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A randomized, open-label, 2-period crossover study was performed to evaluate the pharmacokinetic properties and bioequivalence of 2 erlotinib hydrochloride tablets (a test formulation and a reference formulation) in healthy Chinese subjects. Subjects were randomized to receive a single oral dose of the erlotinib hydrochloride test or reference formulation (150 mg) under fasting conditions. The washout period was 12 days. Blood samples were collected at scheduled time points, and plasma concentrations were determined using a high-performance liquid chromatography-tandem mass spectrometry method. A noncompartmental method was used to calculate pharmacokinetic parameters and to evaluate the bioequivalence of the 2 formulations. Safety assessments were performed during the whole study period. The results suggest that the pharmacokinetic parameter values of the test formulation were similar to those of the reference formulation. The 90% confidence intervals of the geometric least-squares mean ratios of the test to reference formulation were 94.06% to 105.43% for maximum concentration, 88.21% to 97.57% for area under the concentration-time curve to last measurement, and 87.37% to 97.14% for area under the curve extrapolated to infinity, which are all within the accepted bioequivalence range of 80% to 125%. No serious adverse events occurred during the study. These findings suggest that the 2 erlotinib hydrochloride tablets were bioequivalent in accordance with predetermined regulatory criteria.

Titel:	Pharmacokinetics and Bioequivalence Evaluation of Erlotinib Hydrochloride Tablets: Randomized, Open-Label, 2-Period Crossover Study in Healthy Chinese Subjects.
Autor/in / Beteiligte Person:	Wang, L ; Ruan, Z ; Yang, D ; Hu, Y ; Liang, J ; Chen, J ; Shao, R ; Xu, Y ; Guan, Y ; Jiang, B
Zeitschrift:	Clinical pharmacology in drug development, Jg. 10 (2021-02-01), Heft 2, S. 166-172
Veröffentlichung:	2013- : Hoboken, NJ : Wiley ; <i>Original Publication</i>: Thousand Oaks, Calif. : Sage Publications, c2012-, 2021
Medientyp:	academicJournal
ISSN:	2160-7648 (electronic)
DOI:	10.1002/cpdd.811
Schlagwort:	Adolescent Adult Area Under Curve Asian People Chromatography, High Pressure Liquid Cross-Over Studies Drugs, Generic administration & dosage Erlotinib Hydrochloride administration & dosage Female Humans Male Protein Kinase Inhibitors administration & dosage Tablets Tandem Mass Spectrometry Therapeutic Equivalency Young Adult Drugs, Generic pharmacokinetics Erlotinib Hydrochloride pharmacokinetics Protein Kinase Inhibitors pharmacokinetics
Sonstiges:	Nachgewiesen in: MEDLINE Sprachen: English Publication Type: Comparative Study; Journal Article; Randomized Controlled Trial Language: English [Clin Pharmacol Drug Dev] 2021 Feb; Vol. 10 (2), pp. 166-172. <i>Date of Electronic Publication: </i>2020 May 16. MeSH Terms: Drugs, Generic / pharmacokinetics ; Erlotinib Hydrochloride / pharmacokinetics ; Protein Kinase Inhibitors / *pharmacokinetics ; Adolescent ; Adult ; Area Under Curve ; Asian People ; Chromatography, High Pressure Liquid ; Cross-Over Studies ; Drugs, Generic / administration & dosage ; Erlotinib Hydrochloride / administration & dosage ; Female ; Humans ; Male ; Protein Kinase Inhibitors / administration & dosage ; Tablets ; Tandem Mass Spectrometry ; Therapeutic Equivalency ; Young Adult References: Jemal A, Bray F, Center MM, Ferlay J, Ward E, Forman D. Global cancer statistics. CA Cancer J Clin. 2011;61(2):69-90. ; Bray F, Ferlay J, Soerjomataram I, Siegel RL, Torre LA, Jemal A. Global cancer statistics 2018: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. CA Cancer J Clin. 2018;68(6):394-424. ; da Cunha Santos G, Shepherd FA, Tsao MS. EGFR mutations and lung cancer. Annu Rev Pathol. 2011;6:49-69. ; Blackhall FH, Shepherd FA, Albain KS. Improving survival and reducing toxicity with chemotherapy in advanced non-small cell lung cancer: a realistic goal? Treat Respir Med. 2005;4(2):71-84. ; Sörenson S, Glimelius B, Nygren P, SBU-group. Swedish Council of Technology Assessment in Health Care. A systematic overview of chemotherapy effects in non-small cell lung cancer. Acta Oncol. 2001;40(2-3):327-339. ; Liu X, Wang P, Zhang C, Ma Z. Epidermal growth factor receptor (EGFR): a rising star in the era of precision medicine of lung cancer. Oncotarget. 2017;8(30):50209-50220. ; Janne PA, Engelman JA, Johnson BE. Epidermal growth factor receptor mutations in non-small-cell lung cancer: implications for treatment and tumor biology. J Clin Oncol. 2005;23(14):3227-3234. ; Rossi A, Muscarella LA, Di Micco C, et al. Pharmacokinetic drug evaluation of osimertinib for the treatment of non-small cell lung cancer. Expert Opin Drug Metab Toxicol. 2017;13(12):1281-1288. ; Liao BC, Lin CC, Yang JC. First-line management of EGFR-mutated advanced lung adenocarcinoma: recent developments. Drugs. 2013;73(4):357-369. ; Liao BC, Lin CC, Lee JH, Yang JC. Optimal management of EGFR-mutant non-small cell lung cancer with disease progression on first-line tyrosine kinase inhibitor therapy. Lung Cancer. 2017;110:7-13. ; Uhm JE, Park BB, Ahn MJ, et al. Erlotinib monotherapy for stage IIIB/IV non-small cell lung cancer: a multicenter trial by the Korean Cancer Study Group. J Thorac Oncol. 2009;4(9):1136-1143. ; Mok T, Wu YL, Au JS, et al. Efficacy and safety of erlotinib in 1242 East/South-East Asian patients with advanced non-small cell lung cancer. J Thorac Oncol. 2010;5(10):1609-1615. ; Peters S, Zimmermann S, Adjei AA. Oral epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of non-small cell lung cancer: comparative pharmacokinetics and drug-drug interactions. Cancer Treat Rev. 2014;40(8):917-926. ; Rosell R, Carcereny E, Gervais R, et al. Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial. Lancet Oncol. 2012;13(3):239-246. ; Scheffler M, Di Gion P, Doroshyenko O, Wolf J, Fuhr U. Clinical pharmacokinetics of tyrosine kinase inhibitors: focus on 4-anilinoquinazolines. Clin Pharmacokinet. 2011;50(6):371-403. ; Frohna P, Lu J, Eppler S, et al. Evaluation of the absolute oral bioavailability and bioequivalence of erlotinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in a randomized, crossover study in healthy subjects. J Clin Pharmacol. 2006;46(3):282-290. ; Ranson M, Shaw H, Wolf J, et al. A phase I dose-escalation and bioavailability study of oral and intravenous formulations of erlotinib (Tarceva, OSI-774) in patients with advanced solid tumors of epithelial origin. Cancer Chemother Pharmacol. 2010;66(1):53-58. ; Ling J, Fettner S, Lum BL, Riek M, Rakhit A. Effect of food on the pharmacokinetics of erlotinib, an orally active epidermal growth factor receptor tyrosine-kinase inhibitor, in healthy individuals. Anticancer Drugs. 2008;19(2):209-216. ; Johnson JR, Cohen M, Sridhara R, et al. Approval summary for erlotinib for treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. Clin Cancer Res. 2005;11(18):6414-6421. ; Rakhit A, Pantze MP, Fettner S, et al. The effects of CYP3A4 inhibition on erlotinib pharmacokinetics: computer-based simulation (SimCYP) predicts in vivo metabolic inhibition. Eur J Clin Pharmacol. 2008;64(1):31-41. ; Li J, Zhao M, He P, Hidalgo M, Baker SD. Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes. Clin Cancer Res. 2007;13:3731-3737. ; Ling J, Johnson KA, Miao Z, et al. Metabolism and excretion of erlotinib, a small molecule inhibitor of epidermal growth factor receptor tyrosine kinase, in healthy male volunteers. Drug Metab Dispos. 2006;34(3):420-426. ; Petit-Jean E, Buclin T, Guidi M, et al. Erlotinib: another candidate for the therapeutic drug monitoring of targeted therapy of cancer? A pharmacokinetic and pharmacodynamic systematic review of literature. Ther Drug Monit. 2015;37(1):2-21. ; Choi HG, Jeon JY, Im YJ, et al. Pharmacokinetic properties of two erlotinib 150 mg formulations with a genetic effect evaluation in healthy Korean subjects. Clin Drug Invest. 2015;35(1):31-43. ; Solassol I, Pinguet F, Quantin X. FDA- and EMA-approved tyrosine kinase inhibitors in advanced EGFR-mutated non-small cell lung cancer: safety, tolerability, plasma concentration monitoring, and management. Biomolecules. 2019;9(11):668. Contributed Indexing: Keywords: Chinese subjects; bioequivalence; erlotinib hydrochloride; pharmacokinetics; safety Substance Nomenclature: 0 (Drugs, Generic) ; 0 (Protein Kinase Inhibitors) ; 0 (Tablets) ; DA87705X9K (Erlotinib Hydrochloride) Entry Date(s): Date Created: 20200517 Date Completed: 20211214 Latest Revision: 20221207 Update Code: 20231215

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Pharmacokinetics and Bioequivalence Evaluation of Erlotinib Hydrochloride Tablets: Randomized, Open-Label, 2-Period Crossover Study in Healthy Chinese Subjects.