Enhertu (trastuzumab deruxtecan; Daiichi Sankyo/AstraZeneca) is an antibody-drug conjugate composed of a monoclonal antibody that targets human epidermal growth factor receptor 2 (HER2), an enzymatically cleavable peptide-linker, and a topoisomerase 1 inhibitor derived from exatecan. The drug-to-antibody ratio of Enhertu is 8:1.
By targeting HER2-expressing cells, Enhertu selectively delivers the topoisomerase 1 inhibitor to cancer cells, reducing systematic exposure to the cytotoxic drug. Once the inhibitor is in the cell, it binds to topoisomerase 1 cleavable complexes and causes cell death through the induction of double-strand DNA breaks and apoptosis. Expression of Trop-1 is associated with poor prognosis of several human cancers, including oral, pancreatic, gastric, ovarian, colorectal, breast, and lung tumors.
4 Drug Overview
5 Product Profiles
5 Enhertu : Breast cancer: triple-negative
LIST OF FIGURES
10 Figure 1: Datamonitor Healthcare’s drug assessment summary of Enhertu for TNBC
10 Figure 2: Datamonitor Healthcare’s drug assessment summary of Enhertu for TNBC
LIST OF TABLES
5 Table 1: Recent high-impact events for Enhertu in TNBC
6 Table 2: Enhertu drug profile
8 Table 3: Late-phase trials of Enhertu for TNBC
9 Table 4: Enhertu for TNBC – SWOT analysis
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