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C min is a term used in pharmacokinetics for the minimum blood plasma concentration reached by a drug during a dosing interval, which is the time interval between administration of two doses. This definition is slightly different from C trough , the concentration immediately prior to administration of the next dose. [ 1 ]
Druglikeness can be estimated for any molecule, and does not evaluate the actual specific effect that the drug achieves (biological activity). Simple rules are not always accurate and may unnecessarily limit the chemical space to search: many best-selling drugs have features that cause them to score low on various druglikeness indices. [7]
Peak-to-trough ratio in pharmacokinetics is the ratio of peak (C max) and trough (C min) levels of a drug over its dosing interval (τ) at steady state.. Peak-to-trough ratio (PTR), also known as peak-to-trough variation or peak-to-trough fluctuation, is a parameter in pharmacokinetics which is defined as the ratio of C max (peak) concentration and C min (trough) concentration over a dosing ...
Lipinski's rule of five, also known as Pfizer's rule of five or simply the rule of five (RO5), is a rule of thumb to evaluate druglikeness or determine if a chemical compound with a certain pharmacological or biological activity has chemical properties and physical properties that would likely make it an orally active drug in humans.
For oral drugs, a LogP value comprised between 2 and 3 is often considered optimal to achieve a compromise between permeability and first-pass clearance. LiPE allows capturing both values in a single parameter, and empirical evidence suggest that quality drug candidates have a high LiPE (>6); this value corresponds to a compound with a pIC 50 ...
The drug apparent permeability (P app) is calculated by normalizing the drug flux (j) over the initial concentration of the API in the donor compartment (c 0) as: Equation 2: = / Dimensionally, the P app represents a velocity, and it is normally expressed in cm/sec. The highest is the permeability, the highest is expected to be the ...
K i is the inhibition constant for a drug; the concentration of competing ligand in a competition assay which would occupy 50% of the receptors if no ligand were present. [ 5 ] The Cheng-Prusoff equation produces good estimates at high agonist concentrations, but over- or under-estimates K i at low agonist concentrations.
Short term drug side effects are most likely to occur at or near the C max, whereas the therapeutic effect of drug with sustained duration of action usually occurs at concentrations slightly above the C min. [citation needed] The C max is often measured in an effort to show bioequivalence (BE) between a generic and innovator drug product. [4]