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Anticancer Drugs Medicine Oncology Pharmacology Physiotherapy Sacituzumab govitecan-hziy

Sacituzumab govitecan-hziy (Mechanism of Action)

In this article we will discuss Sacituzumab govitecan-hziy
(Mechanism of Action)

In this article, we will discuss Sacituzumab govitecan-hziy (Mechanism of Action). So, let’s get started.

Mechanism of Action

Sacituzumab govitecan-hziy is a Trop-2-directed antibody-drug conjugate. Sacituzumab is a humanized antibody that
recognizes Trop-2. The small molecule, SN-38, is a topoisomerase I inhibitor, which is covalently attached to the antibody
by a linker. Pharmacology data suggest that sacituzumab govitecan-hziy binds to Trop-2-expressing cancer cells and is
internalized with the subsequent release of SN-38 via hydrolysis of the linker. SN-38 interacts with topoisomerase I and
prevents re-ligation of topoisomerase I-induced single strand breaks. The resulting DNA damage leads to apoptosis and
cell death. Sacituzumab govitecan-hziy decreased tumor growth in mouse xenograft models of triple-negative breast
cancer.

Pharmacodynamics

The Sacituzumab govitecan-hziy exposure-response relationships and pharmacodynamic time course for efficacy have not been fully characterized.

Cardiac electrophysiology
The maximum mean change from baseline was 9.7 msec (the upper bound of the two-sided 90% confidence interval is 16.8 msec) at the recommended dose. A positive exposure-response relationship was observed between QTc increases and SN-38 concentrations.

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