Sacituzumab govitecan: antibody-drug conjugate in triple-negative breast cancer and other solid tumors

Drugs Today (Barc). 2019 Sep;55(9):575-585. doi: 10.1358/dot.2019.55.9.3039669.

Abstract

Patients with metastatic triple-negative breast cancer (mTNBC) that has progressed on first-line therapy have a poor prognosis with limited therapeutic options. Sacituzumab govitecan (SG) is a novel antibody-drug conjugate (ADC) that has shown promising efficacy in mTNBC. SG is comprised of SN-38, the active metabolite of irinotecan, conjugated via a hydrolyzable linker to the humanized RS7 antibody targeting trophoblast cell surface antigen 2 (Trop-2), a glycoprotein that is expressed at high levels in many epithelial solid tumors. It has received breakthrough therapy status by the U.S. Food and Drug Administration (FDA) for the treatment of patients with pretreated mTNBC. In this review, we summarize available data regarding the pharmacology, pharmacokinetics, safety and efficacy of SG and describe ongoing and future clinical studies investigating this agent.

Keywords: Antibody-drug conjugates; IMMU-132; Inhibitors of Trop-2; Metastatic triple-negative breast cancer; Sacituzumab govitecan; Treatment of solid tumors.

Publication types

  • Review

MeSH terms

  • Antibodies, Monoclonal, Humanized / therapeutic use*
  • Antigens, Neoplasm
  • Camptothecin / analogs & derivatives*
  • Camptothecin / therapeutic use
  • Cell Adhesion Molecules
  • Female
  • Humans
  • Immunoconjugates / therapeutic use*
  • Triple Negative Breast Neoplasms / drug therapy*
  • United States
  • United States Food and Drug Administration

Substances

  • Antibodies, Monoclonal, Humanized
  • Antigens, Neoplasm
  • Cell Adhesion Molecules
  • Immunoconjugates
  • TACSTD2 protein, human
  • sacituzumab govitecan
  • Camptothecin