Bioequivalence and Pharmacokinetic Evaluation of Regorafenib Tablets in Healthy Chinese Volunteers.

Publisher: Wiley Country of Publication: United States NLM ID: 101572899 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 2160-7648 (Electronic) Linking ISSN: 2160763X NLM ISO Abbreviation: Clin Pharmacol Drug Dev Subsets: MEDLINE

Publication: 2013- : Hoboken, NJ : Wiley
Original Publication: Thousand Oaks, Calif. : Sage Publications, c2012-

Pyridines*/pharmacokinetics ; Pyridines*/administration & dosage ; Pyridines*/adverse effects ; Phenylurea Compounds*/pharmacokinetics ; Phenylurea Compounds*/administration & dosage ; Phenylurea Compounds*/adverse effects ; Phenylurea Compounds*/blood ; Therapeutic Equivalency* ; Cross-Over Studies* ; Healthy Volunteers* ; Tablets* ; Fasting* ; Food-Drug Interactions* ; Area Under Curve*; Humans ; Male ; Adult ; Young Adult ; Administration, Oral ; Female ; Asian People ; China ; East Asian People

This was a single-center, randomized, open-label, 2-formulation, and 2-cycle crossover trial conducted in 48 healthy Chinese volunteers, under fasting and fed conditions. The participants received oral doses of the test formulation (regorafenib) and reference formulation (40 mg) during each study period. Blood samples were collected before and up to 144 hours after the formulations were administered to determine changes in the pharmacokinetic parameters and adverse reactions, which were then used to evaluate bioequivalence and safety. The geometric mean ratios of maximum blood concentration, area under the plasma concentration-time curve from time 0 to the last quantifiable concentration , and area under the plasma concentration-time curve from time 0 to infinity for regorafenib were as follows: 94.7%, 91.4%, and 91.7%, respectively, under fasting conditions; and 94.6%, 97.7%, and 98.8%, respectively, under fed conditions. The 90% confidence intervals for the geometric mean ratios were within the 80%-125% equivalence interval for both the fasting and fed tests. Ingesting high-fat and high-calorie foods increases exposure to regorafenib, leading to slower rates of absorption. The safety profiles of the 2 preparations were similar.
(© 2024, The American College of Clinical Pharmacology.)

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Keywords: bioequivalence; healthy Chinese volunteers; pharmacokinetic; regorafenib

24T2A1DOYB (regorafenib)
0 (Pyridines)
0 (Phenylurea Compounds)
0 (Tablets)

Date Created: 20241023 Date Completed: 20241202 Latest Revision: 20241202

20241204

10.1002/cpdd.1474

39439380