In Vivo Antitumor Activities and Pharmacokinetics of DW2282 Depending on Vehicles

DW2282의 용매의존성 항암효과 및 약동력학

  • Moon, Eun-Yi (Central Research Laboratories of Dong-Wha Pharm. Ind. Co. Ltd.) ;
  • Choi, Chung-Ha (Central Research Laboratories of Dong-Wha Pharm. Ind. Co. Ltd.) ;
  • Seong, Seung-Kyoo (Central Research Laboratories of Dong-Wha Pharm. Ind. Co. Ltd.) ;
  • Lee, Jin (Central Research Laboratories of Dong-Wha Pharm. Ind. Co. Ltd.) ;
  • Ryu, Jei-Man (Central Research Laboratories of Dong-Wha Pharm. Ind. Co. Ltd.) ;
  • Lee, Moon-Sun (Central Research Laboratories of Dong-Wha Pharm. Ind. Co. Ltd.) ;
  • Jung, Sang-Hun (College of Pharmacy, Chung-Nam National University) ;
  • Chung, Yong-Ho (Central Research Laboratories of Dong-Wha Pharm. Ind. Co. Ltd.) ;
  • Lee, Dog-Keun (Central Research Laboratories of Dong-Wha Pharm. Ind. Co. Ltd.) ;
  • Yoon, Sung-June (Central Research Laboratories of Dong-Wha Pharm. Ind. Co. Ltd.)
  • 문은이 (동화약품(주)중앙연구소) ;
  • 최청하 (동화약품(주)중앙연구소) ;
  • 성승규 (동화약품(주)중앙연구소) ;
  • 이진 (동화약품(주)중앙연구소) ;
  • 유제만 (동화약품(주)중앙연구소) ;
  • 이문선 (동화약품(주)중앙연구소) ;
  • 정상현 (충남대학교 약학대학) ;
  • 정용호 (동화약품(주)중앙연구소) ;
  • 이덕근 (동화약품(주)중앙연구소) ;
  • 윤성준 (동화약품(주)중앙연구소)
  • Published : 1998.12.01

Abstract

DW2282, (S)- (+)-4-phenyl -1-[N-(4-am mob enzoyl) -indolin-5- sulfonyl]-4,5- dihydro-2-imidazolone hydrochloride, is a novel anticancer agent thought to have an unique mechanism of action on the inhibition of tumor growth. In this study, we estimated in vivo antitumor activities and pharmacokinetics of Dw2282 depending on various vehicles. The inhibition rate of tumor growth was increased by 50, 100 and 200 mg/kg of Dw2282 in a dose-dependent manner. When Dw2282 dissolved in 4 sorts of vehicles was orally single dosed to rats at 50 mg/kg, Cmax of Dw2282 in 0.5% CMC.Na was a half as high as those in PG, PG+CP and PG+CP+DW. When Dw2282 was orally administered to mice for 5 days, antitumor activity of 130 mg/kg suspended in 0.5% CMC.Na was as effective as that of 65 mg/kg dissolved in the rest of vehicles. Taken together, it is thought that antitumor activities of Dw2282 are resulted from the absorption extent of it and related to the vehicle used.

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