A Single- and Multiple-Dose Study to Evaluate the Pharmacokinetics of Fixed-Dose Grazoprevir/Elbasvir in Healthy Chinese Participants

التفاصيل البيبلوغرافية
العنوان: A Single- and Multiple-Dose Study to Evaluate the Pharmacokinetics of Fixed-Dose Grazoprevir/Elbasvir in Healthy Chinese Participants
المؤلفون: Jun Jiang, Shuang Xie, Meng Li, Yudong Wei, Hwa-Ping Feng, Haiyan Li, Xu Min Zhao, Luzelena Caro, Jacqueline B. McCrea, Zhenhua Yang, Shuang Zhang, Jiangdian Wang, Shengmei Mu, Lin Xu
المصدر: Clinical Pharmacology: Advances and Applications. 12:1-11
بيانات النشر: Informa UK Limited, 2020.
سنة النشر: 2020
مصطلحات موضوعية: medicine.medical_specialty, Elbasvir, business.industry, Multiple dose, Gastroenterology, Fixed dose, Tolerability, Pharmacokinetics, Grazoprevir, Oral administration, Internal medicine, medicine, Pharmacology (medical), business, Blood sampling
الوصف: Purpose The burden of hepatitis C virus infection is particularly high in Asian countries, and new treatments are urgently needed. The purpose of this study was to characterize the pharmacokinetics (PK) and safety of the fixed-dose combination tablet of elbasvir/grazoprevir in healthy Chinese participants. Patient and Methods In this Phase I, single-site, open-label, 3-period study in healthy Chinese adults, participants received a single tablet of elbasvir 50 mg/grazoprevir 100 mg, followed by blood sampling for up to 96 hrs (http://www.chinadrugtrials.org.cn/ CTR20160034; Protocol PN071). Participants then received 1 tablet daily for 10 days, followed by a minimum 10-day washout, after which participants received a single dose of 2 tablets (elbasvir 100 mg/grazoprevir 200 mg). Elbasvir and grazoprevir PK were assessed following single and multiple doses. Safety and tolerability were also evaluated. Results Twelve participants (50% male) were enrolled in and completed the study. Following single-dose oral administration of elbasvir 50 mg/grazoprevir 100 mg or elbasvir 100 mg/grazoprevir 200 mg, the median Tmax was 3-4 hrs and elimination half-life was 18 hrs (elbasvir) and 30 hrs (grazoprevir). Multiple-dose administration resulted in AUC0-24 accumulation ratios of 1.58 (elbasvir) and 2.35 (grazoprevir). Both elbasvir 50 mg/grazoprevir 100 mg and 100 mg/200 mg regimens were generally well tolerated. Conclusion Single-dose administration of elbasvir 50 mg/grazoprevir 100 mg or 100 mg/200 mg and once-daily administration of elbasvir 50 mg/grazoprevir 100 mg for 10 days has been adequately characterized, with PK values within the expected range, and was generally well tolerated in healthy Chinese male and female participants.
تدمد: 1179-1438
DOI: 10.2147/cpaa.s224662
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::89504977879b5fde8a3387ac929a0f97
https://doi.org/10.2147/cpaa.s224662
Rights: OPEN
رقم الانضمام: edsair.doi...........89504977879b5fde8a3387ac929a0f97
قاعدة البيانات: OpenAIRE
الوصف
تدمد:11791438
DOI:10.2147/cpaa.s224662