Journal of Korean Society for Clinical Pharmacology and Therapeutics (임상약리학회지)

Korean Society for Clinical Pharmacology and Therapeutics (대한임상약리학회)
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Evaluation of Safety and Pharmacokinetics of Tegaserod After Multiple Oral Administrations in Healthy Korean Subjects

건강한 한국인 자원자에서 테가세로드(Tegaserod) 반복 투여에 의한 안전성 및 약동학 평가

  • Chung, Jae-Yong (Department of Pharmacology, Seoul National University College of Medicine) ;
  • Lim, Hyeong-Seok (National Cancer Center) ;
  • Hong, Kyoung-Sup (Clinical Pharmacology Unit, Seoul National University Hospital) ;
  • Bae, Kyun-Seop (Clinical Research Center, Asan Medical Center) ;
  • Yu, Kyung-Sang (Clinical Pharmacology Unit, Seoul National University Hospital) ;
  • Cho, Joo-Youn (Department of Pharmacology, Seoul National University College of Medicine) ;
  • Yi, So-Young (Department of Pharmacology, Seoul National University College of Medicine) ;
  • Ko, Jae-Wook (Novartis Korea) ;
  • Jang, In-Jin (Department of Pharmacology, Seoul National University College of Medicine,Clinical Pharmacology Unit, Seoul National University Hospital) ;
  • Shin, Sang-Goo (Department of Pharmacology, Seoul National University College of Medicine,Clinical Pharmacology Unit, Seoul National University Hospital)
  • 정재용 (서울대학교 의과대학 약리학 교실) ;
  • 임형석 (국립암센터) ;
  • 홍경섭 (서울대학교병원 임상약리실) ;
  • 배균섭 (서울아산병원 임상연구지원센터) ;
  • 유경상 (서울대학교병원 임상약리실) ;
  • 조주연 (서울대학교 의과대학 약리학 교실) ;
  • 이소영 (서울대학교 의과대학 약리학 교실) ;
  • 고재욱 (한국 노바티스) ;
  • 장인진 (서울대학교 의과대학 약리학 교실,서울대학교병원 임상약리실) ;
  • 신상구 (서울대학교 의과대학 약리학 교실,서울대학교병원 임상약리실)
  • Published : 2003.12.30

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Abstract

Background: Tegaserod is a selective partial agonist at the $5HT_4$ receptor. Tegaserod belongs to a new class of agents in development for the treatment of functional motility disorders of the gastrointestinal(GD tract. This Phase I clinical study was conducted to evaluate the safety and pharmacokinetics(PK) of tegaserod in Korean for bridging foreign clinical data. Methods: A randomized, double blind, placebo controlled, multiple oral dosing(2 mg, 6 mg, twice a day for 7 days) study was conducted in 32 healthy Korean volunteers(M:F=16:16). Serial blood samples for pharmacokinetic analysis were taken. Safety evaluation was performed by adverse event monitoring, physical examination including vital signs, ECG and clinical labororatory analysis. Results: Plasma concentration of tegaserod reached peak levels $1.0{\sim}1.5$ hours after single and multiple dose administration and declined with a terminal half life of about 12 hours. PK parameters of 2 mg group were not calculated well due to low plasma concentration. Tegaserod showed linear pharmacokinetic characteristics, and little accumulation occurred after multiple administrations. There were no gender differences in PK parameters. Neither serious nor dose-limiting adverse events were observed. PK of tegaserod in Koreans was comparable to Caucasian data. Conclusion: Tegaserod was found to be safe and showed similar PK characteristics to Caucasians. This study demonstrates comparability between Korean and Caucasian healthy subjects in the PK of tegaserod and supports the use of Caucasian data in the evaluation of PK, safety, and efficacy for Korean patients.

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