Erteberel: Difference between revisions

Erteberel
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Latest revision as of 10:58, 23 March 2025

Selective estrogen receptor modulator

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[edit]

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[edit]

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[edit]

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[edit]

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[edit]

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[edit]

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-'''Erteberel''' (also known as LY500307) is a selective [[Estrogen receptor beta|estrogen receptor beta]] agonist that has been under investigation for its potential therapeutic applications. The development of Erteberel was driven by the hypothesis that selective activation of estrogen receptor beta could offer beneficial effects in conditions such as [[Menopause|menopausal symptoms]], [[Prostate cancer|prostate cancer]], and possibly [[Cardiovascular disease|cardiovascular diseases]], without the adverse effects associated with estrogen therapy that activates both estrogen receptor alpha and beta.
+{{Short description|Selective estrogen receptor modulator}}
+{{Drugbox
+| verifiedfields = changed
+| verifiedrevid = 477002123
+| IUPAC_name = (2S)-2-(4-Hydroxyphenyl)-3-methyl-1-[4-(2-pyrrolidin-1-ylethoxy)phenyl]butan-1-one
+| image = Erteberel_skeletal.svg
+| image2 =
+}}
+'''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 exerts its effects by selectively binding to and activating the estrogen receptor beta (ERβ). The [[Estrogen receptor|estrogen receptors]] (ERα and ERβ) are nuclear hormone receptors that, upon activation by their ligands, can modulate the expression of genes involved in a wide range of biological processes. By selectively targeting ERβ, Erteberel aims to harness the beneficial effects of estrogen signaling in tissues where ERβ is predominantly expressed, while minimizing stimulation of ERα, which has been associated with the proliferative effects of estrogens in tissues such as the breast and uterus.
+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.
-==Clinical Development==
+==Potential Therapeutic Uses==
-The clinical development of Erteberel has included studies exploring its efficacy and safety in various conditions. In the context of menopausal symptoms, research has focused on its potential to alleviate hot flashes and improve bone density without the risks associated with traditional hormone replacement therapy. In prostate cancer, the rationale for investigating Erteberel is based on the role of ERβ in inhibiting the proliferation of prostate cancer cells. Despite these promising applications, the development of Erteberel has faced challenges, and as of the last available information, it has not received approval for clinical use.
+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.
-==Potential Therapeutic Applications==
+===Other Investigated Uses===
-===Menopausal Symptoms===
+In addition to BPH, erteberel has been studied for its potential effects on other conditions, such as:
-Erteberel has been studied for its potential to relieve menopausal symptoms, such as hot flashes and osteoporosis, by mimicking the beneficial effects of estrogens in a more targeted manner.
+* [[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.
-===Prostate Cancer===
+==Development and Research==
-Given the anti-proliferative effects of ERβ activation on prostate cancer cells, Erteberel has been explored as a potential therapeutic agent in the treatment of prostate cancer.
+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.
-===Cardiovascular Disease===
+==Chemical Structure==
-There is also interest in the potential of Erteberel to confer cardiovascular benefits, based on the protective roles that estrogen and ERβ activation have been shown to play in cardiovascular health.
+[[File:Erteberel_skeletal.svg|Chemical structure of Erteberel|thumb|right]]
+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.
-==Safety and Efficacy==
+==Related Pages==
-The safety and efficacy of Erteberel for any indication have yet to be conclusively established. Clinical trials are necessary to determine its therapeutic potential and to fully understand its safety profile, especially in long-term use.
+* [[Selective estrogen receptor modulator]]
+* [[Estrogen receptor beta]]
-==Conclusion==
+* [[Benign prostatic hyperplasia]]
-Erteberel represents a novel approach to estrogen receptor modulation, with the potential to offer therapeutic benefits in conditions traditionally treated with estrogen therapy, but with a potentially improved safety profile. Ongoing research and clinical trials will be crucial in determining its place in future therapeutic strategies.
+* [[Eli Lilly and Company]]
 [[Category:Selective estrogen receptor modulators]]
-[[Category:Investigational drugs]]
+[[Category:Experimental drugs]]
+[[Category:Estrogens]]
-{{Pharmacology-stub}}
-{{Medicine-stub}}