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Fast PK and Semi Quantitative Analysis of Metabolites Using High Resolution MS
EP20291
Poster Title: Fast PK and Semi Quantitative Analysis of Metabolites Using High Resolution MS
Submitted on 19 Dec 2013
Author(s): Rohan A. Thakur and Mike Koleto
Affiliations: PharmaNet
Poster Views: 1,645
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Poster Information
Abstract: Fast PK quantitative studies are traditionally performed using a technique known as selected reaction monitoring (SRM) on a triple quadrupole mass spectrometer. In the SRM mode, the ions specific to the NCE are focused onto the detection system, while all other non-specific ions are filtered away. As a result, only the NCE is quantified and its PK estimates determined, but any metabolite information contained in the sample is lost.

With the understanding of this limitation of the SRM technique is the acknowledgement that potentially efficacious NCEs may be prematurely eliminated due to poor PK characteristics, when in fact more complete feedback from the same Fast PK study could provide the support for the decision to make a simple tweak of the chemical structure to improve bioavailability. This is where Orbitrap technology (OT) has the potential to revolutionize Lead Optimization, by providing metabolite information during the Fast PK analysis.
Summary: It has become essential to eliminate poor candidates as early as possible in the drug development process. This realization led to the application of high throughput principles to the in vivo Lead Optimization process, wherein the NCE is first given to rodents to determine the PK profile in a rapid and limited study. This rapid primary screen is known as Fast PK and several critical decisions are based on this initial study.
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