A randomized, crossover, phase I clinical study to evaluate bioequivalence and safety of tofacitinib and Xeljanz® in Chinese healthy subjects

Xu, Zhongnan; Wang, Yanli; Liu, Zhengzhi; Zhang, Renjie; Zhou, Yixin; Yu, Jihong; Jiang, Lan; Liang, Wenzhong; Liu, Guangwen; Qu, Xinyao; Chen, Jiahui; Su, Zhengjie; Yu, Shuang; Cheng, Yong; Wang, Wanhua; Ren, Qing; Deng, Qiaohuan; Zhao, Yicheng; Yang, Haimiao

doi:10.1016/j.intimp.2022.108780

Cited by 4 publications

(5 citation statements)

References 25 publications

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“…In our study trial, the values of C max and T max are similar to previous studies and food afection on exposure of tofacitinib. Te value of C max in average decreased by 25.90%, and it is similar to previous studies [12][13][14]. In our study, the value of AUC 0-t and AUC 0-∞ was in average increased by 16.57% and 14.08%, respectively, after a high-fat diet in the fasted state, which is similar to the previous study [13].…”

Section: Discussionsupporting

confidence: 92%

“…Te value of C max in average decreased by 25.90%, and it is similar to previous studies [12][13][14]. In our study, the value of AUC 0-t and AUC 0-∞ was in average increased by 16.57% and 14.08%, respectively, after a high-fat diet in the fasted state, which is similar to the previous study [13]. However, another study showed that a high-diet had no efect on AUC 0-t and AUC 0-∞ [14].…”

Section: Discussionsupporting

confidence: 92%

“…Previous studies demonstrated that the pharmacokinetic profle of tofacitinib is characterized by rapid absorption, T max are within 0.5-1.5 h, and t 1/2 are within 2-3.5 h [12,13]. In our study trial, the values of C max and T max are similar to previous studies and food afection on exposure of tofacitinib.…”

Section: Discussionsupporting

confidence: 89%

“…In our study trial, the value of t 1/2 was in average delayed 0.45 h after a high-fat diet, and it is diferent to the previous studies [12,14]; the previous study showed that there was no signifcant difference in the value of t 1/2 . But in another study [13], it was also proven that a high-fat diet can extend t 1/2 about 0.2 h. Overall, a high-fat diet can afect the pharmacokinetic behavior of tofacitinib. A high-fat diet can delay the absorption of tofacitinib and result in a signifcant decrease in C max , as well as a delayed in C max and an extension of t 1/2 .…”

Section: Discussionmentioning

confidence: 92%

“…Te aim of this study was to evaluate the bioequivalence between a preparation of tofacitinib citrate tablets developed by Jiangxi Qingfeng Pharmaceutical Co. Ltd. and the reference preparation of tofacitinib citrate tablets (Xeljanz ® ) developed by Pfzer Manufacturing Deutschland Gmbh in healthy Chinese volunteers and observed the safety of both. (12) difculty in blood collection, patients who cannot tolerate venipuncture, and people with a history of needle sickness and blood sickness; (13) excessive intake of tea, cofee, or other caffeinated beverage; (14) intake of drinks or foods rich in cafeine or grapefruit or ingesting any beverage or food rich in cafeine or grapefruit within 48 hours before the frst administration of the study; (15) ingestion of drugs within 30 days before study drug administration; and (16) pregnancy or lactation.…”

Section: Introductionmentioning

confidence: 99%

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Bioequivalence and Safety of Two Formulations of Tofacitinib Citrate Tablets in Healthy Chinese Volunteers under Fasting and Fed Conditions: Randomized, Open-Label, 2-Period, Single-Dose, Crossover Trials

Liu,

Ning,

Shi

et al. 2024

Journal of Clinical Pharmacy and Therapeutics

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Purpose. To evaluate the bioequivalence of two different tofacitinib citrate tablets formulations among healthy Chinese subjects under fasting and fed conditions and to observe the safety of test preparation and reference preparation in healthy subjects. Method. This randomized, open-label, 2-period, crossover, bioequivalence study included 64 healthy Chinese subjects (fasting: n = 32, fed: n = 32). The subjects were assigned to receive a single 5-mg dose of the test or a reference tofacitinib citrate tablets. Blood samples were collected at predose and up to 24 hours after dosing. Area under the plasma concentration time curve from zero to the last measurable concentration (AUC0-t), the area from time zero to infinite (AUC0-∞), and maximum plasma concentration (Cmax) were used for bioequivalence assessment. Safety assessment was conducted by vital signs, physical examination, laboratory examination, and 12-lead electrocardiogram during the study, from the time the subject receiving the test drug to the end of the last visit. Results. Under fed condition, the 90% CIs of the geometric mean ratios of the test/reference for tofacitinib citrate tablets were 98.40–104.16% for AUC0-t, 89.96–116.70% for Cmax, and 98.50–104.15% for AUC0-∞. Under fasting condition, the 90% CIs of the geometric mean ratios of the test/reference for tofacitinib citrate tablets were 93.65–101.60% for AUC0-t, 90.06–109.15% for Cmax, and 93.88–101.51% for AUC0-∞. There were no serious events. Conclusion. The 90% CI for the geometric mean ratio (test/reference) of Cmax, AUC0-t, and AUC0-∞ were within the range of 80.00%–125.00%, indicating that the test formulation was equivalent to the reference formulation in healthy Chinese subjects under both fasting and fed conditions. They are similar in terms of safety. This trial is registered with CTR20190366.

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