Sacituzumab govitecan, sold under the brand name Trodelvy, is an antibody drug conjugate that combines a humanized antibody targeting the Trop-2 protein with SN-38, a topoisomerase inhibitor. It is used to treat metastatic triple negative breast cancer, hormone receptor positive HER2 negative breast cancer, and metastatic urothelial cancer. The drug received United States approval in April 2020 and European Union approval in November 2021, and was recognized by both regulators as a first in class medication. Common side effects include nausea, low neutrophil counts, diarrhea, and fatigue, with boxed warnings for severe neutropenia and diarrhea.
Facts
Drug ClassTrop-2 directed antibody-drug conjugate with a topoisomerase inhibitor payload 1 Mechanism of ActionAnti-Trop-2 antibody conjugated to SN-38, the active metabolite of irinotecan 1 Approved UseTreats metastatic triple negative breast cancer, HR-positive HER2-negative breast cancer and metastatic urothelial cancer 1 First Approved / Isolated Year Significant RiskBoxed warning for severe neutropenia and severe diarrhea 1 Classification
Approval Status ATC ClassSourced to the subject's own accountL: Antineoplastic and Immunomodulating Agents 2 Route of Administration Connections
Sources
1. Sacituzumab govitecan (Wikipedia)
Lead section
Sacituzumab govitecan, sold under the brand name Trodelvy by Gilead Sciences, is a Trop-2-directed antibody and topoisomerase inhibitor drug conjugate used for the treatment of metastatic triple-negative breast cancer, previously treated metastatic hormone receptor-positive, HER2-negative breast cancer, and metastatic urothelial cancer.
Mechanism section
Sacituzumab govitecan is a conjugate of the humanized anti-Trop-2 monoclonal antibody linked with SN-38, the active metabolite of irinotecan.
History section
approved for medical use in the United States in April 2020
Lead section, paragraph 2
has a boxed warning about the risk of severe neutropenia
Lead section [significant-risk]
Sacituzumab govitecan has a boxed warning about the risk of severe neutropenia (abnormally low levels of white blood cells) and severe diarrhea.
Lead section, approval-status statement
Sacituzumab govitecan was approved for medical use in the United States in April 2020, and in the European Union in November 2021.
View the Source2. Anatomical Therapeutic Chemical Classification System (Wikipedia)
WikipediaFirst-level anatomical group codes, Code LQuote, First-level anatomical group codes, Code L
Antineoplastic and immunomodulating agents
3. Sacituzumab govitecan (Wikipedia)
WikipediaInfobox drug, routes_of_administrationQuote, Infobox drug, routes_of_administration
Intravenous
Frequently Asked Questions
What is SN-38 and how does sacituzumab govitecan deliver it?
SN-38 is irinotecan's active metabolite, carried as the drug's payload by an antibody that targets the Trop-2 protein.
SN-38 is the active metabolite of the chemotherapy drug irinotecan. In sacituzumab govitecan it serves as the topoisomerase inhibitor payload, chemically linked to a humanized antibody that targets the Trop-2 protein. This antibody drug conjugate design carries SN-38 to Trop-2 expressing cells rather than delivering it as a standalone chemotherapy agent.
Reader Challenges (0)
No disputes yet. Spotted an error or a better source? Open the first one.
Sign in to dispute this or suggest a correction.