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Safety, tolerability and pharmacokinetics of udenafil, a novel PDE-5 inhibitor, in healthy young Korean subjects

Cited 47 time in Web of Science Cited 51 time in Scopus
Authors
Kim, Bo-Hyung; Lim, Hyeong-Seok; Chung, Jae-Yong; Kim, Jung-Ryul; Lim, Kyoung Soo; Sohn, Dong-Ryul; Cho, Joo-Youn; Yu, Kyung-Sang; Shin, Sang-Goo; Paick, Jae-Seung; Jang, In-Jin
Issue Date
2008-03-06
Publisher
Wiley-Blackwell
Citation
Br J Clin Pharmacol. 2008;65(6):848-854
Keywords
Administration, OralAdultArea Under CurveDose-Response Relationship, DrugDouble-Blind MethodErectile Dysfunction/*drug therapyHumansKoreaMalePenile Erection/*drug effectsPhosphodiesterase Inhibitors/adverse effects/chemistry/*pharmacokineticsPyrimidines/adverse effects/chemistry/*pharmacokinetics
Abstract
WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT: The phosphodiesterase (PDE) type 5 inhibitor is a widely used agent that facilitates penile erection. Udenafil is newly developed as a PDE-5 inhibitor. WHAT THIS STUDY ADDS: This is the first study to determine the safety, tolerability and pharmacokinetics of udenafil in healthy subjects. Udenafil was safe and well tolerated in healthy Korean subjects. The AUC and C(max) of udenafil increased supraproportionally with increasing dose upon single administration, but there was no significant drug accumulation upon multiple administrations. AIM: To evaluate the safety, tolerability and pharmacokinetics (PK) of udenafil, a novel phosphodiesterase type 5 inhibitor. METHODS: A double-blind, randomized, placebo-controlled, dose-rising, parallel-group, single- and multiple-dose study was conducted in healthy Korean subjects. The subjects were allocated to single-dose groups of 25, 50, 100, 200 or 300 mg (eight subjects in each dose group, including two placebos), or to multiple-dose groups of 100 or 200 mg (once-daily dosing for 7 days; nine subjects in each dose group, including three placebos). Serial samples of blood and urine were collected after oral administration and the drug concentrations in plasma and urine were determined by high-performance liquid chromatography. Safety and tolerability were evaluated by monitoring clinical laboratory parameters and adverse events. RESULTS: Udenafil reached peak plasma concentrations at 0.8-1.3 h, and then declined mono-exponentially with a terminal half-life of 7.3-12.1 h in the single-dose study. The area under the time-concentration curves (AUC) and maximum plasma concentrations (C(max)) increased supraproportionally with increasing dose in the single-dose study. During multiple dosing, a steady state was reached at 5 days and little accumulation occurred after repeated dosing for 7 days. Udenafil was generally well tolerated in these healthy subjects, and no serious adverse events occurred. CONCLUSIONS: Udenafil was safe and well tolerated in healthy volunteers. The AUC and C(max) of udenafil increased supraproportionally with increasing dose upon single administration, but there was no significant drug accumulation upon multiple administrations.
ISSN
1365-2125 (Electronic)
Language
English
URI
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=18318773

http://hdl.handle.net/10371/68085
DOI
https://doi.org/10.1111/j.1365-2125.2008.03107.x
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College of Medicine/School of Medicine (의과대학/대학원)Urology (비뇨기과학전공)Journal Papers (저널논문_비뇨기과학전공)
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