In the treatment of breast diseases, the emergence of Elacestrant is of great significance. As an oral SERD, it is able to directly degrade estrogen receptors, thereby inhibiting the growth of diseased cells. This innovative drug brings good news to patients with ER, HER2- and breast diseases with ESR1 mutations. So, how effective is Elacestrant?
How effective is Elacestrant?
Elacestrant has shown significant efficacy in the treatment of estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, ESR1-mutated advanced or metastatic breast disease. The following is a detailed analysis of the effects of Elacestrant:
1.Clinical trial evidence
The EMERALD Phase III trial included 478 patients with ER/HER2- metastatic breast disease, of whom 228 had ESR1 mutations. The results of the trial showed that Elacestrant significantly extended the progression-free survival (PFS) of patients, particularly in patients with ESR1 mutations, with a median PFS of 3.8 months in the Elacestrant group compared to 1.9 months in the control group, and a 45% reduction in the risk of disease progression or death.
2. Efficacy characteristics
ErElacestrantt was effective in prolonging progression-free survival in patients with mutant advanced breast disease, with progression-free survival of up to 8.61 months in patients with pre-cyclin-dependent kinase (CDK4/6) inhibitors for more than 12 months.
Elacestrant has shown significant efficacy and good tolerability in the treatment of advanced or metastatic breast disease with ER/HER2-, ESR1 mutations. However, specific efficacy may vary from person to person, and patients should consult a medical professional and follow their doctor's advice before use.
What is the mechanism of action of Elacestrant?
The mechanism of action of Elacestrant(Orserdu) is mainly related to the binding and degradation process with the estrogen receptor (ER). Here's a closer look at its mechanism of action:
1.Conjugated estrogen receptors
Elacestrant is an oral, selective estrogen receptor degrader(SERD) whose structural features allow it to bind specifically to estrogen receptors. This combination is the first step in the therapeutic action of Elacestrant.
2.Promote estrogen receptor degradation
Binding of Elacestrant to estrogen receptors triggers a conformational change in the receptor, which in turn induces its internalization and subsequent proteasome-mediated degradation. This process effectively lowers the levels of estrogen receptors within cells, thereby blocking the estrogen signaling pathway.
Through its unique mechanism of action, Elacestrant has shown obvious therapeutic effects in the treatment of breast diseases, bringing new treatment options to patients with breast diseases.
