Following studies in the late 1990s that indicated that poor pharmacokinetics and toxicity
were important causes of costly late-stage failures in drug development, it has become …

Fundamental physiochemical features of CNS drugs are related to their ability to penetrate
the blood-brain barrier affinity and exhibit CNS activity. Factors relevant to the success of …

The oral bioavailability of BCS (biopharmaceutics classification system) class II drugs with
poor solubility and reasonable permeability is limited by the drug dissolution step from drug …

The process of drug discovery applies rigorous selection pressures. Marketed oral drugs will
generally possess favorable physiochemical properties with respect to absorption …

Conclusion Conferences on in vitro technologies are common, but the data presented at this
meeting showed why–the rapid progress in this field requires constant updating of the …

Comparisons of the calculated physicochemical properties of oral drugs launched prior to
1983 (864 drugs) and between 1983 and 2002 (329 drugs) show that mean values of …

An increasingly competitive pharmaceutical market demands improvement in the efficiency
and probability of drug candidate discovery. Usually these new drug candidates are targeted …

Human jejunal permeability (P eff) is determined in the intestinal region with the highest
expression of carrier proteins and largest surface area. Intestinal P eff are often based on …

Multidrug resistant transporter MDR1WP-glycoprotein, the gene product of MDR1, is a
glycosylated membrane protein of 170 kDa, belonging to the ATP-binding cassette …

Efforts to improve oral drug bioavailability have grown in parallel with the pharmaceutical
industry. As the number and chemical diversity of drugs has increased, new strategies have …