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Afatinib efficacy against squamous cell carcinoma of the head and neck cell lines in vitro and in vivo.

Young NR, Soneru C, Liu J, Grushko TA, Hardeman A, Olopade OI, Baum A, Solca F, Cohen EE - Target Oncol (2015)

Bottom Line: Two EGFR-amplified cell lines that are resistant to gefitinib are sensitive to afatinib.Cetuximab was not found to have a synergistic effect with afatinib either in vitro or in vivo.Both afatinib and cetuximab were effective in tumor xenograft model.

View Article: PubMed Central - PubMed

Affiliation: Department of Medicine and Comprehensive Cancer Center, University of Chicago, 900 E. 57th Street, Chicago, IL, 60637, USA. natyoung@bsd.uchicago.edu.

ABSTRACT
Epidermal growth factor receptor (EGFR) inhibitors have demonstrated efficacy in squamous cell carcinoma of the head and neck (SCCHN). In addition to EGFR, other ErbB family members are expressed and activated in SCCHN. Afatinib is an ErbB family blocker that has been approved for treating patients with EGFR-mutated nonsmall cell lung cancer. We sought to determine the efficacy of afatinib in preclinical models and compare this to other EGFR-targeted agents. Afatinib efficacy was characterized in a panel of ten SCCHN cell lines and found to be most effective against cell lines amplified for EGFR. Afatinib had lower IC(50) values than did gefitinib against the same panel. Two EGFR-amplified cell lines that are resistant to gefitinib are sensitive to afatinib. Cetuximab was not found to have a synergistic effect with afatinib either in vitro or in vivo. Both afatinib and cetuximab were effective in tumor xenograft model. Afatinib is an effective agent in SCCHN especially in models with EGFR amplification.

No MeSH data available.


Related in: MedlinePlus

PTEN expression in SCCHN cell lines. Western blotting shows that PTEN expression is consistent across cell lines. Actin serves as loading control
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Fig6: PTEN expression in SCCHN cell lines. Western blotting shows that PTEN expression is consistent across cell lines. Actin serves as loading control

Mentions: PTEN protein expression was examined by immunoblotting of SCCHN cell line lysates. We found that all lines express the protein at approximately equal levels (Fig. 6), eliminating PTEN loss as an explanation of primary EGFR inhibitor resistance in these lines.Fig. 6


Afatinib efficacy against squamous cell carcinoma of the head and neck cell lines in vitro and in vivo.

Young NR, Soneru C, Liu J, Grushko TA, Hardeman A, Olopade OI, Baum A, Solca F, Cohen EE - Target Oncol (2015)

PTEN expression in SCCHN cell lines. Western blotting shows that PTEN expression is consistent across cell lines. Actin serves as loading control
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4492891&req=5

Fig6: PTEN expression in SCCHN cell lines. Western blotting shows that PTEN expression is consistent across cell lines. Actin serves as loading control
Mentions: PTEN protein expression was examined by immunoblotting of SCCHN cell line lysates. We found that all lines express the protein at approximately equal levels (Fig. 6), eliminating PTEN loss as an explanation of primary EGFR inhibitor resistance in these lines.Fig. 6

Bottom Line: Two EGFR-amplified cell lines that are resistant to gefitinib are sensitive to afatinib.Cetuximab was not found to have a synergistic effect with afatinib either in vitro or in vivo.Both afatinib and cetuximab were effective in tumor xenograft model.

View Article: PubMed Central - PubMed

Affiliation: Department of Medicine and Comprehensive Cancer Center, University of Chicago, 900 E. 57th Street, Chicago, IL, 60637, USA. natyoung@bsd.uchicago.edu.

ABSTRACT
Epidermal growth factor receptor (EGFR) inhibitors have demonstrated efficacy in squamous cell carcinoma of the head and neck (SCCHN). In addition to EGFR, other ErbB family members are expressed and activated in SCCHN. Afatinib is an ErbB family blocker that has been approved for treating patients with EGFR-mutated nonsmall cell lung cancer. We sought to determine the efficacy of afatinib in preclinical models and compare this to other EGFR-targeted agents. Afatinib efficacy was characterized in a panel of ten SCCHN cell lines and found to be most effective against cell lines amplified for EGFR. Afatinib had lower IC(50) values than did gefitinib against the same panel. Two EGFR-amplified cell lines that are resistant to gefitinib are sensitive to afatinib. Cetuximab was not found to have a synergistic effect with afatinib either in vitro or in vivo. Both afatinib and cetuximab were effective in tumor xenograft model. Afatinib is an effective agent in SCCHN especially in models with EGFR amplification.

No MeSH data available.


Related in: MedlinePlus