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Drug Discovery

 

Figure 1: Schematic representation of body compartments in physiologically based pharmacokinetic modelling. Abbreviations: Qorgan: Blood flow to organ
Figure 1: Schematic representation of body compartments in physiologically based pharmacokinetic modelling. Abbreviations: Qorgan: Blood flow to organ
article

Physiologicaly based pharmacokinetic modelling of transporters in drug discovery and development

3 September 2012 | By Pradeep Sharma and Katherine Fenner, Global DMPK, AstraZeneca R&D

Physiologically based pharmacokinetic (PBPK) models describe the different compartments (tissues) in the body linked via arterial and venous blood flow (Figure 1). The volume of each tissue and blood flows are available from literature data1-5 and PBPK models have been developed for many species including rat, mouse, dog, pig and…

Man on a phone analysing data and charts on computer screen
Man on a phone analysing data and charts on computer screen
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Integrating preclinical data into early clinical development

3 September 2012 | By Vikash Sinha, Clinical Pharmacology Leader, Janssen Research and Development

One of the important goals in preclinical and early clinical drug development is to reduce attrition rates and to improve our ability to pick winners and drop potential loser drug candidates. By being able to efficiently translate preclinical data and observations into possible clinical outcomes, one can make the drug…

drug discovery & drug development
drug discovery & drug development
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The need for proteomic-based biomarkers in the drug development pipeline

10 July 2012 | By Paul C. Guest, Department of Chemical Engineering and Biotechnology, University of Cambridge and Sabine Bahn Department of Chemical Engineering and Biotechnology, University of Cambridge & Department of Neuroscience, Erasmus Medical Centre

Pharmaceutical companies are under increasing pressure to improve their efficiency and returns on drug discovery projects. This is a daunting task considering that the average drug costs approximately one billion US dollars to develop and takes around 12 years from initial discovery to reach the market1. In addition, approximately 70…

article

Discovery chemistry outsourcing

26 April 2012 | By Luigi La Vecchia, Director of the Preparations Laboratories, Novartis Institute for Biomedical Research

In 2002, Novartis decided to create a new research centre in Cambridge, MA. This was accompanied by a significant increase in headcount in medicinal chemistry. Within two years, this resulted in a strongly increased demand for prep-scale synthesis which in turn led to priority issues and to prolonged turnaround times…

article

Outsourcing in early drug discovery: Evolution and opportunities

26 April 2012 | By Jayshree Mistry, Paul Lloyd, Kevin Oliver and Peter North, GlaxoSmithKline R&D and Duncan Judd, Awridian

This article describes the evolution of outsourcing within early drug discovery at GlaxoSmithKline (GSK), specifically for chemistry services applied to developing a compound from the screening hit through lead optimisation. It will touch on different business models, factors to consider when selecting potential CROs, the benefits of outsourcing and CRO…

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GPCR screening and drug discovery: Challenges and latest trends

26 April 2012 | By Sofia M.A. Martins, João R.C. Trabuco, Gabriel A. Monteiro and Duarte Miguel Prazeres, Institute for Biotechnology and Bioengineering, Instituto Superior Técnico, Technical University of Lisbon

G-protein coupled receptors (GPCRs) are one of the most popular drug targets today. Almost one third of the approved drugs currently available rely on some kind of interaction with these receptors. The annual revenues are around USD 30 billion (109) and the fact that one quarter of the top US…

article

MRI in drug discovery

28 February 2012 | By Peter R. Allegrini, Novartis Institutes for BioMedical Research

MRI is widely used for clinical diagnosis as well as in research areas such as preclinical drug discovery, clinical development and also in therapy monitoring. MRI allows non-invasive acquisition of tomographic images of soft tissue with high resolution and contrast. Furthermore, its ability to assess organ function in a broad…

article

Drug discovery leaders roundtable

13 December 2011 | By Andrew A. Parsons, Vice President Preclinical Drug Development, GlaxoSmithKline and Steve Street, Vice President, Head of Research Centres of Emphasis, Head of WRD Continuous Improvement, Pfizer and William Strohl, Vice President of Biologics Research, Centocor R&D, a division of Johnson & Johnson Pharmaceutical Research & Development and Eckhard von Keutz, Senior Vice President, Head Global Early Development, Bayer HealthCare

External economic pressures have been identified as the major driver for the pharmaceutical outsourcing market. Over and above the fiscal advantages of adopting this strategy, what other benefits and indeed risks do you see associated with this approach? Steve Street: We definitely began our out - sourcing efforts based on…

FIGURE 1 Schematic overview of a typical homology modelling procedure that is used to build threedimensional coordinates for a protein of unknown structure
FIGURE 1 Schematic overview of a typical homology modelling procedure that is used to build threedimensional coordinates for a protein of unknown structure
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Status and challenges in structure-based drug discovery for G protein-coupled receptors

13 December 2011 | By Henri Xhaard, Head of Computational Drug Discovery Group, Centre for Drug Research, University of Helsinki

The central location of G protein-coupled receptors (GPCRs) at the interface between the interior and exterior of cells, as well as their key role in signalling events, make GPCRs a prominent class of pharmaceutical targets. To date, approximately 40 per cent of known drugs are thought to act on GPCRs…

Drug discovery assays for the histone deacetylase class of enzymes
Drug discovery assays for the histone deacetylase class of enzymes
article

Implementing electronic laboratory notebooks to improve the efficiency of pre-clinical drug discovery

13 December 2011 | By Sheraz Gul, Vice President and Head of Biology, European ScreeningPort GmbH

The pre-clinical phase of drug discovery spans a period in the region of five years and requires contributions from multi-disciplinary teams often working at different sites. These teams can generate significant amounts of data which are processed using standard as well as specialist software. The recording of a substantial amount…

FIGURE 1 The rapid evolution of sequencing technologies. A. First generation Sanger sequencing technology. B. Second ‘Next’ generation massively parallel sequencing technology (454 Sequencing © Roche Diagnostics) C. Third ‘Next-Next’ generation single molecule, real-time sequencing technology. In the coming years, second or third generation technologies may develop to an extent where a human genome can be sequenced for a USD 1,000 in a matter of hours
FIGURE 1 The rapid evolution of sequencing technologies. A. First generation Sanger sequencing technology. B. Second ‘Next’ generation massively parallel sequencing technology (454 Sequencing © Roche Diagnostics) C. Third ‘Next-Next’ generation single molecule, real-time sequencing technology. In the coming years, second or third generation technologies may develop to an extent where a human genome can be sequenced for a USD 1,000 in a matter of hours
article

DNA sequencing technologies and emerging applications in drug discovery

13 December 2011 | By Nalini A.L. Mehta & David J. Dow, Molecular and Cellular Technologies, Platform Technology and Science, GlaxoSmithKline and Anthony M. Battram, Molecular and Cellular Technologies, Platform Technology and Science, GlaxoSmithKline & Department of Life Sciences, Imperial College London

In recent years, the development of Next Generation DNA Sequencing (NGS) technology has significantly impacted molecular biology research, resulting in many new insights and discoveries. NGS technology goes beyond traditional DNA sequencing with applications that reach across the central dogma of molecular biology from DNA to RNA and protein science.…

FIGURE 1 Schematic overview of the MALDI-MSI process as applied to imaging compound and metabolite distributions in a whole body rat sample. From one section of an animal dosed with the unlabelled compound, the substance and metabolite distributions can be acquired
FIGURE 1 Schematic overview of the MALDI-MSI process as applied to imaging compound and metabolite distributions in a whole body rat sample. From one section of an animal dosed with the unlabelled compound, the substance and metabolite distributions can be acquired
article

MALDI-mass spectrometry imaging applied to drug discovery and development

19 October 2011 | By Brendan Prideaux, Dieter Staab, Gregory Morandi, Nicole Ehrhard and Markus Stoeckli, Novartis Institutes for BioMedical Research

Since its introduction in the field of biomedical imaging over 10 years ago1, matrixassisted laser desorption/ionisation mass spectrometry imaging (MALDI-MSI) has played an ever increasing role in drug discovery and development and is now utilised in laboratories of many leading pharmaceutical companies and collaborating academic institutions.