Info

🌱 來自: Antibody Drug Conjugates

trastuzumab deruxtecan

• Mechanism:
  • HER2-targeted antibody-drug conjugated to a topoisomerase I inhibitor (DXd, an exatecan derivative)
• Approved indications:
  • Breast cancer, gastric cancer
• Dosing:
  • Breast cancer (unresectable/metastatic):
    • 5.4 mg/kg q3wks;
  • gastric cancer (locally advanced/metastatic): 6.4 mg/kg q3wks;
  • adjust for neutropenia, neutropenic fever, thrombocytopenia, cardiotoxicity, infusion rxns, pulmonary toxicity;
  • 1st-dose reduction breast 4.4 mg/kg, gastric 5.4 mg/kg,
  • 2nd-dose reduction breast 3.2 mg/kg, gastric 4.4 mg/kg
• PK/PD: T1/2 ∼5-6 d
• AEs:
  • Hepatotoxicity,
  • ↓ LVEF,
  • pancytopenia,
  • GI tox,
  • ILD,
  • ↓ K,
  • alopecia,
  • ↑ LFT,
  • ↑ Tbili,
  • fatigue,
  • headache
• DDI: Minor CYP3A4 substrate, P-gp substrate