Natural Science > Chemistry > DG CY2020 8029

Research Title Metabolite Profiling Using Imaging Mass Spectrometry (Year 2 of 3)
Research Personnel Leader:
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Research Duration Start:
End:
2 May 2019
1 May 2022
Research Location USA
Research Description The program will establish the requisite in vitro and in vivo (animal) ADME-Tox assays to help identify the best iteration of the lead compounds in the drug discovery pipeline. The suite of assays can constitute the bulk of ADME-Tox package that will be required by regulatory authorities for an investigational new drug application (IND). Most of the assays to be described are in vitro, for several reasons. Firstly, they are simple, convenient, and provide a fast way of testing the drug-like properties of a lead series. Secondly, they require limited amounts of a test compound. Thirdly, SAR studies for metabolic activity are in fact more difficult to study animals because of confounding factors. Lastly, speciesrelated differences make ADME studies in animals less appealing, as they often fail to estimate human clinical outcomes.
Research Objectives 1. To examine and determine the spatial distribution and localization of drug candidate in dosed tissue section of liver, kidney, heart and lungs using MALDI Imaging Mass Spectrometry; 2. To systematically assess the effect of the drug candidate in dosed tissue sections of the liver, kidney, heart and lungs using MALDI Imaging Mass Spectrometry and histopathology; 3. To quantitatively visualize the spatial distribution of the potential drug candidate in dosed tissue sections of liver kidney, heart and lungs using MALDI Imaging Mass Spectrometry; 4. To unambiguously detect and identify drug metabolites and their spatial distribution using HRMS measurement, MS/MS, MSn and MALDI Imaging mass spectrometry.
Research Beneficiary(ies) This will benefit all parties involved in their discovery and development as joint owners of all intellectual property generated. Most importantly, patients are the ultimate beneficiaries should the drugs survive clinical trials and FDA approval.
Research Accoplishments [CY 2019] 1) Data and information to support efficacy, safety and toxicity of potential drug candidate; and 2) Identity of drug metabolites [CY 2020] 1) Data and information to support efficacy, safety and toxicity of potential drug candidate; and 2) Identity of drug metabolites [CY 2021] 1) Data and information to support efficacy, safety and toxicity of potential drug candidate; and 2) Identity of drug metabolites
Total Research Cost ₱6,841,843.85
Research Agencies Funding:
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USA


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Code DG CY2020 8029
KRA Code
Priority Thrust DOST
R&D


Sector Natural Sciences
Actual Sector Chemistry
Related sectors Medical science
Entry revision: February 2021