Phase IB Trial of the Anti-Cancer Stem Cell DLL4-Binding Agent Demcizumab with Pemetrexed and Carboplatin as First-Line Treatment of Metastatic Non-Squamous NSCLC.

Background: Delta-like ligand 4-Notch (DLL4-Notch) signaling contributes to the maintenance of chemotherapy-resistant cancer stem cells and tumor vasculature.Objective: This phase IB trial of demcizumab, an IgG2 humanized monoclonal antibody directed against DLL4, was undertaken to determine its max...

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Publicado en:Targeted Oncology Vol. 13; no. 1; pp. 89 - 99
Autores principales: McKeage, Mark J., Kotasek, Dusan, Markman, Ben, Hidalgo, Manuel, Millward, Michael J., Jameson, Michael B., Harris, Dean L., Stagg, Robert J., Kapoun, Ann M., Xu, Lu, Hughes, Brett G. M.
Formato: research Journal Article
Publicado: Springer Nature Feb2018
Acceso en línea:Ver este registro en EBSCOhost
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      pub: Springer Nature
      place: New York, New York
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        10.1007/s11523-017-0543-0
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        atl: Phase IB Trial of the Anti-Cancer Stem Cell DLL4-Binding Agent Demcizumab with Pemetrexed and Carboplatin as First-Line Treatment of Metastatic Non-Squamous NSCLC.
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        au:
          McKeage, Mark J.
          Kotasek, Dusan
          Markman, Ben
          Hidalgo, Manuel
          Millward, Michael J.
          Jameson, Michael B.
          Harris, Dean L.
          Stagg, Robert J.
          Kapoun, Ann M.
          Xu, Lu
          Hughes, Brett G. M.
        affil: , University of Auckland and Auckland City Hospital, Auckland, New Zealand
      sug:
        subj:
          Antibodies, Monoclonal Therapeutic Use
          Carcinoma, Non-Small-Cell Lung Drug Therapy
          Carboplatin Therapeutic Use
          Lung Neoplasms Drug Therapy
          Human
          Female
          Adult
          Carboplatin Pharmacodynamics
          Antibodies, Monoclonal Pharmacodynamics
          Carcinoma, Non-Small-Cell Lung Pathology
          Male
          Aged
          Lung Neoplasms Pathology
          Middle Age
          Validation Studies
          Comparative Studies
          Evaluation Research
          Multicenter Studies
          Scales
          Adult: 19-44 years
          Aged: 65+ years
          Middle Aged: 45-64 years
          Female
          Male
      ab: Background: Delta-like ligand 4-Notch (DLL4-Notch) signaling contributes to the maintenance of chemotherapy-resistant cancer stem cells and tumor vasculature.Objective: This phase IB trial of demcizumab, an IgG2 humanized monoclonal antibody directed against DLL4, was undertaken to determine its maximum tolerated dose, safety, immunogenicity, preliminary efficacy, pharmacokinetics, and pharmacodynamics, combined with standard chemotherapy.Patients and Methods: Forty-six treatment-naive patients with metastatic non-squamous non-small cell lung cancer (NSCLC) were enrolled in this open-label, dose-escalation study using a standard 6 + 6 design. Demcizumab (2.5, 5.0, and 7.5 mg/kg) was given once every 3 weeks with standard doses of pemetrexed and carboplatin using a continuous (six cycles followed by demcizumab maintenance) or a truncated demcizumab regimen (four cycles followed by pemetrexed maintenance).Results: Initially, continuous demcizumab was given until progression but two patients developed grade 3 pulmonary hypertension and congestive heart failure after eight or more infusions. Thereafter, 23 patients were treated with a truncated regimen of demcizumab, which was not associated with any grade 3 or greater cardiopulmonary toxicity. Common adverse events were hypertension, raised brain natriuretic peptide, and those expected from carboplatin and pemetrexed alone. Twenty of 40 evaluable patients (50%) had objective tumor responses. In peripheral blood, demcizumab treatment modulated the expression of genes regulating Notch signaling and angiogenesis, and achieved concentrations exceeding those saturating DLL4 binding.Conclusions: This study has identified a truncated dosing regimen and recommended phase II dose of demcizumab (5 mg/kg q3-weekly ×4) for subsequent clinical evaluation in combination with standard carboplatin and pemetrexed chemotherapy. NCT01189968.
      pubtype: Academic Journal
      doctype:
        research
        Journal Article
      ougenre: Article
    language: English
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