Which in vitro screens guide the prediction of oral absorption and volume of distribution?
The development of medium to high-throughput in vitro screening of ADME (Absorption, Distribution, Metabolism, Excretion) properties has been the reply to higher demands on drug metabolism scientists to cope with progress in chemistry and biology. Two areas will be discussed here, namely screens for oral absorption and for volume of distribution. The prediction of these human pharmacokinetic parameters can be based on proper combination of simple physicochemical measurements. In the future in vitro screens most likely will be combined with in silico assessments of various ADME properties leading to the concept of in combo screening in drug discovery.
van de Waterbeemd
Han
H
Pfizer Global Research and Development, PDM, Sandwich Laboratories, IPC 664, Ramsgate Road, Sandwich, Kent CT13 9NJ, U.K. han_waterbeemd@sandwich.pfizer.com
D000284:Administration, Oral; D000818:Animals; D015374:Biosensing Techniques; D002352:Carrier Proteins / Q000502:physiology; D002460:Cell Line; D006801:Humans; D007408:Intestinal Absorption; D008081:Liposomes / Q000378:metabolism; D008823:Micelles; D010539:Permeability; D012995:Solubility
D002352:Carrier Proteins; D008081:Liposomes; D008823:Micelles