LY-117018

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LY-117018 is a synthetic nonsteroidal estrogen that was developed for potential use in hormone replacement therapy and other estrogen-related treatments. It is a selective estrogen receptor modulator (SERM) and is structurally related to other compounds in its class, such as tamoxifen and raloxifene.

Chemical Structure and Properties

LY-117018 is characterized by its benzofuran structure, which is a common feature among many nonsteroidal estrogens. The compound has a molecular formula of C₁₇H₁₆O₃ and a molecular weight of 268.31 g/mol. Its structure includes a phenyl group and a hydroxyphenyl group, which are important for its activity as an estrogen receptor modulator.

Mechanism of Action

As a selective estrogen receptor modulator, LY-117018 binds to estrogen receptors in various tissues, exerting either estrogenic or anti-estrogenic effects depending on the target tissue. This dual action is similar to other SERMs, which can act as estrogen receptor agonists in some tissues (such as bone) and antagonists in others (such as breast tissue). This property makes LY-117018 a candidate for treating conditions like osteoporosis and breast cancer.

Pharmacokinetics

The pharmacokinetic profile of LY-117018 includes its absorption, distribution, metabolism, and excretion. Like other SERMs, it is expected to be well-absorbed orally, undergo hepatic metabolism, and be excreted primarily in the urine. The specific pharmacokinetic parameters such as half-life, bioavailability, and metabolic pathways are subjects of ongoing research.

Clinical Applications

LY-117018 has been investigated for its potential use in hormone replacement therapy, particularly for postmenopausal women. Its ability to selectively modulate estrogen receptors makes it a promising candidate for reducing the risk of osteoporosis and cardiovascular disease while minimizing the risk of breast and uterine cancers.

Research and Development

Research on LY-117018 is ongoing, with studies focusing on its efficacy and safety profile compared to other SERMs. Preclinical studies have shown promising results, but further clinical trials are necessary to fully understand its therapeutic potential and side effects.

Also see

• Selective estrogen receptor modulator
• Tamoxifen
• Raloxifene
• Hormone replacement therapy
• Estrogen receptor

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