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Exkivity
Published
Product name
Exkivity
Active ingredient
Mobocertinib
Submission type
New chemical entity
Decision
Approved for provisional registration
Decision date
Registration date
What this medicine was approved for
Exkivity (mobocertinib) was approved for the following therapeutic use:
Exkivity has provisional approval in Australia for the treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) that has an exon 20 insertion mutation of the epidermal growth factor receptor (EGFR), who have received prior platinum-based chemotherapy.
The decision to approve this indication has been made on the basis of objective response rate and duration of response in a single arm study. Continued approval of this indication depends on verification and description of benefit in a confirmatory study.
How this medicine works
Mobocertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR) that irreversibly binds to and inhibits EGFR harbouring an exon 20 insertion mutation at lower concentrations than wild type (WT)-EGFR. Two pharmacologically active metabolites (AP32960 and AP32914) with similar inhibitory profiles to mobocertinib have been identified in the plasma after oral administration of mobocertinib. In vitro, mobocertinib also inhibited the activity of EGFR family members (human epidermal growth factor receptor 2 [HER2] and human epidermal growth factor receptor 4 [HER4]), and one additional kinase (B lymphoid tyrosine kinase [BLK]) at clinically relevant concentrations (half maximal inhibitory concentration (IC50) values < 2 nM).
In cell culture models, mobocertinib inhibited the proliferation of cells driven by different EGFR exon 20 insertion mutation variants at 1.5- to 10-fold lower concentrations than those required for WT-EGFR signalling inhibition.
In murine tumour implantation models, mobocertinib demonstrated anti-tumour activity against xenografts carrying either the NPH or the ASV EGFR exon 20 insertion mutation.
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 Exkivity was considered favourable for the therapeutic use approved.
ARTG details
- 370160