Natural Science > Chemistry > DG CY2020 8028

Research Title HPLC and Mass Spectral Studies to Support Various ADMET Assays (Year 2 of 3)
Research Personnel Leader:
Staff:


Research Duration Start:
End:
1 December 2018
30 November 2021
Research Location UPD-IC
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 develop and validate LCMS methods specific to the compounds; 2. To quantify the amount of drug absorbed and distributed from the site of administration to the bloodstream based on standard calibration curves; 3. To identify metabolites of the drug by using available software to interpret mass spectral fragmentation patterns; 4. To determine the degradation rate of the drug in the plasma; 5. To quantify the amount of the drug excreted in the urine including its removal rate.
Research Beneficiary(ies) The study will provide lead optimized compounds(i.e., compounds with most drug-like features) for downstream formulation, pre clinical and clinical studies. These high value compounds can be licensed out or partnered for further development. 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 2018] The part of the program will answer the question on what happens to the drug once it enters the body both in the qualitative and quantitative aspect. It is expected to provide quantitative data regarding the ADME and use these to assess the drug efficiency.
Total Research Cost ₱6,171,802.32
Research Agencies Funding:
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UPD-IC


Research Budget Breakdown Year:
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Code DG CY2020 8028
KRA Code
Priority Thrust DOST
R&D


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