Pharmacokinetics of Afatinib, a Selective Irreversible ErbB Family Blocker, in Patients with Advanced Solid Tumours (original) (raw)

• Li D, Ambrogio L, Shimamura T, et al. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene. 2008;27(34):4702–11.
  Article CAS PubMed Google Scholar
• Solca F, Dahl G, Zoephel A, et al. Target binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blocker. J Pharmacol Exp Ther. 2012;343(2):342–50.
  Article CAS PubMed Google Scholar
• Eskens FA, Mom CH, Planting AS, et al. A phase I dose escalation study of BIBW 2992, an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinase in a 2-week on, 2-week off schedule in patients with advanced solid tumours. Br J Cancer. 2008;98(1):80–5.
  Article CAS PubMed Google Scholar
• Marshall J, Hwang J, Eskens FA, et al. A phase I, open-label, dose escalation study of afatinib, in a 3-week-on/1-week-off schedule in patients with advanced solid tumors. Invest New Drugs. 2013;31(2):399–408.
  Article CAS PubMed Google Scholar
• Yap TA, Vidal L, Adam J, et al. Phase I trial of the irreversible EGFR and HER2 kinase inhibitor BIBW 2992 in patients with advanced solid tumors. J Clin Oncol. 2010;28(25):3965–72.
  Article CAS PubMed Google Scholar
• Gordon MS, Mendelson DS, Gross M, et al. A phase I, open-label, dose-escalation study of continuous once-daily oral treatment with afatinib in patients with advanced solid tumors. Invest New Drugs. 2013;31(2):409–16.
  Article CAS PubMed Google Scholar
• Kristeleit H, Puglisi M, Middleton GW, et al. Phase II, open-label trial to assess the effect of continuous oral afatinib (BIBW 2992) at a daily dose of 50 mg on QTc, pharmacokinetics, and efficacy in relapsed or refractory solid tumors including brain metastases and glioblastoma that is not amenable to other therapy [abstract no. 2613]. J Clin Oncol. 2011;29:15 (Suppl).
  Google Scholar
• Ang J, Mikropoulos C, Stavridi F, et al. A phase I study of daily BIBW 2992, an irreversible EGFR/HER-2 dual kinase inhibitor, in combination with weekly paclitaxel [abstract]. J Clin Oncol. 2009;27(15):e14541.
  Google Scholar
• Awada AH, Dumez H, Hendlisz A, et al. Phase I study of pulsatile 3-day administration of afatinib (BIBW 2992) in combination with docetaxel in advanced solid tumors. Invest New Drugs. 2013;31(3):734–41.
  Article CAS PubMed Google Scholar
• Bahleda R, Soria J, Berge Y, et al. Phase I trial assessing safety and pharmacokinetics of afatinib (BIBW 2992) with intravenous weekly vinorelbine in advanced solid tumors [abstract no. 2585]. J Clin Oncol. 2011;29:15 (Suppl).
  Google Scholar
• Vermorken JB, Rottey S, Ehrnrooth E, et al. A phase Ib, open-label study to assess the safety of continuous oral treatment with afatinib in combination with two chemotherapy regimens: cisplatin plus paclitaxel and cisplatin plus 5-fluorouracil, in patients with advanced solid tumors. Ann Oncol. 2013;24(5):1392–400.
  Article CAS PubMed Google Scholar
• Miller VA, Hirsh V, Cadranel J, et al. Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trial. Lancet Oncol. 2012;13(5):528–38.
  Article CAS PubMed Google Scholar
• Yang JC, Shih JY, Su WC, et al. Afatinib for patients with lung adenocarcinoma and epidermal growth factor receptor mutations (LUX-Lung 2): a phase 2 trial. Lancet Oncol. 2012;13(5):539–48.
  Article CAS PubMed Google Scholar
• Cohen EEW, Fayette J, Cupissol D, et al. A randomized, open-label, phase II study of afatinib (BIBW 2992) versus cetuximab in recurrent or metastatic squamous cell carcinoma of the head and neck: final data [abstract PP101]. Eur Arch Otorhinolaryngol. 2012;269(4):1374.
  Google Scholar
• Lin NU, Winer EP, Wheatley D, et al. A phase II study of afatinib (BIBW 2992), an irreversible ErbB family blocker, in patients with HER2-positive metastatic breast cancer progressing after trastuzumab. Breast Cancer Res Treat. 2012;133(3):1057–65.
  Article CAS PubMed Google Scholar
• Sequist LV, Yang JC, Yamamoto N, et al. Phase III study of afatinib or cisplatin/pemetrexed in metastatic lung adenocarcinoma patients with epidermal growth factor receptor mutations. J Clin Oncol. 2013 (in press).
• Stopfer P, Marzin K, Narjes H, et al. Afatinib pharmacokinetics and metabolism after oral administration to healthy male volunteers. Cancer Chemother Pharmacol. 2012;69(4):1051–61.
  Article CAS PubMed Google Scholar
• Smith BP, Vandenhende FR, DeSante KA, et al. Confidence interval criteria for assessment of dose proportionality. Pharm Res. 2000;17(10):1278–83.
  Article CAS PubMed Google Scholar
• Heise T, Graefe-Mody EU, Huttner S, et al. Pharmacokinetics, pharmacodynamics and tolerability of multiple oral doses of linagliptin, a dipeptidyl peptidase-4 inhibitor in male type 2 diabetes patients. Diabetes Obes Metab. 2009;11(8):786–94.
  Article CAS PubMed Google Scholar
• Baselga J, Rischin D, Ranson M, et al. Phase I safety, pharmacokinetic, and pharmacodynamic trial of ZD1839, a selective oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with five selected solid tumor types. J Clin Oncol. 2002;20(21):4292–302.
  Article CAS PubMed Google Scholar
• Ranson M, Hammond LA, Ferry D, et al. ZD1839, a selective oral epidermal growth factor receptor–tyrosine kinase inhibitor, is well tolerated and active in patients with solid, malignant tumors: results of a phase I trial. J Clin Oncol. 2002;20(9):2240–50.
  Article CAS PubMed Google Scholar
• Hidalgo M, Bloedow D. Pharmacokinetics and pharmacodynamics: maximizing the clinical potential of erlotinib (Tarceva). Semin Oncol. 2003;30(3 Suppl 7):25–33.
  Article CAS PubMed Google Scholar
• Burris HA III, Hurwitz HI, Dees EC, et al. Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas. J Clin Oncol. 2005;23(23):5305–13.
  Article CAS PubMed Google Scholar
• van Erp NP, Gelderblom H, Guchelaar HJ. Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009;35(8):692–706.
  Article PubMed Google Scholar
• Hirsh V. Managing treatment-related adverse events associated with EGFR tyrosine kinase inhibitors in advanced non-small-cell lung cancer. Curr Oncol. 2011;18(3):126–38.
  Article CAS PubMed Google Scholar
• Bruno R, Mass RD, Jones C, et al. Preliminary population pharmacokinetics (PPK) and exposure–safety (E–S) relationships of erlotinib HCL in patients with metastatic breast cancer (MBC) [abstract no. 823]. Proc Am Soc Clin Oncol. 2003;22.
• Lu JF, Eppler SM, Wolf J, et al. Clinical pharmacokinetics of erlotinib in patients with solid tumors and exposure–safety relationship in patients with non-small cell lung cancer. Clin Pharmacol Ther. 2006;80(2):136–45.
  Article CAS PubMed Google Scholar
• Thomas F, Rochaix P, White-Koning M, et al. Population pharmacokinetics of erlotinib and its pharmacokinetic/pharmacodynamic relationships in head and neck squamous cell carcinoma. Eur J Cancer. 2009;45(13):2316–23.
  Article CAS PubMed Google Scholar