MECHANISM OF ACTION
How does ENHERTU work?
Redefine expectations of breast cancer therapy with the engineered mechanism of action of ENHERTU.1–4
This promotional website is
intended for UK healthcare professionals only
This promotional website is intended for UK healthcare professionals only
- Adverse event reporting
- UK Prescribing Information
- Contact us
ENHERTU (trastuzumab deruxtecan) as monotherapy is indicated for the treatment of adult patients with unresectable or metastatic HER2-positive breast cancer who have received one or more prior anti-HER2-based regimens1
ENHERTU as monotherapy is indicated for the treatment of adult patients with unresectable or metastatic HER2-low breast cancer who have received prior chemotherapy in the metastatic setting or developed disease recurrence during or within 6 months of completing adjuvant chemotherapy1
Enhertu has a Conditional Marketing Authorisation
HER2-directed ADC
Ensures delivery of the toxic payload to tumour cells expressing HER2.3
The proposed mechanism of action is based on pre-clinical data and clinical outcomes cannot be inferred.
Tumour-selective cleavable linker2,4
Linker-payload is stable in plasma and cleaved by proteases highly expressed in cancer cells for enhanced, tumour-specific delivery of toxic payload
High-potency topoisomerase I inhibitor1
Highly potent payload is an exatecan derivative, known as DXd, and is more potent than SN-38, the active metabolite of irinotecan1
High antibody-drug ratio and membrane-permeable toxin2–5
Enables reliable and consistent delivery of toxic payload (8:1 drug-to-antibody ratio) to the tumour and the neighbouring cells, with and without HER2 expression (bystander anti-tumour effect).
What is the dosage for ENHERTU and how is it given?
Recommended dosage and schedule1
Please refer to the ENHERTU Summary of Product Characteristics for full information on dosing and dose modifications.
Permanently discontinue ENHERTU in cases of severe infusion reactions1
Slow or interrupt the infusion rate if the patient develops infusion-related symptoms1
Do not substitute ENHERTU with trastuzumab or trastuzumab emtansine1
Premedication
ENHERTU is emetogenic, which includes delayed nausea and/or vomiting. Prior to each dose of ENHERTU, patients should be premedicated with a combination regimen of two or three medicinal products (e.g. dexamethasone with either a 5-HT3 receptor antagonist and/or an NK1 receptor antagonist, as well as other medicinal products as indicated) for prevention of chemotherapy-induced nausea and vomiting.1
Dosage forms and strengths
For injection: 100 mg of ENHERTU as a white to yellowish-white lyophilised powder in a single-dose vial for reconstitution and further dilution.1
How to prepare ENHERTU for use
- In order to prevent medication errors, check the vial labels to ensure that the drug being prepared and administered is ENHERTU and not trastuzumab or trastuzumab emtansine1
- ENHERTU requires reconstituting and diluting prior to intravenous infusion1
- Use appropriate aseptic technique1
- ENHERTU is a cytotoxic drug. Follow applicable special handling and disposal procedures1
Steps to prepare ENHERTU for use
- Reconstitution
- Dilution
- Administration
How to reconstitute ENHERTU1
- Reconstitute immediately before dilution
- More than one vial may be needed for a full dose. Calculate the dose (mg), the total volume of reconstituted ENHERTU solution required and the number of vial(s) of ENHERTU needed
- Reconstitute each 100 mg vial by using a sterile syringe to slowly inject 5 mL of sterile water for injection into each vial to obtain a final concentration of 20 mg/mL
- Swirl the vial gently until completely dissolved. Do not shake
- If not used immediately, store the reconstituted ENHERTU vials in a refrigerator at 2–8°C for up to 24 hours from the time of reconstitution, protected from light. Do not freeze
- The reconstituted product contains no preservative and is intended for single use only
How to dilute ENHERTU1
- Withdraw the calculated amount from the vial(s) using a sterile syringe. Inspect the reconstituted solution for particulates and discolouration. The solution should be clear and colourless to light yellow. Do not use if visible particles are observed or if the solution is cloudy or discoloured
- Dilute the calculated volume of reconstituted ENHERTU in an infusion bag containing 100 mL of 5% glucose solution. Do not use sodium chloride solution. An infusion bag made of polyvinylchloride or polyolefin (copolymer of ethylene and polypropylene) is recommended
- Gently invert the infusion bag to thoroughly mix the solution. Do not shake
- Cover the infusion bag to protect it from light
- If not used immediately, store at room temperature for up to 4 hours, including preparation and infusion, or in a refrigerator at 2–8°C for up to 24 hours, protected from light. Do not freeze
- Discard any unused portion left in the vial
How to give ENHERTU1
- If the prepared infusion solution was stored refrigerated (2–8°C), it is recommended that the solution be allowed to equilibrate to room temperature prior to administration, protected from light
- Administer ENHERTU as an IV infusion only with a 0.20 or 0.22 micron in-line polyethersulfone or polysulfone filter
- The initial dose should be administered as a 90-minute IV infusion. If the prior infusion was well tolerated, subsequent doses of ENHERTU may be administered as 30-minute infusions. Do not administer as an IV push or bolus
- Cover the infusion bag to protect from light
- Do not mix ENHERTU with other medicinal products or administer other medicinal products through the same IV line
Abbreviations
ADC, antibody-drug conjugate; AE, adverse event; DXd, deruxtecan derivative; 5-HT, 5-hydroxytryptamine; HER2, human epidermal growth factor receptor 2; IV, intravenous; NK1, neurokinin 1.
Important safety information
For further information, including safety information, see the ENHERTU Summary of Product Characteristics.
Adverse events should be reported. Reporting forms and information can be found at https://yellowcard.mhra.gov.uk/ or search for MHRA Yellow Card in Google Play or Apple App store. Adverse events should also be reported to Daiichi Sankyo UK Pharmacovigilance on 0800 028 5122 or by email to pharmacovigilance@daiichi-sankyo.co.uk. As ENHERTU is a biological medicine, healthcare professionals should report adverse reactions by brand name and batch number.
References
- ENHERTU (trastuzumab deruxtecan). Summary of Product Characteristics.
- Yver A, et al. Ann Oncol 2020;31:430–4.
- Ogitani Y, et al. Clin Cancer Res 2016;22:5097–108.
- Nakada T, et al. Chem Pharm Bull (Tokyo) 2019;67:173–85.
- Ogitani Y, et al. Cancer Sci 2016;107:1039–46.
UK/ADC/01/25/0007 | April 2025
