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The free drug hypothesis is a critical idea that allows fairly accurate predictions of therapeutic drug dosing based upon preclinical data. The key equation for determining a dose relies on just four variables: the desired unbound plasma concentration (Cpunbound), the intrinsic clearance of the molecule (CLint), the dosing interval (tau), and bioavailability (F). The desired unbound plasma concentration is generally determined by potency assays, and an example of a possible value would be an IC50 value for an enzyme inhibitor. Dosing predictions are important for advancement of a lead in a discovery program. Dosing predictions fall under the idea of PK/PD - using pharmacokinetic parameters to predict how to achieve pharmacodynamic effects in an organism.
free drug hypothesis, dosing predictions, & PK/PD
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Chem Help ASAPchemhelpasapdrug discoverydrug developmentmedicinalchemistrymedicinal chemistrymed chempharmacokineticsPKADMEplasmaplasma proteinplasma protein bindingprotein bindingserum protein bindingalbuminalbumin bindinghuman serum albuminfree drug hypothesisfree drugfree drug concentrationdrug dose predictiondrug dosedose predictiondosepharmacodynamicsPK PDpk pd modelPK/PDPK/PD modelclinical pharmacologypharmacology