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GTx-878
- Development stage
- Discontinued
- Lead developer
- GTx
- Modality
- Small Molecules
01
Overview
GTx-878 (also known as beta-LGND2) is a synthetic, nonsteroidal small molecule that acts as a selective agonist of the estrogen receptor beta (ERbeta). Developed by GTx, Inc., it is an isoquinolinone derivative designed to provide the therapeutic benefits of estrogen receptor activation while minimizing the side effects associated with estrogen receptor alpha (ERalpha) stimulation, such as breast and uterine tissue proliferation. GTx-878 demonstrates approximately 25-fold selectivity for ERbeta over ERalpha, with an EC50 of 2 nM for ERbeta and 52 nM for ERalpha. It was investigated for the treatment of benign prostatic hyperplasia (BPH), prostatitis, and rheumatoid arthritis, though development was ultimately discontinued and the drug was never marketed.
- Other names
- ERbeta-selective ligand 2beta-LGND2beta-LGND-2beta-LGND 2
02
Targets
ESR2 (ERβ)ESR1 (ERα)
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