I need to examine the in vitro antiviral activity of a drug in the presence of a series of dilutions of
human serum up to 40 percent (e.g., 5 percent, 10 percent, 20 percent, 40 percent).
An EC50 value for 100 percent human serum can be extrapolated from these data and the serum-adjusted EC50 values reported. In addition, I need to determine EC50 values in the presence of physiological concentrations of α-acidic glycoprotein and human serum albumin.
What will be the difference between the data from the first paragraph vs the second?
Hi,
Differences will be related to different affinity and binding of different drugs for albumins and α-acidic glycoprotein. If your drug has a higher affinity for α-acidic glycoprotein than albumin then differences in concentrations of α-acidic glycoprotein may be important for a free fraction of the drug in vivo and in vitro. It should be always recognized for what fraction of plasma proteins your drug has high affinity. It's especially important in the case of lipophilic drugs and for drug-drug interactions related to concurrence for the same proteins.
Article Unbound Fraction of Clozapine Significantly Decreases with E...
Article An overview of albumin and alpha-1-acid glycoprotein main ch...
https://pubmed.ncbi.nlm.nih.gov/11495502/
Best regards,
Tomasz
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