Multispecific organic anion transporter is responsible for the biliary excretion of the camptothecin derivative irinotecan and its metabolites in rats

XY Chu, Y Kato, K Niinuma, KI Sudo, H Hakusui… - … of Pharmacology and …, 1997 - ASPET
Irinotecan, 7-ethyl-10-[4-(1-piperidino)-1-piperidino]-carbonyloxycamptothecin (CPT-11), is
a potent anticancer drug that is increasingly used in chemotherapy. A frequent limiting side …

Biliary excretion mechanism of CPT-11 and its metabolites in humans: involvement of primary active transporters

XY Chu, Y Kato, K Ueda, H Suzuki, K Niinuma… - Cancer research, 1998 - AACR
After administration of CPT-11, a camptothecin derivative exhibiting a wide spectrum of
antitumor activity, dose-limiting gastrointestinal toxicity with great interpatient variability is …

Which concentration of the inhibitor should be used to predict in vivo drug interactions from in vitro data?

…, S Kanamitsu, M Kato, I Kawahara, K Niinuma… - AAPS PharmSci, 2002 - Springer
When the metabolism of a drug is competitively or noncompetitively inhibited by another drug,
the degree of in vivo interaction can be evaluated from the [I] u /K i ratio, where [I] u is the …

Temocaprilat, a novel angiotensin-converting enzyme inhibitor, is excreted in bile via an ATP-dependent active transporter (cMOAT) that is deficient in Eisai …

…, K Sasahara, Y Kawahara, K Niinuma… - … of Pharmacology and …, 1997 - ASPET
Temocapril · HCl (α-{(2S,6R)-6-[(1S)-1-ethoxy-carbonyl-3-phenyl-propyl]amino-5-oxo-2-(2-thienyl)perhydro-1,4-thiazepin-4yl}acetic
acid hydrochloride) is a novel prodrug of an …

Primary active transport of organic anions on bile canalicular membrane in humans

K Niinuma, Y Kato, H Suzuki… - American Journal …, 1999 - journals.physiology.org
Biliary excretion of several anionic compounds was examined by assessing their ATP-dependent
uptake in bile canalicular membrane vesicles (CMV) prepared from six human liver …

Kinetic Analysis of the Primary Active Transport of Conjugated Metabolites Across the Bile Canalicular Membrane: Comparative Study ofS-(2, 4-Dinitrophenyl) …

K Niinuma, O Takenaka, T Horie, K Kobayashi… - … of Pharmacology and …, 1997 - ASPET
Eisai hyperbilirubinemic rat (EHBR) is a mutant strain with a hereditary defect in canalicular
multispecific organic anion transporter (cMOAT). We examined the uptake and mutual …

Carrier-mediated hepatic uptake of the cationic cyclopeptide, octreotide, in rats: Comparison between in vivo and in vitro

T Yamada, K Niinuma, M Lemaire, T Terasaki… - Drug metabolism and …, 1997 - ASPET
The plasma concentration and biliary excretion profiles of a cationic cyclic octapeptide,
octreotide, were compared between control rats and rats given an intravenous infusion of a bile …

Mechanism of the tissue distribution and biliary excretion of the cyclic peptide octreotide.

T Yamada, K Niinuma, M Lemaire, T Terasaki… - … of Pharmacology and …, 1996 - ASPET
The hepatobiliary transport and tissue distribution of the cationic cyclooctapeptide octreotide
were studies at steady state after its infusion, at various rates, in rats. After an increase in …

Hepatobiliary transport mechanism for the cyclopentapeptide endothelin antagonist BQ-123

…, Y Kato, T Yamada, K Niinuma… - American Journal …, 1997 - journals.physiology.org
The hepatobiliary transport of an anionic cyclopentapeptide endothelin antagonist, BQ-123,
was studied in rats. Biliary excretion of [3H]BQ-123 was extensive in vivo (approximately 75…

Role of ABC transporters for the biliary excretion of organic anions

…, K ITO, T HIROHASHI, K NIINUMA… - Drug Metabolism and …, 1996 - jstage.jst.go.jp
Several organic anions, including the glutathione-and glucuronide-conjugates, are excreted
into the bile via a canalicular multispecific organic anion transporter (cMOAT), which is …