The FDA granted the selective oral tyrosine kinase inhibitor mobocertinib priority review for patients with pretreated metastatic non-small cell lung cancer harboring insertion mutations in EGFR exon 20.


Mobocertinib approved for the treatment of patients with locally advanced or metastatic nonsmall cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 20 insertion mutations.

Trade name Exkivity.

The drug is limited to use in patients whose disease has progressed on or after platinum-based chemotherapy and who have had the EGFR exon20 insertion mutation detected on an FDA-approved test.

Mobocertinib is the first oral tyrosine kinase inhibitor (TKI) specifically designed to target these mutations, which are less common than the more predominant EGFR mutations in this lung cancer.

It is for the treatment of patients with metastatic non-small cell lung cancer (mNSCLC) and an EGFR exon 20 insertion mutation who have received prior platinum-based chemotherapy.

EGFR exon 20 insertion positive] mNSCLC with current treatment options results in poor survival outcomes.


EGFR Exon20 insertion+ NSCLC makes up approximately 1%-2% of patients with NSCLC.


There is an next-generation sequencing (NGS) companion diagnostic test which identifies NSCLC patients with EGFR Exon20 insertions.

EGFR Exon20 insertion NSCLC  is more common in Asian populations compared with Western populations.

Studies included 114 patients who received prior platinum-based therapy and were treated as part of the dose-escalation and dose-expansion portions of the phase 1/2 trial. 

Patients were treated with mobocertinib at 160 mg once daily.


In a phase 1/2 trial consisting of 114 patients with EGFR Exon20 insertion+ NSCLC who received prior platinum-based therapy and were treated with the 160-mg dose: it demonstrated a confirmed overall response rate of 28% and a median duration  of 17.5 months.

Mobocertinib demonstrated clinically meaningful responses and a noteworthy duration of response in patients with EGFR exon 20 insertion-positive metastatic NSCLC who received prior platinum-based therapy.

The most common adverse reactions (> 20%) were diarrhea, rash, nausea, stomatitis, vomiting, decreased appetite, paronychia, fatigue, dry skin, and musculoskeletal pain.

Warnings for QTc prolongation and Torsades de Pointes, and warnings and precautions for interstitial lung disease/pneumonitis, cardiac toxicity, and diarrhea are given.

Discontinuations due to AEs occurred in 17% of patients, most commonly from diarrhea (4%) and nausea (4%).

Responses in patients who were previously treated with TKIs were also noted.


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