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Generic physiologically-based models of pharmacokinetics were evaluated for early drug discovery. Plasma profiles after intravenous and oral dosing were simulated in rat for 68 compounds from six chemical classes. Input data consisted of structure based predictions of lipophilicity, ionization, and protein binding plus intrinsic clearance measured in rat hepatocytes, single measured values of aqueous solubility, and artificial membrane permeability. LogP of compounds was high with a mean of 3.9 while free fraction in plasma (mean 9%) and solubility (mean 37 µg/mL) were low. Predicted and observed clearance and volume showed mean fold-error and R2 of 1.8, 0.56, and 1.9, 0.25 respectively. Predicted bioavailability showed strong bias to under prediction correlated to very low aqueous solubility and a theoretical correction for bile salt solubilization in vivo brought some improvement in average prediction error (to 31%). Overall, this evaluation shows that generic simulation may be applicable for typical drug-like compounds to predict differences in pharmacokinetic parameters of more than twofold based upon minimal measured input data. However verification of the simulations with in vivo data for a few compounds of each compound class is recommended since recent discovery compounds may have properties beyond the scope of the current generic models.

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Cambridge Biomedical Inc

Comparative Biosciences, Inc

QUINTA-ANALYTICA s.r.o

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CZECH REPUBLIC

UNITED STATES

Virtual BoothQuinta-Analytica, a leading Central European one-stop-shop CRO located in Czech Republic. Providing end-to-end solution to its partners

Pharmacokinetics & Statistical Evaluation

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Specialized software is used for pharmacokinetic and statistical evaluation of study results: SAS® (SAS Institute Inc.,www.sas.com); WinNonlin® Professional (Pharsight Corporation, www.pharsight.com)

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Pharma Service: Analytical

Category: BioAnalytical Services

Sub Category: Calculation and Modeling of Pharmacokinetic Parameters

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Pharmacokinetics

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CBI provides a range of pharmacology and pharmacokinetics capabilities across a spectrum of indications that ensure reliable results in the drug discovery and translation process.

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Pharma Service: Analytical

Category: BioAnalytical Services

Sub Category: Calculation and Modeling of Pharmacokinetic Parameters

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Ophthalmic Pharmacokinetics

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CBI offers a variety of preclinical ophthalmic pharmacokinetic, pharmacodynamic and biodistribution study capabilities. Our assessment and analysis modalities are fine-tuned to meet the specific requirements demanded in each targeted area of ophthalmologic pharmacokinetic investigation.

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Pharma Service: Analytical

Category: BioAnalytical Services

Sub Category: Calculation and Modeling of Pharmacokinetic Parameters

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Pharmacokinetics / Pharmacodynamics

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Cambridge Biomedical utilizes selective and sensitive immunoassays such as ELISA, MSD and Luminex to implement your PK studies. High performance liquid chromatography, various ligand-binding assays (LBA), cell based assays, and biomarker detection methods to assess pharmacodynamic profiles.

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Pharma Service: Analytical

Category: BioAnalytical Services

Sub Category: Calculation and Modeling of Pharmacokinetic Parameters

Generic physiologically-based models of pharmacokinetics were evaluated for early drug discovery. Plasma profiles after intravenous and oral dosing were simulated in rat for 68 compounds from six chemical classes. Input data consisted of structure based predictions of lipophilicity, ionization, and protein binding plus intrinsic clearance measured in rat hepatocytes, single measured values of aqueous solubility, and artificial membrane permeability. LogP of compounds was high with a mean of 3.9 while free fraction in plasma (mean 9%) and solubility (mean 37 µg/mL) were low. Predicted and observed clearance and volume showed mean fold-error and R2 of 1.8, 0.56, and 1.9, 0.25 respectively. Predicted bioavailability showed strong bias to under prediction correlated to very low aqueous solubility and a theoretical correction for bile salt solubilization in vivo brought some improvement in average prediction error (to 31%). Overall, this evaluation shows that generic simulation may be applicable for typical drug-like compounds to predict differences in pharmacokinetic parameters of more than twofold based upon minimal measured input data. However verification of the simulations with in vivo data for a few compounds of each compound class is recommended since recent discovery compounds may have properties beyond the scope of the current generic models.

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