Formulation Test and Optimization for PK

Pharmacodynamics (PD) is the study of the biological body's response to compounds, that is, the pharmacological effects of compounds on the body. Pharmacokinectics (PK) is the study of the dynamic distribution process of compounds in biological organisms, that is, the process of biological organisms processing compounds.

After the drug enters the biological body, it reaches the target or off-target site through the distribution process, but the relevant pharmacological activity cannot be observed immediately. Take receptor kinase inhibitors as an example, after the compound reaches the site of action, the phosphorylated kinase can still activate the signal pathway at this time. Only these phosphorylated kinases are removed from the cell surface by the ubiquitination system or ligand mediated endocytosis, etc. , the activity of the newly expressed kinase receptor will be inhibited by the compounds, thereby inhibiting the activation of subsequent signaling pathways and eventually causing cell apoptosis or growth arrest. Therefore, understanding the relationship between the concentration of a compound and its activity is very important for choosing the dose and frequency of administration of the compound.

When studying the PK/PD relationship of a compound, it is very important to select the appropriate PD marker. In preclinical experiments, you can choose to use the phosphorylation of the target itself or the changes in key molecules downstream of its signaling pathway as PD molecular markers. In addition, related molecules in plasma or skin can also be selected as surrogate PD molecular markers.
In preclinical PK-PD relationship analysis, PK is usually determined by analyzing the compound concentration in plasma and target tissues (such as tumors), and PD molecular markers are analyzed by common cytological methods (such as WB, IF, ELISA, etc.).


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