GTx-758
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| Formula | C19H13F2NO3 |
| Molar mass | 341.308226 g/mol |
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GTx-758 (tentative brand name Capesaris) is a synthetic, non-steroidal estrogen that is under development by GTx, Inc. for the treatment of advanced prostate cancer. As of 2016, it has completed two phase II clinical trials.
GTx-758 acts as a selective agonist of the estrogen receptor (ER), with a more than 10-fold preference for activation of ERα relative to ERβ (EC50 = 2.1 and 27 nM, respectively). The selectivity of GTx-758 for ERα over ERβ may confer reduced hypercoagulability and thrombophilia, as estradiol directly produces these effects in platelets via activation of ERβ, which is the predominant isoform of the ER expressed in platelets. It has been said that suppression of free testosterone levels by ERα activation-induced increase in hepatic sex hormone-binding globulin (SHBG) production is the primary mechanism of action of GTx-758 in the treatment of prostate cancer.
In animal studies, GTx-758 reversibly suppresses testosterone concentrations to castrate levels, reduces prostate size and levels of prostate-specific antigen (PSA), but does not induce typical side effects associated with hyperestrogenism (or hypoestrogenism) including hot flashes, bone loss, thrombophilia, hypercoagulation, or increased body fat. Interestingly, unlike diethylstilbestrol, GTx-758 also does not induce gynecomastia in male monkeys, despite similarly suppressing testosterone levels to the castrate range (≤50 ng/dL) and markedly reducing PSA levels.
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