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Enhertu
Published
Product name
Enhertu
Active ingredient
Trastuzumab deruxtecan
Submission type
New biological entity
Decision
Approved for provisional registration
Decision date
Registration date
What this medicine was approved for
Enhertu (trastuzumab deruxtecan) was approved for the following therapeutic use:
Enhertu is 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.
This indication is approved via the provisional approval pathway, based on overall response rate and duration of response. Full registration for this indication depends on verification and description of clinical benefit in a confirmatory trial.
How this medicine works
Trastuzumab deruxtecan, is a human epidermal growth factor receptor 2 (HER2) targeted antibody-drug conjugate (ADC). The antibody is a humanised anti‑HER2 immunoglobin G1 (IgG1) attached to deruxtecan, a topoisomerase I inhibitor bound by a tetrapeptide based cleavable linker. The ADC is stable in plasma under in vitro conditions. Following binding to HER2 on tumour cells, trastuzumab deruxtecan undergoes internalisation and intracellular linker cleavage by lysosomal enzymes. Upon release, the membrane permeable topoisomerase I inhibitor causes deoxyribonucleic acid (DNA) damage and apoptotic cell death. The topoisomerase I inhibitor, an exatecan derivative, is approximately 10 times more potent than 7‑ethyl‑10‑hydroxycamptothecin (SN38), the active metabolite of irinotecan.
Why the TGA approved or did not approve this medicine
The decision was based on quality (chemistry and manufacturing), nonclinical (pharmacology and toxicology), clinical (pharmacology, safety and efficacy) and risk management plan information submitted by the sponsor. The benefit-risk profile of Enhertu was considered favourable for the therapeutic use approved.
Sponsor