Passive permeability is a key property in drug disposition and delivery. It is critical for
gastrointestinal absorption, brain penetration, renal reabsorption, defining clearance …

The well accepted “free drug hypothesis” for small-molecule drugs assumes that only the
free (unbound) drug concentration at the therapeutic target can elicit a pharmacologic effect …

Drug–drug interactions (DDIs) caused by the co‐administration of multiple drugs are major
safety concerns in the clinic. Several drugs have been withdrawn from the market due to …

The hepatic risk matrix (HRM) was developed and used to differentiate lead clinical and
back-up drug candidates against competitor/marketed drugs within the same …

Systemic exposure of a drug is generally associated with its pharmacodynamic (PD) effect
(eg, efficacy and toxicity). In this regard, the change in area under the plasma concentration …

Today, it is very challenging to develop new active pharmaceutical ingredients. Developing
good preparations of well-recognized natural medicines is certainly a practical and …

Bosentan is a high-affinity antagonist of endothelin receptors and one of the earliest
examples for target-mediated drug disposition [a type of nonlinear pharmacokinetics (PKs) …

Bosentan is a substrate of hepatic uptake transporter organic anion–transporting
polypeptides (OATPs), and undergoes extensive hepatic metabolism by cytochrome P450 …

Introduction: Transporters and enzymes play an important role in absorption, distribution,
clearance and elimination of drugs. Areas covered: This review provides an overview of the …

Psychoactive substances of the 2C‐series (2Cs) are phenethylamine‐derived designer
drugs that can induce psychostimulant and hallucinogenic effects. Chemically, the classic …