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Mobocertinib: First Approval

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Abstract

Mobocertinib (EXKIVITY™) is a first-in-class EGFR tyrosine kinase inhibitor being developed for the treatment of EGFR exon 20 insertion (EGFRex20ins) -positive non-small cell lung cancer (NSCLC). Based on efficacy in patients whose disease had progressed on or after platinum-based therapy in a phase I/II trial, mobocertinib was recently granted accelerated approval in the USA in this indication. The drug is also being assessed for marketing approval in various other countries and territories including the EU and China. This article summarizes the milestones in the development of mobocertinib leading to this first approval in the USA for locally advanced or metastatic EGFRex20ins-positive NSCLC that has progressed on or after platinum-based chemotherapy.

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References

  1. Vyse S, Huang PH. Targeting EGFR exon 20 insertion mutations in non-small cell lung cancer. Signal Transduct Target Ther. 2019;4:5.

    Article  Google Scholar 

  2. Gonzalvez F, Vincent S, Baker TE, et al. Mobocertinib (TAK-788): a targeted inhibitor of EGFR exon 20 insertion mutants in non-small cell lung cancer. Cancer Discov. 2021;11(7):1672–87.

    Article  CAS  Google Scholar 

  3. US Food & Drug Administration. FDA grants accelerated approval to mobocertinib for metastatic non-small cell lung cancer with EGFR exon 20 insertion mutations [media release]. 15 Sep 2021.

  4. Takeda Pharmaceuticals. EXKIVITY™ (mobocertinib) capsules, for oral use. 2021. https://www.accessdata.fda.gov. Accessed 17 Sep 2021.

  5. Ariad Pharmaceuticals. ARIAD announces FDA clearance to begin clinical development of AP32788 [media release]. 1 Feb 2016.

  6. Takeda Pharma. Takeda completes acquisition of ARIAD pharmaceuticals, inc [media release]. 16 Feb 2017.

  7. Thermo Fisher. Thermo Fisher Scientific signs new agreements to expand Oncomine Dx target test [media release]. 1 May 2018.

  8. Foundation Medicine. Foundation Medicine and Takeda announce collaboration to develop FoundationOne® CDx and FoundationOne® liquid CDx as companion diagnostics for Takedas late-stage lung cancer portfolio [media release] 18 Sep 2020.

  9. Riely GJ, Neal JW, Camidge DR, et al. Activity and safety of mobocertinib (TAK-788) in previously treated non-small cell lung cancer with EGFR exon 20 insertion mutations from a phase I/II trial. Cancer Discov. 2021;11(7):1688–99.

    Article  CAS  Google Scholar 

  10. Zhang S, Jin S, Griffin C, et al. Effects of itraconazole and rifampin on the pharmacokinetics of mobocertinib (TAK-788), an oral epidermal growth factor receptor inhibitor, in healthy volunteers. Clin Pharmacol Drug Dev. 2021;10(9):1044–53.

    Article  CAS  Google Scholar 

  11. Zhou C, Ramalingam S, Kim TM, et al. Treatment outcomes and safety of mobocertinib in platinum-pretreated patients with EGFR exon 20 insertion–positive metastatic non–small cell lung cancer; a phase 1/2 open-label nonrandomized clinical trial. JAMA Oncol. 2021. https://doi.org/10.1001/jamaoncol.2021.4761.

    Article  PubMed  PubMed Central  Google Scholar 

  12. Takeda. Takedas EXKIVITY™ (mobocertinib) approved by US FDA as the first oral therapy specifically designed for patients with EGFR exon20 insertion+ NSCLC [media release] 16 Sep 2021.

  13. Janne PA, Wu YL, Kato T, et al. Mobocertinib (TAK-788) as first-line treatment vs platinum-based chemotherapy (CT) for NSCLC with EGFR exon 20 insertions (exon20ins) [abstract no. 1412TiP]. Ann Oncol. 2020;31(Suppl 4):S892–3.

    Article  Google Scholar 

  14. Hida T, Nishino M, Yoh T, et al. A phase I dose-escalation study of mobocertinib (TAK-788), an oral tyrosine kinase inhibitor (TKI), in Japanese NSCLC patients [abstract no. 1246P]. Ann Oncol. 2021;32(Suppl 5):S949–1039.

    Google Scholar 

  15. Takeda. Takeda announces US FDA breakthrough therapy designation for mobocertinib (TAK-788) for the treatment of NSCLC patients with EGFR exon 20 insertion mutations [media release] 27 Apr 2020.

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Authors and Affiliations

  1. Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand

    Anthony Markham

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  1. Anthony Markham
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Correspondence to Anthony Markham.

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Funding

The preparation of this review was not supported by any external funding.

Authorship and Conflict of interest

During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the authors on the basis of scientific completeness and accuracy. A. Markham is a salaried employee of Adis International Ltd/Springer Nature, and declares no relevant conflicts of interest. All authors contributed to the review and are responsible for the article content.

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This profile has been extracted and modified from the AdisInsight database. AdisInsight tracks drug development worldwide through the entire development process, from discovery, through pre-clinical and clinical studies to market launch and beyond.

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Markham, A. Mobocertinib: First Approval. Drugs 81, 2069–2074 (2021). https://doi.org/10.1007/s40265-021-01632-9

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  • DOI: https://doi.org/10.1007/s40265-021-01632-9

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