PMID- 23006442
OWN - NLM
STAT- MEDLINE
DCOM- 20130423
LR  - 20121123
IS  - 0946-1965 (Print)
IS  - 0946-1965 (Linking)
VI  - 50
IP  - 12
DP  - 2012 Dec
TI  - Assessment of the influence of severe renal impairment on the pharmacokinetics of 
      mirodenafil in Korean male volunteers.
PG  - 880-8
LID - 10.5414/CP201721 [doi]
AB  - OBJECTIVE: To evaluate and compare the pharmacokinetics and tolerability of a 
      single oral dose of mirodenafil in volunteer patients with severe renal 
      impairment and healthy volunteers. METHODS AND MATERIALS: This open-label, 
      single-dose, parallel group clinical study enrolled a total 12 volunteers (6 
      healthy volunteers and 6 volunteer patients with severe renal impairment). Each 
      volunteer was orally administered 50 mg mirodenafil and serial blood samples were 
      obtained after drug administration to determine the plasma concentration of 
      mirodenafil using LC-MS/MS. The measured individual plasma concentrations were 
      used to calculate the pharmacokinetic parameters using noncompartmental methods. 
      Tolerability was also assessed using measurements of vital signs, clinical 
      chemistry tests, and interviews. RESULTS: All of the volunteers completed the 
      study with no serious adverse events (AEs). A total of 4 AEs were reported, but 
      all were of mild or moderate intensity and not considered to be related to the 
      study drug. The geometric mean (95% CI) of the terminal half-life (t1/2beta) and the 
      apparent clearance (CL/F) values of mirodenafil were 2.2 (1.4 - 3.4) h and 127.2 
      (95.1 - 170.2) l/h in the volunteer patients, and 3.0 (2.1 - 4.4) h and 136.1 
      (74.4 - 249.2) l/h in the healthy volunteers, respectively. The geometric mean of 
      the AUC0-t of the volunteer patients was 8% higher and the geometric mean for 
      clearance was 7% lower compared with the healthy volunteers. However, the 
      geometric mean of the Cmax of the volunteer patients was 38% higher than that of 
      the healthy volunteers. CONCLUSIONS: A single oral 50-mg dose of mirodenafil was 
      well tolerated. Exposure (AUC0-t) to mirodenafil was similar in both healthy 
      volunteers and volunteer patients with severe renal impairment and healthy 
      volunteers.
FAU - Noh, Yook-Hwan
AU  - Noh YH
AD  - Department of Clinical Pharmacology and Therapeutics, University of Ulsan, Seoul, 
      Korea.
FAU - Lim, Hyeong-Seok
AU  - Lim HS
FAU - Cho, Sang-Heon
AU  - Cho SH
FAU - Ghim, Jong-Lyul
AU  - Ghim JL
FAU - Choe, Sangmin
AU  - Choe S
FAU - Jung, Jin Ah
AU  - Jung JA
FAU - Kim, Mi Jo
AU  - Kim MJ
FAU - Kim, Yo Han
AU  - Kim YH
FAU - Jin, Seok-Joon
AU  - Jin SJ
FAU - Kim, Soon Bae
AU  - Kim SB
FAU - Park, Jung Sik
AU  - Park JS
FAU - Lee, Sang Koo
AU  - Lee SK
FAU - Yang, Won Seok
AU  - Yang WS
FAU - Chang, Jai Won
AU  - Chang JW
FAU - Lee, Bongyong
AU  - Lee B
FAU - Bae, Kyun-Seop
AU  - Bae KS
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Germany
TA  - Int J Clin Pharmacol Ther
JT  - International journal of clinical pharmacology and therapeutics
JID - 9423309
RN  - 0 (Phosphodiesterase 5 Inhibitors)
RN  - 0 (Pyrimidinones)
RN  - 0 (Sulfonamides)
RN  - 504G362H0H (mirodenafil)
SB  - IM
MH  - Adult
MH  - Chromatography, Liquid
MH  - Humans
MH  - Male
MH  - Middle Aged
MH  - Phosphodiesterase 5 Inhibitors/*pharmacokinetics
MH  - Pyrimidinones/adverse effects/*pharmacokinetics
MH  - Renal Insufficiency/*metabolism
MH  - Sulfonamides/adverse effects/*pharmacokinetics
MH  - Tandem Mass Spectrometry
EDAT- 2012/09/26 06:00
MHDA- 2013/04/24 06:00
CRDT- 2012/09/26 06:00
PHST- 2012/11/22 00:00 [accepted]
PHST- 2012/09/26 06:00 [entrez]
PHST- 2012/09/26 06:00 [pubmed]
PHST- 2013/04/24 06:00 [medline]
AID - 10001 [pii]
AID - 10.5414/CP201721 [doi]
PST - ppublish
SO  - Int J Clin Pharmacol Ther. 2012 Dec;50(12):880-8. doi: 10.5414/CP201721.