Highly potent payload is an exatecan derivative, known as DXd, with a short systemic half-life 1,3; Upon release, membrane-permeable payload causes DNA damage and cell death, resulting in destruction of targeted tumor cells and neighboring cells present in the tumor microenvironment, known as the bystander antitumor effect 1,3,4

2025年1月28日 · ENHERTU is a HER2-directed antibody and topoisomerase inhibitor conjugate indicated for the treatment of: adult patients with unresectable or metastatic HER2-positive (IHC 3+ or ISH positive) breast cancer who have received a prior anti-HER2-based regimen either: in the metastatic setting, or

Trastuzumab deruxtecan, sold under the brand name Enhertu, is an antibody-drug conjugate consisting of the humanized monoclonal antibody trastuzumab (Herceptin) covalently linked to the topoisomerase I inhibitor deruxtecan (a derivative of exatecan).

Indicated for unresectable or metastatic HER2-positive (IHC 3+ or ISH positive) breast cancer in adults who received prior anti-HER2-based regimen in the metastatic setting OR neoadjuvant or...

ENHERTU is indicated for the treatment of adult patients with unresectable or metastatic HER2-low (IHC 1+ or IHC 2+/ISH-) breast cancer who have received a prior chemotherapy in the metastatic...

Trastuzumab deruxtecan is a HER2 directed antibody-drug conjugate (ADC). The humanized IgG1 monoclonal antibody (trastuzumab) is linked to DXd (topoisomerase I inhibitor) by a tetrapeptide-based cleavable linker. Following binding to HER2 receptors on tumour cells, trastuzumab deruxtecan is internalized and DXd is released intracellularly.

2024年12月3日 · In cycle 3, the apparent elimination half-life (t 1/2) of trastuzumab deruxtecan and released DXd was approximately 7 days. Moderate accumulation (approximately 35% in cycle 3 compared to cycle 1) of trastuzumab deruxtecan was observed.

2019年5月20日 · Half-life. In a pharmacokinetic study, the median elimination half-life of trastuzumab deruxtecan was about 5.8 days. 6. Clearance. Trastuzumab deruxtecan is rapidly cleared from systemic circulation. 2 Estimated systemic clearance of trastuzumab deruxtecan is 0.42 L/day, according to a population pharmacokinetic analysis.

Enhertu™ trastuzumab deruxtecan is a HER2 targeted antibody drug conjugate (ADC). It contains a humanized anti-HER2 IgG1 monoclonal antibody (trastuzumab) attached to the cytotoxic component, a topoisomerase I inhibitor (DXd), by a cleavable tetrapeptide based linker. Deruxtecan is composed of the linker and the topoisomerase I inhibitor.

ENHERTU is a HER2-directed antibody and topoisomerase inhibitor conjugate indicated for the treatment of adult patients with unresectable or metastatic HER2-positive breast cancer who have received two or more prior anti-HER2-based regimens