The Effect of CYP3A Genetic Polymorphism on the Pharmacokinetics of Phosphodiesterase type5 Inhibitors in Male Subjects (CYP3APDE5I)

Inje University

Status and phase: Completed; Phase 1

Conditions: Pharmacokinetics of Three PDE5Is; Healthy Subjects; Genetic Polymorphic CYP3A5

Treatments: Drug: phosphodiesterase type 5 inhibitor

Study type: Interventional

Funder types: Other

Identifiers

NCT00767598

07-109

Details and patient eligibility

About

In order to evaluate the effect of CYP3A5*3 allele on the pharmacokinetics of sildenafil, udenafil, and vardenafil, the clinical trial using a single oral dose was conducted in Korean healthy male subjects whose genotype of CYP3A5 had been determined.

Full description

The aim of this study is to evaluate the different effect of the CYP3A5 genotype on the pharmacokinetics(PK) of sildenafil, udenafil, and vardenafil in healthy male subjects. Twenty one healthy male subjects with CYP3A5*1/*1, *1/*3, or *3/*3 were enrolled. An open-label 3-way crossover study was performed with a week washout. A single oral dose of PDE5I (100 mg sildenafil; 200 mg udenafil; 20 mg vardenafil) was administered, respectively. After a single oral dose of phosphodiesterase type 5 inhibitor (PDE5I), plasma levels of the parent and the major metabolite were measured up to 24 or 48 h.

Enrollment: 21 patients

Sex: Male

Ages: 20+ years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

• Healthy male subject whose CYP3A5 genotype was determined

Exclusion criteria

• Subject whose CYP3A5 genotype was not determined

Trial design

Primary purpose: Basic Science

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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21 participants in 3 patient groups

A

Active Comparator group

Description:

Vardenafil

Treatment:

Drug: phosphodiesterase type 5 inhibitor

Drug: phosphodiesterase type 5 inhibitor

Drug: phosphodiesterase type 5 inhibitor

B

Active Comparator group

Description:

Sildenafil

Treatment:

Drug: phosphodiesterase type 5 inhibitor

Drug: phosphodiesterase type 5 inhibitor

Drug: phosphodiesterase type 5 inhibitor

C

Active Comparator group

Description:

Udenafil

Treatment:

Drug: phosphodiesterase type 5 inhibitor

Drug: phosphodiesterase type 5 inhibitor

Drug: phosphodiesterase type 5 inhibitor