A Bioequivalence Study of Avanafil in Healthy Chinese Male Subjects Under Fasting and Fed Conditions: Results of a Randomized, Open‐Label, Single‐Dose, 2‐Sequence, 2‐Period Crossover Study

Abstract

This bioequivalence study was conducted to determine the pharmacokinetics and safety profiles of an originator and a generic avanafil formulation in Chinese male subjects under fed and fasting conditions. Each eligible subject was initially randomly given avanafil (200 mg) in a test-reference or reference-test order, before being switched to another study drug sequence after 7 drug-free days. The bioequivalence of test and reference avanafil were determined if the 90%CIs of the geometric mean ratio (GMR) for the area under plasma concentration-time curve (AUC) from time 0 to infinity (AUC 0-∞ ), AUC from time 0 to the last detectable concentration (AUC 0-t ), and the maximum plasma concentration (C max ) fell within the range 80%-125%. Under fasting/fed conditions, the 90%CIs of GMR for AUC 0-∞ , AUC 0-t , and C max were 98.9% to 109.5%/96.0% to 101.2%, 99.6% to 110.3%/96.6% to 102.4%, and 99.3% to 116.8%/94.3% to 106.7%, respectively, which were all within the 80%-125% range. Adverse events (AEs) occurred in 20.8% of subjects under fasting conditions and 20.7% of subjects under fed conditions, with a severity of grade 1. No significant difference was found in the rate of occurrence of AEs and drug-related AEs in the test and reference-avanafil groups (all P > .05). We concluded that the test and reference avanafil were bioequivalent in healthy Chinese male subjects under fasting and fed conditions.

Characteristics and Analytical Methods of Novel PDE5 Inhibitor Avanafil: An Update

“…In the literature survey, eleven methods [44,[49][50][51][52][53][54][55][57][58][59] found to be published based on LC-MS techniques for different matrices. Coupling of MS to chromatographic techniques has always been attractive due to the sensitive and exceptionally explicit nature of MS contrasted with other chromatographic detectors [72,73,74].…”