[{"data":1,"prerenderedAt":-1},["ShallowReactive",2],{"detail-sidebar-cat-0-en-105":3,"doc-seo-411157-105":59,"doc-detail-411157-en":130},{"code":4,"msg":5,"data":6},0,"success",[7,13,18,23,28,33,38,43,48,51,55],{"id":8,"doc_module":4,"doc_module_name":9,"category_name":10,"show_sort_weight":11,"slug":12},1,"Document","Story & Novel",90,"story-novel",{"id":14,"doc_module":4,"doc_module_name":9,"category_name":15,"show_sort_weight":16,"slug":17},2,"Literature",80,"literature",{"id":19,"doc_module":4,"doc_module_name":9,"category_name":20,"show_sort_weight":21,"slug":22},4,"Exam",70,"exam",{"id":24,"doc_module":4,"doc_module_name":9,"category_name":25,"show_sort_weight":26,"slug":27},5,"Comic",60,"comic",{"id":29,"doc_module":4,"doc_module_name":9,"category_name":30,"show_sort_weight":31,"slug":32},6,"Technology",50,"technology",{"id":34,"doc_module":4,"doc_module_name":9,"category_name":35,"show_sort_weight":36,"slug":37},7,"Healthcare",40,"healthcare",{"id":39,"doc_module":4,"doc_module_name":9,"category_name":40,"show_sort_weight":41,"slug":42},8,"Research & Report",30,"research-report",{"id":44,"doc_module":4,"doc_module_name":9,"category_name":45,"show_sort_weight":46,"slug":47},9,"Religion & Spirituality",20,"religion-spirituality",{"id":46,"doc_module":4,"doc_module_name":9,"category_name":49,"show_sort_weight":46,"slug":50},"World Cup","world-cup",{"id":52,"doc_module":4,"doc_module_name":9,"category_name":53,"show_sort_weight":52,"slug":54},10,"Lifestyle","lifestyle",{"id":56,"doc_module":4,"doc_module_name":9,"category_name":57,"show_sort_weight":24,"slug":58},19,"General","general",{"code":4,"msg":60,"data":61},"ok",{"site_id":62,"language":63,"slug":64,"title":65,"keywords":66,"description":67,"schema_data":68,"social_meta":123,"head_meta":125,"extra_data":127,"updated_unix":129},105,"en","pharmacokinetics-and-safety-of-the-antitumor-drug-everolimus-in-healthy-chinese-subjects-a-single-dose-open-label-randomized-two-sequence-two-period-crossover-phase-i-bioequivalence-study","Pharmacokinetics and safety of the antitumor drug everolimus in healthy Chinese subjects - a single-dose, open-label, randomized, two-sequence, two-period crossover, phase I bioequivalence study","","Purpose: Evaluate pharmacokinetic (PK) similarity and safety of everolimus in whole blood under fasting versus postprandial conditions, and assess bioequivalence of a generic versus reference formulation in Chinese healthy subjects. Methods: Conducted a single-dose, open-label, randomized, two-sequence, two-period crossover study (CTR20220446) with fasting and fed arms, measuring everolimus concentrations using validated LC-MS/MS. Results: 90% CIs for geometric mean ratios of Cmax, AUC0-t, and AUC0-∞ stayed within 80.00%–125.00%; Tmax decreased with food, and no serious adverse events occurred. Conclusion: Fed state reduced systemic availability of a 5 mg dose, while test and reference formulations were bioequivalent.",{"@graph":69,"@context":122},[70,84,105],{"@type":71,"itemListElement":72},"BreadcrumbList",[73,77,79,82],{"item":74,"name":75,"@type":76,"position":8},"https://docshare.wps.com","Home","ListItem",{"item":78,"name":9,"@type":76,"position":14},"https://docshare.wps.com/document/",{"item":80,"name":35,"@type":76,"position":81},"https://docshare.wps.com/document/healthcare/",3,{"item":83,"name":65,"@type":76,"position":19},"https://docshare.wps.com/document/pharmacokinetics-and-safety-of-the-antitumor-drug-everolimus-in-healthy-chinese-subjects-a-single-dose-open-label-randomized-two-sequence-two-period-crossover-phase-i-bioequivalence-study/411157/",{"url":83,"name":65,"@type":85,"image":86,"author":91,"headline":65,"publisher":94,"fileFormat":97,"inLanguage":63,"description":67,"dateModified":98,"datePublished":99,"encodingFormat":97,"isAccessibleForFree":100,"interactionStatistic":101},"DigitalDocument",{"url":87,"@type":88,"width":89,"height":90},"https://docshare.wps.com/thumbnails/pharmacokinetics-and-safety-of-the-antitumor-drug-everolimus-in-healthy-chinese-subjects-a-single-dose-open-label-randomized-two-sequence-two-period-crossover-phase-i-bioequivalence-study/411157.png","ImageObject",300,407,{"name":92,"@type":93},"Nguyễn Văn Học","Person",{"url":74,"name":95,"@type":96},"DocShare","Organization","application/pdf","2026-10-29","2026-09-28",true,{"@type":102,"interactionType":103,"userInteractionCount":24},"InteractionCounter",{"@type":104},"ViewAction",{"@type":106,"mainEntity":107},"FAQPage",[108,114,118],{"name":109,"@type":110,"acceptedAnswer":111},"What is the purpose of this everolimus phase I study in healthy Chinese subjects?","Question",{"text":112,"@type":113},"The study evaluates PK similarity and safety under fasting and postprandial conditions and compares bioequivalence between a test formulation and a reference formulation.","Answer",{"name":115,"@type":110,"acceptedAnswer":116},"How was everolimus pharmacokinetics measured, and what study design was used?",{"text":117,"@type":113},"Healthy subjects received single-dose everolimus in a randomized, open-label, two-sequence, two-period crossover design. Blood everolimus concentrations were quantified using validated LC-MS/MS.",{"name":119,"@type":110,"acceptedAnswer":120},"What effect did food have on everolimus exposure, and were test and reference formulations bioequivalent?",{"text":121,"@type":113},"Food intake decreased exposure, reflected by a later Tmax after a high-fat meal. The 90% confidence intervals for Cmax, AUC0-t, and AUC0-∞ geometric mean ratios were within 80.00%–125.00%, supporting bioequivalence.","https://schema.org",{"og:url":83,"og:type":124,"og:title":65,"og:site_name":95,"og:description":67},"article",{"robots":126,"canonical":83},"index,follow",{"doc_id":128,"site_id":62},411157,1790694216,{"code":4,"msg":5,"data":131},{"doc_id":128,"user_id":132,"nickname":92,"user_avatar":133,"doc_module":4,"category_id":34,"category_name":35,"doc_title":65,"doc_description":67,"doc_content":134,"file_id":135,"file_url":136,"file_type":137,"file_size":138,"view_count":24,"is_deleted":4,"is_public":8,"is_downloadable":8,"audit_status":8,"page_count":44,"language":139,"language_code":63,"site_id":62,"html_lang":63,"table_of_contents":140,"faqs":141,"seo_title":142,"seo_description":67,"update_tm":143,"read_time":144,"preview_page_count":4},1374402739827,"https://ap-avatar.wpscdn.com/avatar/14000c97e7351f1a627?x-image-process=image/resize,m_fixed,w_180,h_180&k=1787885694763230660","TYPE Clinical Trial  \nPUBLISHED 18 December 2025 DOI 10.3389/fphar.2025.1718032  \nOPEN ACCESS  \nEDITED BY  \nKhosrow Kashfi,  \nCity University of New York, United States  \nREVIEWED BY  \nPing Du,  \nCapital Medical University, China Cody J. Peer,  \nAmgen, United States  \n*CORRESPONDENCE  \nHong Zhang,  \n [ZLhospital@163.com](ZLhospital@163.com)  \nRECEIVED 03 October 2025  \nREVISED 29 November 2025  \nACCEPTED 08 December 2025  \nPUBLISHED 18 December 2025  \nCITATION  \nChen X, Yi X, Liu Y, Wang X, Peng Y, Wang Q, Shuai Y and Zhang H (2025) Pharmacokineticsand safety of the antitumor drug everolimus in healthy Chinese subjects: a single-dose, openlabel, randomized, two-sequence, two-period crossover, phase I bioequivalence study.  \nFront. Pharmacol. 16:1718032 .  \ndoi: 10.3389/fphar.2025.1718032  \nCOPYRIGHT  \n© 2025 Chen, Yi, Liu, Wang, Peng, Wang, Shuai and Zhang. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY) . The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.  \nPharmacokinetics and safety of the antitumor drug everolimus in healthy Chinese subjects: a single-dose, open-label, randomized, two-sequence, two-period crossover, phase Ibioequivalence study  \nXiaodan Chen 1, Xiaoyi Yi 1, Yuting Liu 1, Xiaosong Wang 1,  \nYahui Peng 1, Qiong Wang 1, Ying Shuai 1 and Hong Zhang 􀀁 1,2*  \n1Clinical Medicine Research Center, Jiangxi Cancer Hospital & Institute (The Second Affiliated Hospital of Nanchang Medical College), Nanchang, China, 2Jiangxi Key Laboratory of Translational Research for Cancer, Jiangxi Clinical Research Center for Cancer, Nanchang, China  \nPurpose: It aims to evaluate the pharmacokinetic (PK) similarity and safety of everolimus in whole blood under fasting and postprandial conditions and its generics in Chinese healthy subjects.  \nMethods: Healthy subjects were enrolled in a single-dose, open-label, randomized, two-sequence, two-period crossover study (Clinical trial registry number: CTR20220446) under fasting and postprandial conditions. The blood concentration of everolimus was quantified by a validated and robust liquid chromatography-tandem mass spectrometry (LC-MS/MS) method.  \nResults: All 90% CIs for the geometric mean ratios of Cmax, AUC0-t, and AUC0−∞ were within the bioequivalence range of 80 . 00%–125 . 00% . the maximum intraindividual CV% of variation were 22.76% and 18.63% under fasting and fed conditions, respectively. The gastrointestinal absorption rate was decreased by food intake: median Tmax was 0 .75 h in the fasted state, and 3 . 00 h after a high-fat meal. The average elimination half-life (t1/2β, 37.19–38.43 h) and mean residence time (MRT, 23.13–25.81 h) did not appear to be affected by food intake regardless of fasting or fed state. In this study, no serious AE (SAEs) were observed throughout the trial.  \nConclusion: The systemic availability of a single oral 5 mg dose of everolimus is significantly reduced by coadministration with fed compared with fasting conditions, the test formulation (T) and the reference formulation (R) were bioequivalent.  \nClinical Trial Registration: [clinicaltrials.gov](clinicaltrials.gov), identifier CTR20220446, ([http://](http://)[ ](http://)[www.chinadrugtrials.org.cn/clinicaltrials.searchlist.dhtml](www.chinadrugtrials.org.cn/clinicaltrials.searchlist.dhtml)) .  \nKEYWORDS  \nbioequivalence, everolimus, healthy subject, pharmacokinetics, the antitumor drug  \nFrontiers in Pharmacology 01 [frontiersin.org](frontiersin.org)  \n1 Introduction  \nEverolimus, a mammalian target of rapamycin (mTOR) inhibitor, achieves triple anti-tumor effects by blocking the PI3KAKT-mTOR signaling pathway: inhibiting tumor cell growth, reducing tumor ce","cbCaimMJ0FvkkxCN","https://ap.wps.com/l/cbCaimMJ0FvkkxCN","pdf",1158990,"English","# Introduction\n## Everolimus background and prior evidence\n# Purpose\n# Methods\n## Study design and analytical method\n# Results\n## Bioequivalence outcomes and food effects\n## Safety findings\n# Conclusion\n# Clinical trial registration","[{\"question\":\"What is the purpose of this everolimus phase I study in healthy Chinese subjects?\",\"answer\":\"The study evaluates PK similarity and safety under fasting and postprandial conditions and compares bioequivalence between a test formulation and a reference formulation.\"},{\"question\":\"How was everolimus pharmacokinetics measured, and what study design was used?\",\"answer\":\"Healthy subjects received single-dose everolimus in a randomized, open-label, two-sequence, two-period crossover design. Blood everolimus concentrations were quantified using validated LC-MS/MS.\"},{\"question\":\"What effect did food have on everolimus exposure, and were test and reference formulations bioequivalent?\",\"answer\":\"Food intake decreased exposure, reflected by a later Tmax after a high-fat meal. The 90% confidence intervals for Cmax, AUC0-t, and AUC0-∞ geometric mean ratios were within 80.00%–125.00%, supporting bioequivalence.\"}]","Pharmacokinetics and safety of the antitumor drug everolimus in healthy Chinese subjects - a single-dose, open-label, randomized, two-sequence, two-period crossover, phase I bioequivalence study | PDF",1790587661,23]