Trojan horse image

Mechanism of Action

THE FIRST TROP-2-DIRECTED ADC: TRODELVY DELIVERS A POTENT TOPOISOMERASE 1 INHIBITOR TO mUC TUMORS1

Trop-2 is a surface protein frequently expressed by many cancers, including locally advanced or mUC tumors2

Trop-2 biomarker testing is not required for use with TRODELVY

TRODELVY binds to the antigen Trop-2 and delivers and concentrates a potent cytotoxic into tumor tissue2

The proposed mechanism of action is based on preclinical data, which may not correlate with clinical outcomes.

TRODELVY® (sacituzumab govitecan-hziy) mechanism of action graphic
 

Humanized monoclonal antibody1

Binds to Trop-2, the trophoblast cell-surface antigen-2
 

Hydrolysable linker1

  • Links the humanized monoclonal antibody to SN-38
  • Hydrolysis of the linker releases SN-38 to kill tumor cells
 

Cytotoxic1

The payload of TRODELVY is SN-38, a topoisomerase inhibitor that prevents repair of DNA damage and leads to apoptosis and cell death

TRODELVY has a high drug-to-antibody ratio, with an average of 7 to 8 molecules of SN-38 per antibody molecule.1

 
  • ADCs use a monoclonal antibody to deliver an attached cytotoxic drug into tumors3
  • Based on pharmacologic data, once inside the tumor, the linker connecting the antibody to the cytotoxic is cleaved, releasing the active drug1,3

ADC=antibody-drug conjugate; mUC=metastatic urothelial cancer.

References: 1. TRODELVY [package insert]. Foster City, CA: Gilead Sciences, Inc.; April 2021. 2. Goldenberg D, Cardillo TM, Govindan S, et al. Trop-2 is a novel target for solid cancer therapy with sacituzumab govitecan (IMMU-132), an antibody-drug conjugate (ADC). Oncotarget. 2015;6(26):22496-22512. 3. Peters C, Brown S. Antibody-drug conjugates as novel anti-cancer chemotherapeutics. Biosci Rep. 2015;35(4):1-20.