Erteberel

Selective estrogen receptor modulator

Erteberel
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Erteberel (developmental code name LY-500307) is a selective estrogen receptor modulator (SERM) that was under development by Eli Lilly and Company for the treatment of benign prostatic hyperplasia (BPH) and other conditions. It is a nonsteroidal compound that acts as a selective agonist of the estrogen receptor beta (ERβ), with high selectivity over the estrogen receptor alpha (ERα).

Mechanism of Action

Erteberel functions by selectively binding to and activating the estrogen receptor beta (ERβ). This receptor is one of the two main types of estrogen receptors, the other being estrogen receptor alpha (ERα). The selective activation of ERβ is thought to provide therapeutic benefits in certain conditions without the side effects associated with ERα activation. This selectivity is particularly important in tissues where ERβ is predominantly expressed, such as the prostate gland.

Potential Therapeutic Uses

Erteberel was primarily investigated for its potential use in treating benign prostatic hyperplasia (BPH), a condition characterized by the enlargement of the prostate gland. By selectively targeting ERβ, erteberel was hypothesized to reduce prostate size and alleviate symptoms associated with BPH without affecting other tissues where ERα is more prevalent.

Other Investigated Uses

In addition to BPH, erteberel has been studied for its potential effects on other conditions, such as:

• Osteoporosis: Due to its estrogenic effects on bone tissue, erteberel may help in maintaining bone density.
• Cognitive disorders: There is interest in the role of ERβ in the brain, suggesting potential benefits in cognitive health.

Development and Research

Erteberel was developed by Eli Lilly and Company, a major pharmaceutical company. Despite its promising mechanism of action, the development of erteberel was eventually discontinued. The reasons for discontinuation are not publicly detailed, but it is common for drug development to be halted due to various factors such as efficacy, safety, or strategic business decisions.

Chemical Structure

Chemical structure of Erteberel

Erteberel is a nonsteroidal compound with a complex chemical structure that allows it to selectively bind to ERβ. Its chemical name is (2S)-2-(4-Hydroxyphenyl)-3-methyl-1-[4-(2-pyrrolidin-1-ylethoxy)phenyl]butan-1-one.

Related Pages

• Selective estrogen receptor modulator
• Estrogen receptor beta
• Benign prostatic hyperplasia
• Eli Lilly and Company