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Bosutinib Inhibits EGFR Activation in Head and Neck Cancer
Carmen Segrelles1,2,3, David Contreras4, Elena M Navarro5
1Molecular Oncology Unit, CIEMAT (ed 70A), Ave Complutense 40, 28040 Madrid, Spain. carmen.segrelles@ciemat.es.
Abstract:
Head and neck squamous cell carcinoma (HNSCC) is the sixth most common cancer worldwide, and although new therapeutic approaches have been recently evaluated, overall patient survival is still poor. Thus, new effective and selective clinical treatments are urgently needed. An analysis of data from large-scale, high-throughput drug screening cell line projects identified Bosutinib, a Src/Abl inhibitor that is currently used for the treatment of chronic myelogenous leukemia, as a candidate drug to treat HNSCC. Using a panel of HNSCC-derived cell lines, we found that treatment with Bosutinib reduced cell proliferation and induced apoptosis of sensitive cell lines. The drug rapidly inhibited Src and EGFR (epidermal growth factor receptor) phosphorylation, and sensitivity to Bosutinib was correlated with the activation status of EGFR. Similar findings were observed in in vivo xenograft assays using HNSCC derived cells. Moreover, in the presence of mutations in PIK3CA, the combination of Bosutinib with the PI3Kα inhibitor Alpelisib showed a synergistic effect. These results suggest that Bosutinib could be a new effective drug for the treatment of HNSCC, particularly in tumors with high EGFR activity. Its combination with Alpelisib could especially benefit patients bearing activating mutations of PIK3CA.
Insights
Bosutinib, a Src/Abl inhibitor, effectively reduced head and neck squamous cell carcinoma (HNSCC) cell growth and induced apoptosis. This drug shows promise for HNSCC treatment, especially when combined with Alpelisib for PIK3CA-mutated tumors.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Head and neck squamous cell carcinoma (HNSCC) remains a significant global health challenge with poor patient survival rates despite recent therapeutic advancements.
- There is an urgent need for novel, effective, and selective treatments for HNSCC.
- Src/Abl inhibitors represent a class of drugs with potential therapeutic applications in various cancers.
Purpose of the Study:
- To investigate the efficacy of Bosutinib, a Src/Abl inhibitor, as a potential treatment for HNSCC.
- To explore the mechanisms underlying Bosutinib's action in HNSCC cells.
- To evaluate the synergistic effect of combining Bosutinib with Alpelisib in specific HNSCC contexts.
Main Methods:
- Drug screening identified Bosutinib as a candidate for HNSCC treatment.
- In vitro studies utilized HNSCC cell lines to assess Bosutinib's effects on proliferation and apoptosis.
- In vivo xenograft assays were performed to validate findings in a preclinical model.
- Analysis included assessment of Src and epidermal growth factor receptor (EGFR) phosphorylation.
- Combination therapy studies involved Bosutinib and Alpelisib, particularly in cells with PIK3CA mutations.
Main Results:
- Bosutinib treatment significantly reduced proliferation and induced apoptosis in sensitive HNSCC cell lines.
- Bosutinib effectively inhibited Src and EGFR phosphorylation, with sensitivity correlating to EGFR activation status.
- In vivo xenograft models confirmed Bosutinib's anti-tumor activity.
- The combination of Bosutinib and Alpelisib demonstrated a synergistic effect in HNSCC cells with PIK3CA mutations.
Conclusions:
- Bosutinib is a promising candidate for HNSCC treatment, particularly in tumors with high EGFR activity.
- The combination of Bosutinib and Alpelisib may offer significant benefits for patients with activating PIK3CA mutations.
- Further clinical investigation of Bosutinib, alone and in combination, is warranted for HNSCC management.
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