Gender differences and dose proportionality in the toxicokinetics of udenafil and its active metabolite following oral administration in rodents

2021 ◽  
Vol 410 ◽  
pp. 115339
Author(s):  
Jong-Hwa Lee ◽  
Dae Young Lee ◽  
Kyung Koo Kang ◽  
Eun Ju Jeong ◽  
Christine E. Staatz ◽  
...  
Keyword(s):  
Gender Differences ◽  
Oral Administration ◽  
Active Metabolite ◽  
Dose Proportionality

Dose Proportionality of Bisoprolol Enantiomers in Humans After Oral Administration of the Racemate

1994 ◽  
Vol 34 (8) ◽  
pp. 829-836 ◽  
Author(s):  
Atanu Dutta ◽  
Robert Lanc ◽  
Evan Begg ◽  
Richard Robson ◽  
Luisa Sia ◽  
...  
Keyword(s):  
Oral Administration ◽  
Dose Proportionality

Influx and Efflux Transporters Contribute to the Increased Dermal Exposure to Active Metabolite of Regorafenib After Repeated Oral Administration in Mice

2019 ◽  
Vol 108 (6) ◽  
pp. 2173-2179 ◽  
Author(s):  
Aya Hasan Al-Shammari ◽  
Yusuke Masuo ◽  
Ken-ichi Fujita ◽  
Yuka Yoshikawa ◽  
Noritaka Nakamichi ◽  
...  
Keyword(s):  
Oral Administration ◽  
Active Metabolite ◽  
Dermal Exposure ◽  
Efflux Transporters

scholarly journals Pharmacokinetic Characterization of LW6, a Novel Hypoxia-Inducible Factor-1α (HIF-1α) Inhibitor in Mice

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2226
Author(s):  
Ji-Yoon Lee ◽  
Kiho Lee ◽  
Kyeong Lee ◽  
Jong Soon Kang ◽  
Min Ju Kim ◽  
...  
Keyword(s):  
Oral Administration ◽  
Active Metabolite ◽  
Parent Compound ◽  
Hypoxia Inducible Factor ◽  
Liver Microsomes ◽  
Cancer Therapeutics ◽  
Volume Of Distribution ◽  
Hypoxia Inducible Factor 1Α ◽  
Plasma Pharmacokinetics

LW6, an (aryloxyacetylamino)benzoic acid derivative, was recently identified to be an inhibitor of hypoxia-inducible factor-1α (HIF-1α), which is an attractive target for cancer therapeutics. Although LW6 is known to act by inhibiting the accumulation of HIF-1α, pharmacokinetics needs to be evaluated to assess its potential as an anti-tumor agent. Here, we investigated the plasma pharmacokinetics and metabolism of LW6 in mice. LW6 exhibited a small volume of distribution (0.5 ± 0.1 L/kg), and a short terminal half-life (0.6 ± 0.1 h). Following intravenous or oral administration, LW6 was rapidly converted to its active metabolite, (4-adamantan-1-yl-phenoxy)acetic acid (APA). Although LW6 was rapidly absorbed, its oral bioavailability, estimated using AUClast values, was low (1.7 ± 1.8%). It was slowly degraded in mouse liver microsomes (t1/2 > 1 h) and serum (t1/2 > 6 h). About 54% or 44.8% of LW6 was available systemically as APA in the mouse after a single intravenous or oral administration, respectively. Thus, our results indicated the need to simultaneously consider the active metabolite as well as the parent compound for successful evaluation during lead optimization.

Disposition of (—)-fenfluramine and its active metabolite, (—)-norfenfluramine in rat: A single dose-proportionality study

Xenobiotica ◽  
1988 ◽  
Vol 18 (5) ◽  
pp. 573-584 ◽  
Author(s):  
R. Spinelli ◽  
C. Fracasso ◽  
G. Guiso ◽  
S. Garattini ◽  
S. Caccia
Keyword(s):  
Single Dose ◽  
Active Metabolite ◽  
Dose Proportionality

scholarly journals Clinical Pharmacokinetics of Oseltamivir and Its Active Metabolite Oseltamivir Carboxylate after Oral Administration in Horses

2007 ◽  
Vol 69 (3) ◽  
pp. 293-296 ◽  
Author(s):  
Takashi YAMANAKA ◽  
Masayuki YAMADA ◽  
Koji TSUJIMURA ◽  
Takashi KONDO ◽  
Shunichi NAGATA ◽  
...  
Keyword(s):  
Oral Administration ◽  
Active Metabolite ◽  
Oseltamivir Carboxylate ◽  
Clinical Pharmacokinetics
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