Pharmacokinetics of afatinib, a selective irreversible ErbB family blocker, in patients with advanced solid tumours

Clinical Pharmacokinetics

Volumn 52, Issue 12, 2013, Pages 1101-1109

  Wind, Sven ^a   Schmid, Marion ^a   Erhardt, Julia ^a   Goeldner, Rainer Georg ^a   Stopfer, Peter ^a  

^a BOEHRINGER INGELHEIM PHARMA GMBH AND CO KG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

AFATINIB;

ADULT; AGED; AREA UNDER THE CURVE; ARTICLE; BREAST CARCINOMA; COLORECTAL CANCER; DIARRHEA; DISEASE SEVERITY; DISTRIBUTION VOLUME; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE INCREASE; DRUG HALF LIFE; ESOPHAGUS CANCER; FEMALE; HEAD AND NECK CANCER; HUMAN; LUNG NON SMALL CELL CANCER; MAJOR CLINICAL STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; METASTASIS; MONOTHERAPY; MULTIPLE CYCLE TREATMENT; OVARY CANCER; PHASE 1 CLINICAL TRIAL; PHASE 2 CLINICAL TRIAL; PRIORITY JOURNAL; RASH; SOLID TUMOR; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADOLESCENT; ADULT; AGED; AGED, 80 AND OVER; ANTINEOPLASTIC AGENTS; FEMALE; HUMANS; MALE; MIDDLE AGED; NEOPLASMS; PROTEIN KINASE INHIBITORS; QUINAZOLINES; RECEPTOR, ERBB-2; YOUNG ADULT;

EID: 84885994849     PISSN: 03125963     EISSN: 11791926     Source Type: Journal    
DOI: 10.1007/s40262-013-0091-4     Document Type: Article

References (28)

1. 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.
2. 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.
3. 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.
4. 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.
5. 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.
6. 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.
7. 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).
8. 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.
9. 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.
10. 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).
11. 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.
12. 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.
13. 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.
14. 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.
15. 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.
16. 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).
17. 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.
18. Smith BP, Vandenhende FR, DeSante KA, et al. Confidence interval criteria for assessment of dose proportionality. Pharm Res. 2000;17(10):1278-83.
19. 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.
20. 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.
21. 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.
22. Hidalgo M, Bloedow D. Pharmacokinetics and pharmacodynamics: maximizing the clinical potential of erlotinib (Tarceva). Semin Oncol. 2003;30(3 Suppl 7):25-33.
23. 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.
24. van Erp NP, Gelderblom H, Guchelaar HJ. Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009;35(8):692-706.
25. 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.
26. 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.
27. 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.
28. 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.