LC/MS applications in drug development

Mass Spectrom Rev. 1999 May-Aug;18(3-4):187-279. doi: 10.1002/(SICI)1098-2787(1999)18:3/4<187::AID-MAS2>3.0.CO;2-K.


The combination of high-performance liquid chromatography and mass spectrometry (LC/MS) has had a significant impact on drug development over the past decade. Continual improvements in LC/MS interface technologies combined with powerful features for structure analysis, qualitative and quantitative, have resulted in a widened scope of application. These improvements coincided with breakthroughs in combinatorial chemistry, molecular biology, and an overall industry trend of accelerated development. New technologies have created a situation where the rate of sample generation far exceeds the rate of sample analysis. As a result, new paradigms for the analysis of drugs and related substances have been developed. The growth in LC/MS applications has been extensive, with retention time and molecular weight emerging as essential analytical features from drug target to product. LC/MS-based methodologies that involve automation, predictive or surrogate models, and open access systems have become a permanent fixture in the drug development landscape. An iterative cycle of "what is it?" and "how much is there?" continues to fuel the tremendous growth of LC/MS in the pharmaceutical industry. During this time, LC/MS has become widely accepted as an integral part of the drug development process. This review describes the utility of LC/MS techniques for accelerated drug development and provides a perspective on the significant changes in strategies for pharmaceutical analysis. Future applications of LC/MS technologies for accelerated drug development and emerging industry trends are also discussed.

Publication types

  • Review

MeSH terms

  • Amino Acid Sequence
  • Biopharmaceutics
  • Chemistry, Pharmaceutical*
  • Chromatography, Liquid / instrumentation
  • Chromatography, Liquid / methods*
  • Humans
  • Mass Spectrometry / instrumentation
  • Mass Spectrometry / methods*
  • Molecular Sequence Data
  • Technology, Pharmaceutical*