English Journal

Human carboxymethylenebutenolidase as a bioactivating hydrolase of olmesartan medoxomil in liver and intestine.

Ishizuka T, Fujimori I, Kato M, Noji-Sakikawa C, Saito M, Yoshigae Y, Kubota K, Kurihara A, Izumi T, Ikeda T, Okazaki O.SourceDrug Metabolism and Pharmacokinetics Research Laboratories, Daiichi Sankyo Co. Ltd., Tokyo, Japan. ishizuka.tomoko.xx@daiichisankyo.co.jp
The Journal of biological chemistry.J Biol Chem.2010 Apr 16;285(16):11892-902. Epub 2010 Feb 19.
Olmesartan medoxomil (OM) is a prodrug type angiotensin II type 1 receptor antagonist widely prescribed as an antihypertensive agent. Herein, we describe the identification and characterization of the OM bioactivating enzyme that hydrolyzes the prodrug and converts to its pharmacologically active me
PMID 20177059

Kinetic assessment of luminal degradation of orally effective prodrugs for rational drug development.

Mizuma T.SourceDepartment of Drug Absorption and Pharmacokinetics, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, Tokyo, Japan. mizuma@ps.toyaku.ac.jp
Journal of pharmaceutical sciences.J Pharm Sci.2010 Feb;99(2):1078-86.
Although prodrugging (prodrug derivatization) is a powerful technique for improving the pharmacokinetic characteristics of drugs, the intestinal pharmacokinetics of prodrugs has yet to be elucidated fully. A previous article reported the kinetic requirement of prodrugs to overcome membrane barriers.
PMID 19623605

Japanese Journal

Differences in postoperative morbidity rates, including infection and dry socket, and differences in the healing process after mandibular third molar surgery in patients receiving 1-day or 3-day prophylaxis with lenampicillin

YOSHII Takashi,HAMAMOTO Yoshihiko,MURAOKA Shigetada,FURUDOI Shungo,KOMORI Takahide
Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy 8(1), 87-93, 2002-03-01
NAID 10013892370