Elacestrant dihydrochloride
[CAS# 1349723-93-8]

Identification

• Classification: API >> Antineoplastic agents
• Name: Elacestrant dihydrochloride
• Synonyms: (6R)-6-[2-[Ethyl[[4-[2-(ethylamino)ethyl]phenyl]methyl]amino]-4-methoxyphenyl]-5,6,7,8-tetrahydro-2-naphthalenol hydrochloride (1:2); Elacestrant hydrochloride; RAD 901 dihydrochloride
• Molecular Formula: C₃₀H₃₈N₂O₂ ^.₂ClH
• Molecular Weight: 531.56
• CAS Registry Number: 1349723-93-8
• SMILES: N(CC1=CC=C(CCNCC)C=C1)(CC)C2=C(C=CC(OC)=C2)[C@H]3CC=4C(CC3)=CC(O)=CC4.Cl

Safety Data

• Hazard Symbols: GHS07 Warning
• Hazard Statements: H315-H319-H335
• Precautionary Statements: P261-P305+351+338-P302+352

Discovory and Applicatios

Elacestrant dihydrochloride is a selective estrogen receptor degrader (SERD) that has emerged as a promising therapeutic agent in the treatment of estrogen receptor-positive (ER+) breast cancer, particularly in cases that are resistant to traditional endocrine therapies. ER+ breast cancer is a subtype of breast cancer that expresses estrogen receptors on its surface, which promote cancer cell growth in the presence of estrogen. Traditional therapies often involve endocrine agents that block estrogen or reduce its levels, but many patients eventually develop resistance to these treatments. Elacestrant dihydrochloride works by binding to the estrogen receptor, leading to its degradation and reducing the receptor's activity, thereby inhibiting cancer cell growth.

The discovery of Elacestrant dihydrochloride was part of the ongoing search for more effective treatments for breast cancer, particularly for patients with advanced or metastatic disease who no longer respond to conventional endocrine therapies. SERDs represent a novel class of drugs that target the estrogen receptor in a way that conventional selective estrogen receptor modulators (SERMs), such as tamoxifen, do not. Unlike SERMs, which block the estrogen receptor's activity, SERDs degrade the receptor itself, offering a potentially more potent and irreversible solution to estrogen-driven breast cancer. Elacestrant dihydrochloride was identified as a promising candidate due to its ability to degrade the estrogen receptor in both ER+ breast cancer cells and in tumors that have developed resistance to other therapies.

In clinical trials, Elacestrant dihydrochloride has demonstrated efficacy in patients with ER+ breast cancer who have developed resistance to aromatase inhibitors or tamoxifen. These patients often have tumors with mutations in the estrogen receptor that prevent the effectiveness of conventional treatments. Elacestrant has shown activity against these mutant forms of the receptor, offering a new line of treatment for patients who previously had limited options. Clinical studies have demonstrated that Elacestrant dihydrochloride can lead to significant tumor regression and improvements in progression-free survival, with a manageable side effect profile.

Elacestrant dihydrochloride is administered orally, making it a convenient option for patients, especially when compared to traditional chemotherapy or intravenous treatments. Its oral bioavailability and manageable side effects contribute to its appeal as a treatment for ER+ breast cancer. Furthermore, the ability of Elacestrant to address drug resistance mechanisms in cancer cells positions it as an important drug in the evolving landscape of breast cancer treatment.

Beyond its use in breast cancer, there is potential for Elacestrant dihydrochloride to be applied in other estrogen receptor-driven cancers, though ongoing research is necessary to explore these possibilities. Additionally, the success of Elacestrant dihydrochloride has spurred further interest in the development of other SERDs that may target different mutations or provide alternative mechanisms of action against resistant tumors.

Elacestrant dihydrochloride represents a significant advancement in the treatment of ER+ breast cancer, particularly for patients who face resistance to existing therapies. Its mechanism of action and clinical effectiveness highlight the potential of SERDs to address some of the most challenging aspects of cancer treatment. As research continues, Elacestrant and similar compounds could play a crucial role in improving outcomes for patients with resistant forms of breast cancer.