Transport of a new erectogenic udenafil in Caco-2 cells
- Authors
- Ji, HY[Ji, Hye Young]; Shim, HJ[Shim, Hyun Joo]; Yoo, M[Yoo, Moohi]; Park, ES[Park, Eun-Seok]; Lee, HS[Lee, Hye Suk]
- Issue Date
- Sep-2007
- Publisher
- PHARMACEUTICAL SOC KOREA
- Keywords
- udenafil; p-glycoprotein; Caco-2; transport
- Citation
- ARCHIVES OF PHARMACAL RESEARCH, v.30, no.9, pp.1168 - 1173
- Indexed
- SCIE
SCOPUS
KCI
- Journal Title
- ARCHIVES OF PHARMACAL RESEARCH
- Volume
- 30
- Number
- 9
- Start Page
- 1168
- End Page
- 1173
- URI
- https://scholarworks.bwise.kr/skku/handle/2021.sw.skku/83988
- DOI
- 10.1007/BF02980254
- ISSN
- 0253-6269
- Abstract
- P-glycoprotein, an ATP-dependent efflux pump, is a membrane transporter that influences the absorption and excretion of drugs. There is a striking overlap between the substrates for CYP3A4 and P-glycoprotein. This study was designed to assess whether udenafil, a substrate of CYP3A4, is also a P-glycoprotein substrate. Udenafil stimulated P-glycoprotein ATPase activity, a putative measure of P-glycoprotein affinity, although with lower affinity than a proven substrate, verapamil. Bidirectional transport studies of udenafil using Caco-2 cell monolayers showed that its efflux (15.9-22.8 x 10(-6) cm/s) was significantly higher than its influx (3.7-9.1 x 10(-6) cm/s). P-glycoprotein inhibitors such as cyclosporine, tariquidar and verapamil significantly increased the influx of udenafil and decreased the efflux of udenafil. These results indicate that udenafil is a substrate for P-glycoprotein. The low bioavailability, variable absorption and drug-drug interactions of udenafil may be related to the variability of CYP3A4 and P-glycoprotein expression and to possible CYP3A4 and P-glycoprotein interactions.
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