Is PAMPA a useful tool for discovery?

Galinis‐Luciani, D.; Nguyen, Loc

doi:10.1002/jps.21071

Cited by 38 publications

(26 citation statements)

References 17 publications

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“…Although it is ideally suited only for transcellular absorption prediction, many advantages, such as high-throughput, low cost, and the possibility of pH profiling and stirring, over the conventional cell-based in vitro assays, such as Caco-2 (1, 2) and MDCK (3), have made PAMPA a widely used screening method (4)(5)(6)(7)(8)(9)(10). A number of groups have developed their own versions of PAMPA with the major difference being embedded in the membrane composition.…”

Section: Introductionmentioning

confidence: 99%

In Situ Artificial Membrane Permeation Assay under Hydrodynamic Control: Permeability-pH Profiles of Warfarin and Verapamil

et al. 2010

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Both warfarin and verapamil exhibit high permeability values, which is consistent with the high fraction absorbed in human. Our results demonstrate that a considerable lag-time, varying with the solute lipophilicity and stirring rate, exists in membrane permeation and leads to incorrect compound ranking if it is not treated properly. Comparison of the permeability data as a function of pH and stirring rate suggests that some transport of the ionized molecules occurs, most likely via ion-pairing.

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Section: Introductionmentioning

confidence: 99%

In Situ Artificial Membrane Permeation Assay under Hydrodynamic Control: Permeability-pH Profiles of Warfarin and Verapamil

et al. 2010

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“…The barrier has historically been derived from a cell line, most commonly Caco-2 or Madin-Darby canine kidney (MDCK) cells. In the last several years, there has been substantial work and significant progress in the development of parallel artificial membrane permeability assays (PAMPA) [56][57][58]. PAMPA assays can decrease the cost of permeability assessment as compared to cell-based assays.…”

Section: Permeability/absorptionmentioning

confidence: 99%

Hit Triage: Medicinal Chemistry Strategies to Improve the Odds of Success in Discovery

Freeman‐Cook

Kung²

2009

Topics in Medicinal Chemistry

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This chapter describes the process of collecting and analyzing information in order to make decisions which help a project move through a key early stage in drug discovery. It explains, in general, the sources of hits for a drug discovery program and explores the link between potency and efficiency in evaluating lead matter. The chapter then illustrates the collection of both pharmacokinetic data as well as safety data, and describes the relevance of that data and the process of using it to make decisions. Of course, there is no one ''right'' or ''wrong'' way to do the work contained in this chapter, but the practice of efficiently building a network of information on compounds, and then using that to make informed decisions can help to shift the odds of success in drug discovery.

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“…The system includes pre-validated protocols for reagent/assay applications and the software for the specific applications. PAMPA Evolution invented by pION Inn is a good example of such a turnkey workstation (Galinis-Luciani et al 2007). It is a turnkey workstation for sample preparation and reading, data analysis, and presentation in a parallel artificial membrane permeability assay.…”

Section: Signal Detectionmentioning

confidence: 99%

Intelligent Automation Platform for Bioprocess Development

Zhou

2012

Computer Aided Chemical Engineering

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Is PAMPA a useful tool for discovery?

Cited by 38 publications

References 17 publications

In Situ Artificial Membrane Permeation Assay under Hydrodynamic Control: Permeability-pH Profiles of Warfarin and Verapamil

In Situ Artificial Membrane Permeation Assay under Hydrodynamic Control: Permeability-pH Profiles of Warfarin and Verapamil

Hit Triage: Medicinal Chemistry Strategies to Improve the Odds of Success in Discovery

Intelligent Automation Platform for Bioprocess Development

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