A phase II study of temsirolimus and erlotinib in patients with recurrent and/or metastatic, platinum-refractory head and neck squamous cell carcinoma

Oral Oncol. 2013 May;49(5):461-7. doi: 10.1016/j.oraloncology.2012.12.016. Epub 2013 Feb 4.

Abstract

Objectives: The epidermal growth factor receptor (EGFR) is a validated target in head and neck squamous cell carcinoma (HNSCC). In recurrent and/or metastatic (R/M) HNSCC, resistance to anti-EGFR therapy inevitably occurs. Downstream activation of the PI3K/Akt/mTOR pathway is an established resistance mechanism. Concurrent mTOR blockade may improve efficacy of anti-EGFR therapy.

Materials and methods: Erlotinib 150 mg daily and temsirolimus 15 mg weekly were administered to patients with platinum-refractory R/M HNSCC and ECOG performance status 0-2. The primary endpoint was progression-free survival (PFS). Correlative studies determined PIK3CA and HRAS mutation status; p16, EGFR, pS6K, pAkt and PTEN expression; and pre- and post-treatment plasma levels of 20 immunomodulatory cytokines.

Results: Twelve patients enrolled; six withdrew within 6 weeks due to toxicity or death, prompting early closure of the trial. Grade ≥ 3 toxicities included fatigue, diarrhea, gastrostomy tube infection, peritonitis, pneumonia, dyspnea, and HN edema. Median PFS was 1.9 months. Median overall survival was 4.0 months. Six/12 tumors were p16(+), 9/11 lacked measurable PTEN expression, and 1/12 harbored a PIK3CA mutation. On exploratory analysis, high baseline plasma VEGF and interferon-gamma levels marginally associated with tumor progression.

Conclusions: The combination of erlotinib and temsirolimus was poorly tolerated. Low prevalence of PTEN expression and 8% incidence of PIK3CA mutations indicate biological relevance of this pathway in R/M disease. Investigation of more tolerable combinations of EGFR and PI3K/Akt/mTOR pathway inhibitors in selected HNSCC patients is warranted.

Publication types

  • Clinical Trial, Phase II
  • Comparative Study
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Aged, 80 and over
  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Combined Chemotherapy Protocols / adverse effects
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Carcinoma, Squamous Cell / drug therapy*
  • Carcinoma, Squamous Cell / secondary
  • Class I Phosphatidylinositol 3-Kinases
  • Cyclin-Dependent Kinase Inhibitor p16 / analysis
  • Cytokines / analysis
  • Drug Resistance, Neoplasm
  • ErbB Receptors / antagonists & inhibitors*
  • Erlotinib Hydrochloride
  • Female
  • Head and Neck Neoplasms / drug therapy*
  • Humans
  • Male
  • Middle Aged
  • Mutation / genetics
  • Neoplasm Recurrence, Local / drug therapy*
  • Oncogene Protein v-akt / analysis
  • PTEN Phosphohydrolase / analysis
  • Phosphatidylinositol 3-Kinases / analysis
  • Phosphatidylinositol 3-Kinases / genetics
  • Platinum
  • Protein Kinase Inhibitors / administration & dosage*
  • Proto-Oncogene Proteins p21(ras) / analysis
  • Proto-Oncogene Proteins p21(ras) / genetics
  • Quinazolines / administration & dosage*
  • Quinazolines / adverse effects
  • Ribosomal Protein S6 Kinases / analysis
  • Sirolimus / administration & dosage
  • Sirolimus / adverse effects
  • Sirolimus / analogs & derivatives*
  • Survival Rate
  • TOR Serine-Threonine Kinases / antagonists & inhibitors
  • Tumor Suppressor Proteins / analysis

Substances

  • Antineoplastic Agents
  • Cyclin-Dependent Kinase Inhibitor p16
  • Cytokines
  • Protein Kinase Inhibitors
  • Quinazolines
  • Tumor Suppressor Proteins
  • Platinum
  • temsirolimus
  • Erlotinib Hydrochloride
  • MTOR protein, human
  • Class I Phosphatidylinositol 3-Kinases
  • PIK3CA protein, human
  • ErbB Receptors
  • Oncogene Protein v-akt
  • Ribosomal Protein S6 Kinases
  • TOR Serine-Threonine Kinases
  • PTEN Phosphohydrolase
  • PTEN protein, human
  • HRAS protein, human
  • Proto-Oncogene Proteins p21(ras)
  • Sirolimus