Drug intelligence / Profile preview

GTx-758

Development stage
Phase 2
Lead developer
GTx
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

GTx-758 (brand name Capesaris) is an orally available, synthetic nonsteroidal small molecule that acts as a selective estrogen receptor alpha (ERα) agonist. It was developed for the treatment of advanced prostate cancer, particularly castration-resistant prostate cancer (CRPC). GTx-758 works by selectively activating ERα, which increases hepatic production of sex hormone-binding globulin (SHBG), thereby reducing free testosterone levels in the blood to castrate levels. This mechanism suppresses androgen-driven tumor growth while potentially avoiding some side effects associated with traditional androgen deprivation therapy such as bone loss and hot flashes. The drug completed phase II clinical trials but development was discontinued after these studies[1][3][7].

Brand names
Capesaris
Other names
938067-78-8UNII-406GR1485ZUNII406GR1485ZUNII 406GR1485ZBenzamide, 3-fluoro-N-(4-fluorophenyl)-4-hydroxy-N-(4-hydroxyphenyl)-406GR1485Z
02

Targets

ESR2 (ERβ)ESR1 (ERα)

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