The effect of food on the pharmacokinetics of Sutetinib maleate capsule, an irreversible EGFR tyrosine kinase inhibitor, in healthy Chinese subjects.
Sutetinib is an irreversible inhibitor of epidermal growth factor receptor (EGFR) and showed favorable efficacy and safety in patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) harbouring nondrug-resistant rare EGFR mutations. To evaluate the potential food effect, eight...
| Publicado en: | Investigational New Drugs Vol. 42; no. 3; pp. 289 - 299 |
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| Autores principales: | , , , , , , , , , , |
| Formato: | research tables/charts randomized controlled trial Journal Article |
| Publicado: |
Springer Nature
Jun2024
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| Acceso en línea: | Ver este registro en EBSCOhost |
| fields | @attributes: recordID: 1 pdfLink: plink: https://search.ebscohost.com/login.aspx?direct=true&db=ccm&AN=177775709&site=ehost-live header: @attributes: shortDbName: ccm uiTerm: 177775709 longDbName: CINAHL Complete uiTag: AN controlInfo: bkinfo: dissinfo: jinfo: jid: 01676997 OH2 jtl: Investigational New Drugs issn: 01676997 maglogo: N pubinfo: dt: Jun2024 vid: 42 iid: 3 pid: 237 pub: Springer Nature place: New York, New York artinfo: ui: 177775709 176521382 177775709 177775709 10.1007/s10637-024-01436-0 177775709 ppf: 289 ppct: 10 formats: tig: atl: The effect of food on the pharmacokinetics of Sutetinib maleate capsule, an irreversible EGFR tyrosine kinase inhibitor, in healthy Chinese subjects. aug: au: Cao, Bei Ma, Tingting Zhang, Yuqiang Huang, Lei Lin, Hui Jiang, Huanhuan Zhao, Yu Geng, Yan Yang, Yuanxun Cao, Sumin Li, Juan affil: Phase I Clinical Trials Unit, Affiliated Hospital of Medical School, Nanjing Drum Tower Hospital, Nanjing University, Zhongshan Road 321#, Gulou District, 210008, Nanjing, China sug: subj: Drug-Food Interactions Protein Kinase Inhibitors Pharmacokinetics Tyrosine Kinase Inhibitors Pharmacokinetics Chinese Persons Epidermal Growth Factor Receptors Food Patient Safety Human Randomized Controlled Trials Crossover Design Protein Kinase Inhibitors Administration and Dosage Liquid Chromatography-Mass Spectrometry Descriptive Statistics Confidence Intervals Random Assignment Funding Source ab: Sutetinib is an irreversible inhibitor of epidermal growth factor receptor (EGFR) and showed favorable efficacy and safety in patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) harbouring nondrug-resistant rare EGFR mutations. To evaluate the potential food effect, eighteen healthy Chinese subjects were enrolled in a single-centre, randomized, open-label, two-sequence, two-period crossover study. Sutetinib was administered as a single oral 100 mg under fasting or fed conditions, and pharmacokinetic sampling was performed following each dose and analysed by a validated liquid chromatography/mass spectrometry method. Safety and tolerability were also evaluated. Food intake slightly decreased maximum plasma concentration (Cmax) and area under the plasma concentration-time curve from time 0 to infinity (AUC0 − inf) of sutetinib (geometric least-squares mean [GLSM] ratio, 80.94% and 86.11%; 90% confidence interval [CI], 68.43–95.72 and 75.88–97.73) and its active metabolite sutetinib N-Oxide (GLSM ratio, 75.58% and 84.00%; 90% CI, 65.69–86.95 and 75.42–93.56), respectively. In addition, the time to maximum plasma concentration (Tmax) of both sutetinib and its metabolite has been prolonged by 2 h under fed conditions. A total of 31 adverse events (AEs) occurred during the study, with no serious adverse events (SAE) reported, and no obvious difference was observed between the fasting and fed groups. Our results demonstrated that a high-fat and high-calorie diet caused a significant delay in drug absorption and a marginal reduction in drug exposure. Sutetinib was generally well tolerated in healthy Chinese subjects. (This trial was registered at http://www.chinadrugtrials.org.cn. The registration No. is CTR20201933, and the date of registration is 2020-10-16). Clinical trials registration number: CTR20201933 (http://www.chinadrugtrials.org.cn/) or ChiCTR2100045180 (https://www.chictr.org.cn/). pubtype: Academic Journal doctype: research tables/charts randomized controlled trial Journal Article ougenre: Article language: English refInfo: holdings: @attributes: islocal: N |
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