Dear Nchioua Zakariya,

if the drug you plan to work with is approved by e.g. FDA, there should be information on PK/PD in the documents submitted by the drug developer to the regulatory authorities (FDA approved drugs are best, since the documents are freely availabel online via the FDA homepage).

If your target drug is not yet approved or in a preclinical stage I would suggest to look at the concentrations necessary to achieve antimycotic activity and compare to already approved triazoles (e.g. Itraconazole, Fluconazole, Voriconazole and Posaconazole) which have published PK/PD-data.

One concentration that should certainly be used is the (estimated) Cmax in plasma/serum. Depending on the route of administration of the drug, 10xCmax or even higher might be useful, since oral administration (and a potentially high extent of hepatic clearance) will lead to higher drug concentrations in the liver.

I suggest to perform a dose-response curve in any case.

From your question I figure you are working with primary human hepatocytes (correct?). So another way would be to compare dose-response curves from the liver cells with those of cells that do not metabolize drugs in the same extent (e.g. fibroblast cell lines etc.)

Additionally it might be useful to compare your novel triazole with other compounds from this drug class (see above).

OK thank you so much.

So first I should conduct an in-vivo test to determine the concentration in plasma/serum after that I can use that concentration in my rat hepatocytes culture.

But I think what you said about the dose-response curve is great.

Article Toxicity of pesticides with fungicide and fungicide + insect...