Trastuzumab Deruxtecan drug aliquots can be used for in vitro or in vivo experiments. Several other reference drugs are also available.
The drug aliquots are generated by aliquoting (dividing and repackaging) the EU-licensed biosimilar drug.
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Up to 10 batches of original drugs for examining batch-to-batch variations
Up to 80% less compared to the original pharmaceutical price
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Up to 80% less compared to the original pharmaceutical price
| Drug name | Enhertu® |
| INN | Trastuzumab Deruxtecan |
| API type | Antibody-drug conjugate (ADC) |
| Pharmacotherapeutic group | Antineoplastic agents, HER2 (Human Epidermal Growth Factor Receptor 2) inhibitors |
| ATC code | L01FD04 |
| Target of antibody | HER2 |
| General function | |
| Short description | Trastuzumab Deruxtecan is an antibody-drug conjugate (ADC) that contains a humanised anti-HER2 IgG1 monoclonal antibody (mAb) with the same amino acid sequence as trastuzumab, produced by mammalian (Chinese Hamster Ovary) cells, covalently linked to DXd, an exatecan derivative and a topoisomerase I inhibitor, via a tetrapeptide-based cleavable linker. Approximately 8 molecules of deruxtecan are attached to each antibody molecule. |
| Pharmacodynamic properties (Mechanism of action; Source EMA document) | Trastuzumab Deruxtecan, is a HER2-targeted antibody-drug conjugate. The antibody is a humanised anti-HER2 IgG1 attached to Deruxtecan, a topoisomerase I inhibitor (DXd) bound by a tetrapeptide-based cleavable linker. The antibody-drug conjugate is stable in plasma. The function of the antibody portion is to bind to HER2 expressed on the surface of certain tumour cells. After binding, the trastuzumab deruxtecan complex then undergoes internalisation and intracellular linker cleavage by lysosomal enzymes that are upregulated in cancer cells. Upon release, the membrane-permeable DXd causes DNA damage and apoptotic cell death. DXd, an exatecan derivative, is approximately 10 times more potent than SN-38, the active metabolite of irinotecan. |
| Pharmacodynamic properties (Pharmacodynamic effects; Source EMA document) | Trastuzumab Deruxtecan undergoes intracellular cleavage by lysosomal enzymes to release the DXd. The humanised HER2 IgG1 monoclonal antibody is expected to be degraded into small peptides and amino-acids via catabolic pathways in the same manner as endogenous IgG. In vitro metabolism studies in the human liver, microsomes indicate that DXd is metabolised mainly by CYP3A4 via oxidative pathways. |
| Original license holder | Daiichi Sankyo Europe GmbH Zielstattstrasse 48 81379 Munich Germany |
| Marketing authorisation numbers | EU/1/20/1508/001 |
| Marketing authorisation holder | Daiichi Sankyo Europe GmbH Zielstattstrasse 48 81379 Munich Germany |
| Name of the manufacturer of the biological active substance | Daiichi Sankyo Chemical Pharma Co., Ltd. Onahama Plant 389-4, Izumimachi Shimokawa Aza Otsurugi, Iwaki, Fukushima 971-8183 Japan |
| Name and address of the manufacturer(s) responsible for batch release | Daiichi Sankyo Europe GmbH Luitpoldstrasse 1 85276 Pfaffenhofen Germany |
| Max shelf life | 3 years |
| Storage conditions | 2°C – 8°C |
| List of excipients | L-histidine L-histidine hydrochloride monohydrate Sucrose Polysorbate 80 |
Evidentic offers multiple batches of original drug aliquots in low binding Eppendorf tubes for research use only. We provide licence-free drug aliquots with long, short or even “negative shelf life” by storing the products at recommended temperatures (either 2-8°C or -80°C) and ensuring fully functional molecules for research purposes.
Evidentic GmbH
Am Mühlenberg 10
14476 Potsdam | Germany
