Info

Sacituzumab govitecan

  • Mechanism:
    • Antitrophoblast cell-surface antigen 2 (Trop-2) antibody coupled to topoisomerase 1 inhibitor SN-38;
    • binds to Trop-2 & is internalized so SN-38 can cause DNA damage, apoptosis, & cell death
  • Approved indications:
    • Breast cancer,
    • urothelial cancer
  • Dosing:
    • 10 mg/kg d 1 & 8 of 21-d cycle;
    • slow infusion if infusion rxn occurs;
    • reduce dose for neutropenia & neutropenic fever;
    • hold dose for grade 3-4 diarrhea, reduce dose for grade 3-4 nausea/vomiting
  • PK/PD:
    • T1/2 15.3 h;
    • free SN-38 T1/2 19.7 h
  • AEs:
    • Diarrhea,
    • nausea/vomiting,
    • cytopenia,
    • ↓ Ca,
    • ↓ Na,
    • ↑ LFTs,
    • fatigue
  • DDI: UGT1A1 substrate