The National Medical Products Administration (NMPA) of China has approved mobocertinib (Exkivity®; Takeda), a first-in-class, oral tyrosine kinase inhibitor (TKI) for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) Exon20 insertion mutations, whose disease has progressed on or after platinum-based chemotherapy.

Mobocertinib has shown clinically meaningful and durable responses in patients with locally advanced or metastatic EGFR Exon20 insertion+ NSCLC and is now the first and only treatment available for this patient population in China. mobocertinib, an oral tyrosine kinase inhibitor designed to target Exon20 insertions, was reviewed as part of the NMPA’s Breakthrough Therapy program.

Full approval for this indication may be contingent upon verification of clinical benefit in a confirmatory trial.

“The approval of mobocertinib in China for patients with locally advanced or metastatic EGFR Exon20 insertion+ NSCLC was only possible through dedicated collaboration and support from the NMPA and the Chinese government,” said Awny Farajallah, Head, Global Medical Affairs Oncology, Takeda.

“Lung cancer is a devastating disease, and we know the discovery and delivery of precision medicines like mobocertinib to target cancer types that are hard-to-treat have the potential to improve patient outcomes. We are thrilled to introduce mobocertinib in China as the second lung cancer therapy from Takeda and remain committed to research and development to meet the needs of this patient community.”

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Lung cancer is the most commonly diagnosed cancer in China, and NSCLC accounts for approximately 85% of all lung cancer cases in the country. [1] Of those patients diagnosed with EGFR-mutated NSCLC in China, up to 10% harbor Exon20 insertions.[2][3][4][5][6][7] Despite this prevalence, patients in China have lacked a targeted treatment option designed to address cancers driven by these mutations.

“Since the discovery of EGFR mutations nearly twenty years ago, patients with Exon20 insertions have been waiting for a targeted therapy to treat their disease,” said Sean Shan, President of Takeda China.

“The approval of mobocertinib in China is a remarkable breakthrough, demonstrating the strong commitment of the Chinese government to encourage and accelerate the introduction of innovative therapies. mobocertinib offers a targeted, oral therapy to a population that has been historically underserved, and this approval brings us one step closer to defeating this complex and heterogeneous disease for patients in this region.”

This approval is based on the results from the platinum-pretreated population in the Phase 1/2 trial of mobocertinib, which consisted of 114 patients with EGFR Exon20 insertion+ NSCLC who received prior platinum-based therapy and were treated at the 160 mg dose. Results demonstrated a confirmed ORR of 28% per IRC as well as a median DoR of 15.8 months per IRC, a median overall survival (OS) of 20.2 months and a median progression-free survival (PFS) of 7.3 months per IRC. The most common treatment-related adverse reactions (TRAEs) were diarrhea (92%), rash (46%), paronychia (38%) and decreased appetite (37%).

Mobocertinib is currently approved in the United States, Great Britain, Switzerland, South Korea, Australia and China for the treatment of adult patients with locally advanced or metastatic NSCLC with EGFR Exon20 insertion mutations, whose disease has progressed on or after platinum-based chemotherapy.

Clinical trial
TAK-788 as First-Line Treatment Versus Platinum-Based Chemotherapy for Non-Small Cell Lung Cancer (NSCLC) With EGFR Exon 20 Insertion Mutations – NCT04129502

Highlights of Prescribing information
Mobocertinib (Exkivity™; Takeda) [Prescribing Information]

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[7] Yang, Guangjian et al. “EGFR exon 20 insertion mutations in Chinese advanced non-small cell lung cancer patients: Molecular heterogeneity and treatment outcome from nationwide real-world study.” Lung cancer (Amsterdam, Netherlands) vol. 145 (2020): 186-194.
[8] Zhou C. Lung cancer molecular epidemiology in China: recent trends. Transl Lung Cancer Res. 2014 Oct;3(5):270-9. doi: 10.3978/j.issn.2218-6751.2014.09.01
[9] Sung H, Ferlay J, Siegel RL, Laversanne M, Soerjomataram I, Jemal A, Bray F. Global Cancer Statistics 2020: GLOBOCAN Estimates of Incidence and Mortality Worldwide for 36 Cancers in 185 Countries. CA Cancer J Clin. 2021 May;71(3):209-249. doi: 10.3322/caac.21660. Epub 2021 Feb 4. PMID: 33538338.
[10] American Cancer Society. What is Non-Small Cell Lung Cancer? Online. Last accessed September 28, 2022.

Featured Image: © 2020 Takeda. Used with permission.

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