Zobrazeno 1 - 10
of 44
pro vyhledávání: '"Takafumi, Iwatsubo"'
Autor:
Takafumi Iwatsubo
Publikováno v:
Drug Metabolism and Pharmacokinetics. 35:71-75
The U.S. Drugs and Food Administration (FDA) and the Ministry of Health, Labor and Welfare of Japan (MHLW) issued the drastically revised draft guidance and final guideline on drug-drug interactions (DDI) in 2017 and 2018, respectively. One of the mo
Autor:
Yoshiaki Ohtsu, Kiyoshi Noguchi, Takuya Sonoda, Yoko Susaki, Yasuhisa Fukunaga, Toshifumi Tohda, Takafumi Iwatsubo
Publikováno v:
Biopharmaceutics & Drug Disposition. 36:34-48
The potent and selective phosphodiesterase 4 inhibitor ASP3258 is a novel therapeutic agent for asthma and chronic obstructive pulmonary disease (COPD). After a single oral administration to rats, ASP3258 is rapidly absorbed with a bioavailability of
Autor:
Virginie Kerbusch, Yutaka Takahashi, Hiroyuki Nemoto, Fumihiko Ushigome, Takafumi Iwatsubo, Aiji Miyashita, Shin Takusagawa, Takashi Usui, Qun Li
Publikováno v:
Molecular Pharmaceutics. 10:1783-1794
Mirabegron, a weak-basic compound, is a potent and selective β3-adrenoceptor agonist for the treatment of overactive bladder. Mirabegron extended release formulation shows dose-dependent oral bioavailability in humans, which is likely attributable t
Autor:
Sjoerd van Marle, Tadashi Hashimoto, Aiji Miyashita, Frank Verheggen, Dorien Groenendaal, Takafumi Iwatsubo, Yukie Kihara, Marten Heeringa, Hartmut Onkels, Katsuhiro Suzuki, Takashi Usui
Publikováno v:
Xenobiotica. 43:534-547
1. The absorption, metabolism and excretion of darexaban (YM150), a novel oral direct factor Xa inhibitor, were investigated after a single oral administration of [(14)C]darexaban maleate at a dose of 60 mg in healthy male human subjects. 2. [(14)C]D
Publikováno v:
Biopharmaceutics & Drug Disposition. 33:304-315
The inhibition potencies of aripiprazole and its active metabolite, dehydroaripiprazole, on the activities of human multidrug resistance protein 1 (MDR1/ABCB1; P-glycoprotein), breast cancer resistance protein (BCRP/ABCG2) and multidrug resistance-as
Publikováno v:
Drug Metabolism and Disposition. 40:1389-1396
The aims of this study were to develop a robust method for simultaneous quantification of carboxylesterases (CESs) 1 and 2 and to quantify those absolute protein levels in human liver tissue fractions. Unique peptide fragments of CES1 and CES2 in try
Publikováno v:
Drug Metabolism and Disposition. 40:902-906
The aim of this study was to conclusively determine the enzyme responsible for the hydrolysis of oxybutynin in human liver. Hydrolysis in human liver microsomes (HLMs) and human liver cytosol (HLC) followed Michaelis-Menten kinetics with similar K(m)
Autor:
Kohichiro Tanaka, Hidetaka Kamimura, Kinya Souda, Akio Kawamura, Yuichi Murakami, Ayako Mera, Katsuhiro Suzuki, Naoyuki Nakada, Takashi Usui, Takafumi Iwatsubo
Publikováno v:
Drug Metabolism and Pharmacokinetics. 25:223-235
The ability to predict circulating human metabolites of a candidate drug before first-in-man studies are carried out would provide a clear advantage in drug development. A recent report demonstrated that while in vitro studies using human liver prepa
Autor:
Hidetaka Kamimura, Takafumi Iwatsubo, K.-I. Umehara, Naoyuki Nakada, Takashi Usui, Kiyoshi Noguchi
Publikováno v:
Drug Metabolism and Disposition. 37:2137-2144
(−)- N -{2-[( R )-3-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)piperidino]ethyl}-4-fluorobenzamide (YM758), a novel “funny” If current channel inhibitor, was being developed as a treatment for stable angina and atrial fibrillation
Autor:
K.-I. Umehara, Nobuaki Shirai, Hidetaka Kamimura, Kiyoshi Noguchi, Takafumi Iwatsubo, Takashi Usui
Publikováno v:
Drug Metabolism and Disposition. 37:1646-1657
(-)-N-{2-[(R)-3-(6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)piperidino]ethyl}-4-fluorobenzamide (YM758) is a novel inhibitor of the "funny" If current channel (If channel) that is expressed in the sinus node of heart and is being develop