High-throughput in vitro profiling assays:: lessons learnt from experiences at Novartis

被引：24

作者：

Faller, Bernard ^{[1
]}

Wang, Jianling

Zimmerlin, Alfred

Bell, Leslie

Hamon, Jacques

Whitebread, Steven

Azzaoui, Kamal

Bojanic, Dejan

Urban, Laszlo

机构：

[1] Novartis Inst Biomed Res, Basel, Switzerland

[2] Novartis Inst Biomed Res, Cambridge, MA USA

来源：

EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY | 2006年 / 2卷 / 06期

关键词：

absorption; adverse effects; drug disposition; exposure; metabolism; molecular properties;

D O I：

10.1517/17425255.2.6.823

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

This article reviews the use of a selection of in vitro assays implemented at Novartis and intends to address exposure and safety in early drug discovery. The authors' own experience, based on a large number of 'real' drug discovery compounds, is described to reflect on what has worked, where improvement is needed and how to best use the data for decision making. Possible strategies are discussed, and guidelines are provided on how to organise assays, extract value and contribute knowledge from the data.

引用

页码：823 / 833

页数：11

共 72 条

[1] IMPROVED BACTERIAL TEST SYSTEM FOR DETECTION AND CLASSIFICATION OF MUTAGENS AND CARCINOGENS
AMES, BN
LEE, FD
DURSTON, WE
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1973, 70 (03) : 782 - 786
[2] Assessment of drug interactions in hepatobiliary transport using rhodamine 123 in sandwich-cultured rat hepatocytes
Annaert, PP
Brouwer, KLR
[J]. DRUG METABOLISM AND DISPOSITION, 2005, 33 (03) : 388 - 394
[3] CORRELATION BETWEEN ORAL-DRUG ABSORPTION IN HUMANS AND APPARENT DRUG PERMEABILITY COEFFICIENTS IN HUMAN INTESTINAL EPITHELIAL (CACO-2) CELLS
ARTURSSON, P
KARLSSON, J
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1991, 175 (03) : 880 - 885
[4] PAMPA - A drug absorption in vitro model 13. Chemical selectivity due to membrane hydrogen bonding: In combo comparisons of HDM-, DOPC-, and DS-PAMPA models
Avdeef, A
Tsinman, O
[J]. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2006, 28 (1-2) : 43 - 50
[5] Caco-2 permeability of weakly basic drugs predicted with the Double-Sink PAMPA pKaflux method
Avdeef, A
Artursson, P
Neuhoff, S
Lazorova, L
Gråsjö, J
Tavelin, S
[J]. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2005, 24 (04) : 333 - 349
[6] Avdeef A., 2003, ABSORPTION DRUG DEV, DOI [10.1002/047145026X, DOI 10.1002/047145026X]
[7] Avdeef Alex, 2001, Current Topics in Medicinal Chemistry, V1, P277, DOI 10.2174/1568026013395100
[8] Accuracy of calculated pH-dependent aqueous drug solubility
Bergström, CAS
Luthman, K
Artursson, P
[J]. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2004, 22 (05) : 387 - 398
[9] A high-throughput screening method for the determination of aqueous drug solubility using laser nephelometry in microtiter plates
Bevan, CD
Lloyd, RS
[J]. ANALYTICAL CHEMISTRY, 2000, 72 (08) : 1781 - 1787
[10] The conduct of in vitro and in vivo drug-drug interaction studies: A Pharmaceutical Research and Manufacturers of America (PhRMA) perspective
Bjornsson, TD
Callaghan, JT
Einolf, HJ
Fischer, V
Gan, L
Grimm, S
Kao, J
King, SP
Miwa, G
Ni, L
Kumar, G
McLeod, J
Obach, RS
Roberts, S
Roe, A
Shah, A
Snikeris, F
Sullivan, JT
Tweedie, D
Vega, JM
Walsh, J
Wrighton, SA
[J]. DRUG METABOLISM AND DISPOSITION, 2003, 31 (07) : 815 - 832

← 1 2 3 4 5 6 7 8 →