elacestrant (Orserdu)

Indications

• ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy

Dosage

• 345 mg PO QD with food

Tabs: 86 mg, 345 mg.

Adverse effects

• common (> 10%)
  • decreased appetite, dyspepsia, nausea, vomiting, diarrhea, constipation
  • abdominal pain, musculoskeletal pain, fatigue, headache, hot flush
  • increased serum cholesterol, increased serum triglycerides
  • increased serum ALT, increased serum AST, increased serum creatinine
  • decreased blood hemoglobin, decreased serum sodium

Drug interactions

• strong & moderate CYP3A4 inducers
• strong & moderate CYP3A4 inhibitors

Mechanism of action

• estrogen receptor antagonist
  • binds to estrogen receptor-alpha
• antineoplastic activity in ER+ HER2- breast cancer resistant to fulvestrant & cyclin-dependent kinase 4/6 inhibitors & in cancers harboring estrogen receptor 1 gene (ESR1) mutations

More general terms

• antineoplastic endocrine agent
• estrogen antagonist

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=23642301
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=67479909
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=101364838
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=127020970