Predicting clearance mechanism in drug discovery: extended clearance classification system (ECCS)

MV Varma, SJ Steyn, C Allerton, AF El-Kattan - Pharmaceutical research, 2015 - Springer
Early prediction of clearance mechanisms allows for the rapid progression of drug discovery
and development programs, and facilitates risk assessment of the pharmacokinetic …

pH-Dependent solubility and permeability criteria for provisional biopharmaceutics classification (BCS and BDDCS) in early drug discovery

MV Varma, I Gardner, SJ Steyn, P Nkansah… - Molecular …, 2012 - ACS Publications
The Biopharmaceutics Classification System (BCS) is a scientific framework that provides a
basis for predicting the oral absorption of drugs. These concepts have been extended in the …

Clearance in drug design: miniperspective

DA Smith, K Beaumont, TS Maurer… - Journal of Medicinal …, 2018 - ACS Publications
Due to its implications for both dose level and frequency, clearance rate is one of the most
important pharmacokinetic parameters to consider in the design of drug candidates …

The next frontier in ADME science: Predicting transporter-based drug disposition, tissue concentrations and drug-drug interactions in humans

F Storelli, M Yin, AR Kumar, MK Ladumor… - Pharmacology & …, 2022 - Elsevier
Predicting transporter-based drug clearance (CL) and tissue concentrations (TC) in humans
is important to reduce the risk of failure during drug development. In addition, when …

Distinguishing between the permeability relationships with absorption and metabolism to improve BCS and BDDCS predictions in early drug discovery

CA Larregieu, LZ Benet - Molecular pharmaceutics, 2014 - ACS Publications
The biopharmaceutics classification system (BCS) and biopharmaceutics drug distribution
classification system (BDDCS) are complementary classification systems that can improve …

Direct comparison of total clearance prediction: computational machine learning model versus bottom-up approach using in vitro assay

Y Kosugi, N Hosea - Molecular Pharmaceutics, 2020 - ACS Publications
The in vitro–in vivo extrapolation (IVIVE) approach for predicting total plasma clearance
(CLtot) has been widely used to rank order compounds early in discovery. More recently, a …

Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification …

CY Wu, LZ Benet - Pharmaceutical research, 2005 - Springer
No Heading The Biopharmaceutics Classification System (BCS) was developed to allow
prediction of in vivo pharmacokinetic performance of drug products from measurements of …

Renal clearance in drug discovery and development: molecular descriptors, drug transporters and disease state

B Feng, JL LaPerle, G Chang… - Expert opinion on drug …, 2010 - Taylor & Francis
Importance of the field: Kidney plays a key role in the elimination of xenobiotics and
metabolic products from the body, where renal clearance is determined by glomerular …

Species differences in drug transporters and implications for translating preclinical findings to humans

X Chu, K Bleasby, R Evers - Expert opinion on drug metabolism & …, 2013 - Taylor & Francis
Introduction: Drug transporters play an important role in the absorption, distribution, and
excretion (ADE) of many drugs. In the last several years it has become increasingly clear …

Predicting drug disposition via application of a biopharmaceutics drug disposition classification system

LZ Benet - Basic & clinical pharmacology & toxicology, 2010 - Wiley Online Library
A Biopharmaceutics Drug Disposition Classification System (BDDCS) was proposed to
serve as a basis for predicting the importance of transporters in determining drug …