Spotlight on Mobocertinib (TAK-788) in NSCLC with EGFR Exon 20 Insertion Mutations
Shannon S Zhang,1 Viola W Zhu1,2 1University of California, Irvine School of Medicine, Department of Medicine, Orange, CA, USA; 2Chao Family Comprehensive Cancer Center, Orange, CA, USACorrespondence: Viola W ZhuUniversity of California, Irvine School of Medicine, Department of Medicine, 200 S Manch...
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| Formato: | article |
| Lenguaje: | EN |
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Dove Medical Press
2021
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| Acceso en línea: | https://doaj.org/article/5baf978ecbe94f9e9c65f45036a12bcd |
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| Sumario: | Shannon S Zhang,1 Viola W Zhu1,2 1University of California, Irvine School of Medicine, Department of Medicine, Orange, CA, USA; 2Chao Family Comprehensive Cancer Center, Orange, CA, USACorrespondence: Viola W ZhuUniversity of California, Irvine School of Medicine, Department of Medicine, 200 S Manchester Ave, Suite 410, Orange, CA, 92868, USATel +1 714-456-8105Fax +1 714-456-2242Email zhuvw@hs.uci.eduAbstract: The EGFR exon 20 insertion (EGFRex20ins) mutations are the third most common EGFR mutations seen in non-small cell lung cancer (NSCLC). More than 50 variants of EGFRex20ins mutations have been identified with A767_V769dupASV being the most common variant across multiple surveys. Treatment with currently available EGFR tyrosine kinase inhibitors (TKIs) including osimertinib is generally ineffective. Amivantamab (JNJ-372), a bispecific monoclonal antibody against EGFR and MET, has recently been approved by the US FDA for patients with advanced or metastatic NSCLC harboring EGFRex20ins mutations after disease progression on platinum-based chemotherapy. Among all the TKIs in clinical development, mobocertinib (TAK-788) has been granted priority review by the FDA for the same indication as amivantamab. Here, we provide a concise review on mobocertinib, with a focus on its chemical structure, preclinical data, and phase 1/2 trial results. Future directions will likely focus on combination approach such as TKI plus chemotherapy in the first-line setting, designing drugs with CNS activity, and exploring disease characteristics of various EGFRex20ins mutation variants and how they may affect treatment response.Keywords: mobocertinib, TAK-788, NSCLC, EGFR exon 20 insertion, TKI, amivantamab |
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