Benefit from Robust PK Assay and Analysis to Determine Drug ADME

Assessing the pharmacological properties of the small chemical compounds is crucial for initially selecting or identifying the chemical lead. For being effective as a potent drug candidate, the molecule should reach its targeted site of action in sufficing concentrations. Furthermore, it is also essential for the molecule to stay there in its bioactive form for long time so that the user can derive the expected therapeutic benefits. The process of drug development involves assessment of different parameters such as absorption, distribution, metabolism, and excretion. 

Throughout the time and resource consuming process of the novel discovery and development of the drug candidates, evaluation of a large count of molecular structures is of paradigm importance. It is quite essential for the molecule to exhibit high biological activity conjointly thereby minimizing toxicity levels. Equally important is assessing its access to including the therapeutic concentration of the potent drug target. 

One of the most traditional ways of considering pharmacokinetics is breaking down various effects impacting the access of the drug candidate to the targeted parameters. Subsequently, these ADME parameters should be evaluated by applying dedicated parameters. 

Both quantitation and identification of the drug metabolites have been critical to the process of drug discovery and development. For the purpose of discovery, having knowledge about the metabolic targets of the drug candidates has always been considered essential. This knowledge aids in the process of selecting compounds possessing favourable pharmacokinetic characteristics thereby aiding the medicinal chemists to modify the soft spots of the metabolites. As a result, there has always been an increasing demand placed for the ADME/PK characterization of the pharmaceutical candidates. Thus, you will always find that the demand for achieving the ADME/PK assay reproducibility and throughput is increasing. This has led to the rising demand for inculcating automation. 

Pharmacokinetic testing thus helps in the process of initial selection of the drug candidates by considering their absorption, distribution, metabolism, and excretion parameters. These activities are usually important from the point of view of the exploratory pharmacology group that is responsible for providing both the in vitro and in vivo pharmacological and physiochemical results for the analysis of the biologically active small molecules. Early-stage pharmacological assessment has always been adopted as one of the important features in the process of probe discovery.

Establishing a high throughput along with the fast ADMET profiling assays facilitates the selection of the prioritization the selection of the drug candidates according to their biopharmaceutical properties. This is accomplished parallel to the optimization of their efficacy during the early drug discovery stages. 

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Pk analysis is performed for improvising on the overall drug quality thereby highlighting the probability of their success in the selection process. Optimally, when PK/PD studies are successfully accomplished, experts belonging to both the DMPK and pharmacology backgrounds evaluates PK/PD analysis, their interpretations and conclusions. The final report thus captures any relevant assumptions made throughout the analysis thereby suggesting the subsequent result analysis. This also reflects the ownership and responsibility underlying with the experts of DMPK and pharmacology. It can thus be concluded that the PK/PD analysis helps in assessing the potent drug compound thereby selecting and guiding an efficient strategy for clinical development. 
 

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  1. author
    27 Aug 2019
    Tomas Mandy

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    1. author
      27 Aug 2019
      Britney Millner

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  2. author
    27 Aug 2019
    Simon Downey

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