2021/07/01 by Shannon Zhang, Viola W. Zhu · 1 citation
Medicine · Biochemistry, Genetics and Molecular Biology · #Lung Cancer Treatments and Mutations #Cancer Genomics and Diagnostics #Colorectal Cancer Treatments and Studies #Medicine #Osimertinib #Exon #Lung cancer #Oncology #Mutation #Chemotherapy #Epidermal growth factor receptor #Cancer research #Internal medicine #Erlotinib #Cancer #Gene #Genetics #Biology
paper · pdf · doi:10.2147/lctt.s307321
openalex publication_date 2021/07/01 · openalex created_date 2025/10/10 · openalex updated_date 2026/07/29
Abstract: The EGFR exon 20 insertion ( EGFR ex20ins) mutations are the third most common EGFR mutations seen in non-small cell lung cancer (NSCLC). More than 50 variants of EGFR ex20ins mutations have been identified with A767V769dupASV 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 EGFR ex20ins 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 EGFR ex20ins mutation variants and how they may affect treatment response. Keywords: mobocertinib, TAK-788, NSCLC, EGFR exon 20 insertion, TKI, amivantamab