Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
권호 표지
DOI QR코드

DOI QR Code

Stereochemical Issues in Chiral Drug Development

광학활성의약품 개발과정에서의 입체화학적 문제

  • Choi, Sun-Ok (Division of Biopharmaceutics, Department of Pharmacology, National Institute of Toxicological Research, Korea Food and Drug Administration) ;
  • Jung, Sung-Hee (Division of Biopharmaceutics, Department of Pharmacology, National Institute of Toxicological Research, Korea Food and Drug Administration) ;
  • Um, So-Young (Division of Biopharmaceutics, Department of Pharmacology, National Institute of Toxicological Research, Korea Food and Drug Administration) ;
  • Jung, Seo-Jeong (Division of Biopharmaceutics, Department of Pharmacology, National Institute of Toxicological Research, Korea Food and Drug Administration) ;
  • Kim, Joo-Il (Division of Biopharmaceutics, Department of Pharmacology, National Institute of Toxicological Research, Korea Food and Drug Administration) ;
  • Chung, Soo-Youn (Division of Biopharmaceutics, Department of Pharmacology, National Institute of Toxicological Research, Korea Food and Drug Administration)
  • 최선옥 (국립독성연구원, 유효성연구부, 생물측정과) ;
  • 정성희 (국립독성연구원, 유효성연구부, 생물측정과) ;
  • 엄소영 (국립독성연구원, 유효성연구부, 생물측정과) ;
  • 정서정 (국립독성연구원, 유효성연구부, 생물측정과) ;
  • 김주일 (국립독성연구원, 유효성연구부, 생물측정과) ;
  • 정수연 (국립독성연구원, 유효성연구부, 생물측정과)
  • Published : 2005.02.20
Download PDF
⟨ Previous Next ⟩

Abstract

Numerous drugs are chiral because they possess one or more chiral centers. Enantiomers may differ in their pharmacokinetic, pharmacological and toxicological properties. However, the significance of stereochemistry of drugs in their therapeutic uses has received relatively little attention until recently. The US FDA issued a guideline on stereoisomeric drugs in 1992, and the European agency describes tests for new drug substances which are optically active in an ICH(International Conference of Harmonization) guideline. According to the guidance, enantiomers may differ in their pharmacokinetic, pharmacological and toxicological properties. Therefore, in this paper, we examined the recently published Canadian guidance, stereochemical issues in chiral drug development, which will be references to make a guidance on stereochemical issues in chiral drug development in Korea.

Keywords

References

  1. B.-C. Sallustio and R.-G. Morris, High-performance liquid chromatographic determination of sotalol in plasma, J. Chromatogr., 576, 321-327 (1992) https://doi.org/10.1016/0378-4347(92)80206-6
  2. B.-A. Persson, K. Balmer and P.-O. Langerstorm, Enantioselective determination of metoprolol in plasma by liquid chromatography on a silica-bonded $\alpha_1$-acid glycoprotein column, J. Chromatogr., 500, 629-636 (1990) https://doi.org/10.1016/S0021-9673(00)96097-7
  3. J. Ducharme, C. Fernandez, F. Gimenez and R. Farinotti, Critical issues in chiral drug analysis in biological fluids by high-performance liquid chromatography, J. Chromatogr. B., 686, 65-75 (1996) https://doi.org/10.1016/S0378-4347(96)00274-5
  4. G. Subramanian, A practical approach to chiral separations by liquid chromatography, 62 (1994)
  5. Guidance for Industry : FDA'S Policy Statement For The Development Of New Stereoisomeric Drugs. CDER, US FDA (1992. 5. 1.)
  6. Q6A International Conference on Harmonisation ; Guidance on Q6A Specifications : Test Procedures and Acceptance Criteria for New Drug Substances and New Drug Products : Chemical Substances (2000)
  7. Guidance for Industry : Stereochemical Issues in Chiral Drug Development. Therapeutic Products Programme, Health Canada (2000. 5. 1.)

Cited by

  1. Comparative toxicity and toxicokinetic studies of oxiracetam and (S)-oxiracetam in dogs pp.1366-5928, 2019, https://doi.org/10.1080/00498254.2018.1528027