Literature DB >> 28823407

Antitumor activity of the dual PI3K/MTOR inhibitor, PF-04691502, in combination with radiation in head and neck cancer.

Nathan Tonlaar1, Sandra Galoforo1, Bryan J Thibodeau2, Samreen Ahmed2, Thomas G Wilson1, Paola Yumpo Cardenas1, Brian Marples1, George D Wilson3.   

Abstract

BACKGROUND AND
PURPOSE: Head and neck squamous cell carcinoma (HNSCC) remains a clinical challenge where new treatments are required to supplement the current-standard-of care of concurrent chemoradiation. The PI3K/AKT/MTOR pathway has been identified from several next generation DNA sequencing studies to be commonly altered and activated in HNSCC.
MATERIAL AND METHODS: In this study we investigated the activity of PF-04691502, an orally active ATP-competitive, dual inhibitor of PI3K and mTOR, in combination with a clinically relevant fractionated radiation treatment in two contrasting, well characterized, low passage HNSCC models.
RESULTS: We found that PF-04691502 combined synergistically with radiation in the UT-SCC-14 model derived from a primary cancer but was ineffective in the UT-SCC-15 model which was derived from a nodal recurrence. Further examination of the status of key signaling pathways combined with next generation DNA sequencing of a panel of 160 cancer-associated genes revealed crucial differences between the two models that could account for the differential effect. The UT-SCC-15 cell line was characterized by a higher mutational burden, an excess of variants in the PI3K/AKT/MTOR pathway, increased constitutive activity of PI3K, AKT1 and 2 and MTOR and an inability to inhibit key phosphorylation events in response to the treatments.
CONCLUSION: This study clearly highlights the promise of agents such as PF-04691502 in selected HNSCCs but also emphasizes the need for molecular characterization and alternative treatment strategies in non-responsive HNSCCs.
Copyright © 2017 Elsevier B.V. All rights reserved.

Entities:  

Keywords:  Head and neck cancer; Next generation DNA sequencing; PI3K/MTOR inhibition; Radiation

Mesh:

Substances:

Year:  2017        PMID: 28823407     DOI: 10.1016/j.radonc.2017.08.001

Source DB:  PubMed          Journal:  Radiother Oncol        ISSN: 0167-8140            Impact factor:   6.280


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