Targeting HER2 Exon 20 Insertion–Mutant Lung Adenocarcinoma with a Novel Tyrosine Kinase Inhibitor Mobocertinib
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Abstract
No targeted treatments are currently approved for HER2 exon 20 insertion–mutant lung adenocarcinoma patients. Mobocertinib (TAK-788) is a potent irreversible tyrosine kinase inhibitor (TKI) designed to target human epidermal growth factor receptor 2 (HER2/ERBB2) exon 20 insertion mutations. However, the function of mobocertinib on HER2 exon 20 insertion–mutant lung cancer is still unclear. Here we conducted systematic characterization of preclinical models to understand the activity profile of mobocertinib against HER2 exon 20 insertions. In HER2 exon 20 insertion–mutant cell lines, the IC50 of mobocertinib was higher than poziotinib and comparable with or slightly lower than afatinib, neratinib, and pyrotinib. Mobocertinib had the lowest HER2 exon 20 insertion IC50/wild-type (WT) EGFR IC50 ratio, indicating that mobocertinib displayed the best selectivity profile in these models. Also, mobocertinib showed strong inhibitory activity in HER2 exon 20YVMA allograft and patient-derived xenograft models. In genetically engineered mouse models, HER2 exon 20G776>VC lung tumors exhibited a sustained complete response to mobocertinib, whereas HER2 exon 20YVMA tumors showed only partial and transient response. Combined treatment with a second antibody–drug conjugate (ADC) against HER2, ado-trastuzumab emtansine (T-DM1), synergized with mobocertinib in HER2 exon 20YVMA tumors. In addition to the tumor cell autonomous effect, sustained tumor growth control derived from M1 macrophage infiltration and CD4+ T-cell activation. These findings support the ongoing clinical development of mobocertinib (NCT02716116) and provide a rationale for future clinical evaluation of T-DM1 combinational therapy in HER2 exon 20YVMA insertion–mutant lung adenocarcinoma patients. Significance: This study elucidates the potent inhibitory activity of mobocertinib against HER2 exon 20 insertion–mutant lung cancer and the synergic effect of combined mobocertinib and T-DM1, providing a strong rationale for clinical investigation.
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Structurally similar to osimertinib, mobocertinib possesses an enhanced inhibitory effect against EGFR exon 20 insertion and other non-sensitive mutations, as well as some inhibitory effect against lung cancer with HER2 exon 20 insertion mutations.
“Structurally similar to osimertinib, it possesses an enhanced inhibitory effect against EGFR exon 20 insertion and other non-sensitive mutations, as well as some inhibitory effect against lung cancer with HER2 exon 20 insertion mutations.150,151”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [151]
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- Authors
- Han, H., Li, S., Chen, T., Fitzgerald, M., Liu, S., Peng, C., Tang, K. H., Cao, S., Chouitar, J., Wu, J., Peng, D., Deng, J., Gao, Z., Baker, T. E., Li, F., Zhang, H., Pan, Y., Ding, H., Hu, H., Pyon, V., Thakurdin, C., Papadopoulos, E., Tang, S., Gonzalvez, F., Chen, H., Rivera, V. M., Brake, R., Vincent, S., & Wong, K.-K.
- Affiliations
- Fudan University Shanghai Cancer Center (CN)
- NYU Langone Health (US)
- 3Millennium Pharmaceuticals, Inc., Cambridge, Massachusetts, a wholly owned subsidiary of Takeda Pharmaceutical Company Limited.
- Harvard University (US)
- 5ARIAD Pharmaceuticals, Inc., Cambridge, Massachusetts, a wholly owned subsidiary of Takeda Pharmaceutical Company Limited.
- Corresponding author
- Li, Shuai
- Vincent, Sylvie
- Wong, Kwok-Kin
- ORCID
- Venue
- Cancer Research
- Published
- 2021-08-11
- Volume
- 81
- Issue
- 20
- Pages
- 5311-5324
- ISSN
- 0008-5472 (ISSN-L)
- 1538-7445
- PMC
- PMC8530969
- OpenAlex
- W3187778387
- Cited by
- 57
- References
- 43
- Citations by year
- 2026: 4 · 2025: 14 · 2024: 7 · 2023: 17 · 2022: 12 · 2021: 3
- FWCI
- 6.32
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Cancer Research (publishedVersion, cc-by-nc-nd)
- PubMed Central (publishedVersion, cc-by-nc-nd)
- PubMed (publishedVersion)
- Funders
- National Institutes of Health (CA154303, CA098101)
- Takeda Oncology
- Topics
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
- Health Sciences › Medicine › Oncology › HER2/EGFR in Cancer Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer Genomics and Diagnostics
- Keywords
- mobocertinib, lung adenocarcinoma, tyrosine kinase inhibitors, trastuzumab emtansine, antibody-drug conjugates, combination therapy, patient-derived xenografts, genetically engineered mouse models, tumor-infiltrating macrophages, CD4+ T cell activation, targeted therapy, poziotinib
- MeSH terms
- Adenocarcinoma of Lung, Ado-Trastuzumab Emtansine, Animals, Antineoplastic Combined Chemotherapy Protocols, Exons, Female, Humans, Lung Neoplasms, Tumor Cells, Cultured, Gene Expression Regulation, Neoplastic, Mice, SCID, Mice, Inbred NOD, Apoptosis, Antibodies, Bispecific, Erb-b2 Receptor Tyrosine Kinases, Xenograft Model Antitumor Assays, Cell Proliferation, Mice, INDEL Mutation
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