The road map to oral bioavailability: an industrial perspective

Expert Opinion on Drug Metabolism & Toxicology
V Hayden ThomasAyman El-Kattan


Optimisation of oral bioavailability is a continuing challenge for the pharmaceutical and biotechnology industries. The number of potential drug candidates requiring in vivo evaluation has significantly increased with the advent of combinatorial chemistry. In addition, drug discovery programmes are increasingly forced into more lipophilic and lower solubility chemical space. To aid in the use of in vitro and in silico tools as well as reduce the number of in vivo studies required, a team-based discussion tool is proposed that provides a 'road map' to guide the selection of profiling assays that should be considered when optimising oral bioavailability. This road map divides the factors that contribute to poor oral bioavailability into two interrelated categories: absorption and metabolism. This road map provides an interface for cross discipline discussions and a systematic approach to the experimentation that drives the drug discovery process towards a common goal - acceptable oral bioavailability using minimal resources in an acceptable time frame.


Sep 1, 1978·Journal of Pharmaceutical Sciences·Z T Chowhan
Jul 1, 1991·European Journal of Drug Metabolism and Pharmacokinetics·G CocchiaraM Strolin Benedetti
Aug 1, 1989·Clinical Pharmacology and Therapeutics·P JaillonO Vergnoux
Oct 1, 1986·Chemical & Pharmaceutical Bulletin·S YakouT Nagai
Dec 1, 1972·Journal of Pharmaceutical Sciences·S F Kramer, G L Flynn
Apr 1, 1974·Journal of Pharmaceutical Sciences·G L FlynnT J Roseman
Apr 26, 1994·Proceedings of the National Academy of Sciences of the United States of America·J P VaccaE Roth
Jul 1, 1993·Pharmaceutical Research·B Davies, T Morris
Mar 6, 1998·Pharmaceutical Research·J E Polli, M J Ginski
Apr 2, 1998·Journal of Pharmaceutical Sciences·A L UngellH Lennernäs
Apr 21, 1998·Journal of Pharmaceutical Sciences·H Lennernäs
Jul 8, 1998·Pharmacology·L Salphati, L Z Benet
Sep 24, 1999·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·J KarlssonP Artursson
Dec 21, 2000·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·A Seelig, E Landwojtowicz
Feb 13, 2001·Journal of Pharmaceutical Sciences·N Jain, S H Yalkowsky
Mar 29, 2001·Journal of Pharmacological and Toxicological Methods·C A Lipinski
Apr 20, 2001·Journal of Medicinal Chemistry·H van De WaterbeemdD K Walker
Jun 26, 2001·European Journal of Drug Metabolism and Pharmacokinetics·J F BergmannJ M Ségrestaa
Jul 24, 2001·Current Drug Metabolism·S A Sheweita
Sep 25, 2001·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·S AbelD K Walker
Nov 8, 2001·Journal of Clinical Pharmacology·K VenkatakrishnanD J Greenblatt
Dec 18, 2001·Journal of Pharmaceutical Sciences·E H Kerns
Feb 12, 2002·Pharmaceutical Research·Colleen GoosenGordon L Flynn
Mar 20, 2002·Current Topics in Medicinal Chemistry·G W CaldwellZ Yan

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Dec 12, 2012·Journal of Chemical Information and Modeling·Maryam SalahinejadDavid A Winkler
Mar 28, 2013·Daru : Journal of Faculty of Pharmacy, Tehran University of Medical Sciences·Ketan PatelPradeep Vavia
Oct 22, 2011·International Journal of Molecular Sciences·Ndidi C NgwulukaRiaz A Khan
Sep 28, 2013·Pharmaceutical Research·Andrés Olivares-MoralesAmin Rostami-Hodjegan
May 20, 2014·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Corrado BlandizziCarmelo Scarpignato
Nov 12, 2015·Drug Development and Industrial Pharmacy·M R LauroG Puglisi
Sep 21, 2012·Expert Opinion on Drug Discovery·John A Arnott, Sonia Lobo Planey
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Oct 25, 2014·Drug Development and Industrial Pharmacy·Shashank JainSenshang Lin
Oct 16, 2012·Expert Opinion on Drug Delivery·Luana Perioli, Cinzia Pagano
Feb 28, 2015·Drug Development and Industrial Pharmacy·Sue May LimSanjay Garg
Jan 15, 2013·Journal of Pharmaceutical Sciences·Johan Bylund, Tjerk Bueters
Jan 3, 2016·Journal of Ethnopharmacology·Feng ChenNian-Kai Zeng
Dec 3, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Katharina MaiselJustin Hanes
Feb 24, 2010·Journal of Pharmacological and Toxicological Methods·Sandhya Kortagere, Sean Ekins
Aug 1, 2015·CPT: Pharmacometrics & Systems Pharmacology·M SundqvistP Gennemark
Sep 23, 2014·Chemistry & Biology·Bradley Croy DoakJan Kihlberg
Jan 3, 2013·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Tjerk BuetersJohan Bylund
Jun 1, 2017·Journal of Chemical Information and Modeling·Natalia KhuriKathleen M Giacomini
Apr 19, 2018·Pest Management Science·Yu ZhangMike R Loso
Jan 26, 2008·Nature Reviews. Drug Discovery·Jarkko RautioJouko Savolainen
Nov 26, 2009·Chemistry & Biodiversity·Jianling Wang, Suzanne Skolnik
Dec 3, 2013·Chemical & Pharmaceutical Bulletin·Shoko NakashimaYukihiro Ikeda
Oct 27, 2016·Biological Chemistry·Janett MüllerStefan Oswald
Feb 20, 2016·Chembiochem : a European Journal of Chemical Biology·Lauri PaasonenTambet Teesalu
Mar 29, 2020·Biochemical Society Transactions·Gurdeep S Minhas, Simon Newstead
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