The review of chemistry, pharmacological properties and bio-analytical methods of oral selective estrogen receptor degrader: Elacestrant Vyas Amitkumar J., Ramani Anjali*, Patel Ajay I. B. K. Mody Government Pharmacy College, Rajkot, Gujarat, India *Corresponding Author E-mail: apatel11287@gmail.com
Online published on 23 May, 2025. Abstract The second most common cancer among women, after lung cancer, is breast cancer. The main form of treatment for the most prevalent subtype of breast cancer, hormone receptor (HR) positive, HER2 negative breast cancer, is endocrine therapy. Although there are various endocrine treatment medications available, virtually all metastatic HR-positive breast tumors will develop drug resistance to them. An essential method of resistance to aromatase drugs is represented by ESR1 mutations. As a potential therapy for ER+ breast cancer, Elacestrant is a new, non-steroidal, selective estrogen receptor degrader with complicated dose-related ER agonist/antagonist action. A brand-new oral selective estrogen receptor degrader (SERD), Elacestrant targets the estrogen receptor specifically on breast cancer cells to stop tumor growth. In patients with HR-positive, HER2-negative metastatic breast cancer, elacestrant showed a significant, albeit moderate, improvement in median progression-free survival (PFS) compared to standard of care endocrine therapy. Importantly, individuals with ESR1 mutations also benefited significantly, which prompted the FDA to approve Elacestrant for use in this patient population. Upper gastrointestinal symptoms were the most common side effects of Elacestrant, which was generally well tolerated. There are numerous current clinical trials assessing the effectiveness of Elacestrant in the treatment of metastatic breast cancer, both alone and in combination with other targeted therapies. The review will provide necessary details regarding Elacestrant. Top Keywords Breast cancer, Elacestrant, Endocrine therapy, ESR1 mutation, Estrogen receptor (ER)-positive, Selective Estrogen Receptor Degrader (SERD). Top |