progesterone (medication), progesterone. AAS were synthesized in the 1930s, and are ...
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Androgen Ester
An androgen or anabolic steroid ester is an ester of an androgen/anabolic steroid (AAS) such as the natural testosterone or dihydrotestosterone (DHT) or the synthetic nandrolone (19-nortestosterone). Esterification renders AAS into metabolism-resistant prohormones of themselves, improving oral bioavailability, increasing lipophilicity, and extending the elimination half-life (which necessitates less frequent administration). In addition, with intramuscular injection, AAS esters are absorbed more slowly into the body, further improving the elimination half-life. Aside from differences in pharmacokinetics (e.g., duration), these esters essentially have the same effects as the parent drugs. They are used in androgen replacement therapy (ART), among other indications. Examples of androgen esters include testosterone esters such as testosterone cypionate, testosterone enanthate, testosterone propionate, and testosterone undecanoate and nandrolone esters such as nandrolone decanoate and ...
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