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Antibiotics and Drug Resistance 2008

Drug Innovation and the Strategy to Combat Antibiotic Resistance Mechanisms

Price: £1,499.00 Approx $2,911.06 (USD) €2,238.92 (EUR)
Overview:
This report reviews new drug innovation and strategy to combat antibiotic resistance mechanisms. This embraces current research-stage activities, patents published in the last five years, the entire pharmaceutical development pipeline and today's existing armoury of anti-bacterial drugs. The report reviews around 400+ pipeline antibiotics and anti-bacterial technologies (from pre-clinical to Phase III/initial launch), 350+ antibiotic patents published between Jan 2002 and Jan 2008 and more than 200 fully launched antibiotics. It identifies and discusses new antibiotics, technologies and strategies at the anti-bacterial mechanistic level, that are specifically being developed to combat resistance mechanisms. The opportunities which they potentially offer in tackling the increasing global threat of antibiotic resistance, are discussed.
This paper is available from one of our partner sites. Click here for details and to download it.

By Dr John Bates / Publication Date: 1st August 2008

Contents:

Report Contents Page
Executive Summary 9
1 INTRODUCTION 14
1.1 Background
1.2 Antibiotic Resistance
1.3 Resistance Mechanisms
1.4 The Resistome
1.5 Pathogenomics
1.6 Antibiotics, Strategies and Targets
1.7 The Cost of Antibiotic Resistance
1.8 Global Surveillance
1.9 This Report
2 ANTIBIOTIC RESISTANCE: GLOBAL FIGURES AND TRENDS 24
Summary
2.1 Antibiotic Resistance
2.2 Europe
2.2.1 Escherichia coli
2.2.2 Streptococcus pneumoniae
2.2.3 Staphylococcus aureus
2.2.4 Enterococci
2.2.5 Klebsiella pneumoniae
2.2.6 Pseudomonas aeruginosa
2.3 England and Wales
2.3.1 Gram-positive cocci
2.3.2 Gram-negative bacilli
2.3.3 Other pathogens
2.4 Other countries
2.5 China
2.6 USA
2.7 Kuwait
2.8 Discussion
3 FULLY LAUNCHED ANTI-BACTERIALS 50
3.1 Current Anti-Infectives
3.2. Anti-bacterials
3.3 Bacterial Cell Wall Inhibitors
3.4 Immune Stimulators
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Antibiotics and Drug Resistance, BioPharm Reports August 2008
3.5 30S/50S Ribosomal Subunit Inhibitors Page
3.6 DNA Gyrase/Topoisomerase Inhibitors
3.7 Other Antibiotics
3.8 Discussion
4 PIPELINE ANTI-BACTERIALS 66
4.1 Pipeline Anti-Infectives
4.2 Developmental Stage
4.3 Mechanisms of Action
4.4 Phase III and Beyond (Late Stage)
4.5 Pre-Clinical to Phase II (Early Stage)
4.5.1 Established Classes
4.5.2 New Classes
4.6 Anti-bacterial Groups
4.6.1 Immune-acting agents
4.6.2 Cell wall inhibitors
4.6.3 DNA topoisomerase ATP hydrolysing inhibitors
4.6.4 Protein 50S ribosomal subunit inhibitors
4.6.5 Protein 30S ribosomal subunit inhibitors
4.6.6 Protein synthesis antagonists
4.6.7 DNA directed DNA polymerase inhibitors
4.6.8 DNA antagonists
4.6.9 DNA topoisomerase IV inhibitors
4.6.10 B anthracis protective antigen inhibitors
4.6.11 Chelating agents
4.6.12 Defensin agonists
4.6.13 Deformylase inhibitors
4.6.14 General pump inhibitors
4.6.15 FABI inhibitors
4.6.16 Membrane integrity antagonists
4.6.17 Membrane permeability enhancers
4.6.18 Dihydrofolate reductase inhibitors
4.6.19 DNA synthesis inhibitors
4.6.20 Lactamase-A inhibitors
4.6.21 Adenosinetriphosphate synthase inhibitors
4.6.22 Deg protease inhibitors
4.6.23 Fab F inhibitors
4.6.24 Gene expression inhibitors
4.6.25 Glutamate racemase inhibitors
4.6.26 Glycosyl transferase inhibitors
4.6.27 Heat shock protein 90 antagonists
4.6.28 Kinase inhibitors
4.6.29 Lipoteichoic acid antagonists
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Antibiotics and Drug Resistance, BioPharm Reports August 2008
4.6.30 PcrV inhibitors Page
4.6.31 Peptidyltransferase inhibitors
4.7 Notable pipeline candidates
4.7.1 Pre-registered and Registered
4.7.2 Phase III
4.7.3 Early-stage
4.8 Discussion
5 EMERGING ANTI-BACTERIALS 80
5.1 Patents
5.2 Antibiotic Classes
5.2.1 Macrolide
5.2.2 Beta-lactam
5.2.3 Peptides
5.2.4 Cephalosporins
5.2.5 Combined antimicrobiols
5.2.6 Carbapenems
5.2.7 Quinolones
5.2.8 General
5.2.9 Vaccines (therapeutic)
5.2.10 Lytics
5.2.11 Bioenhancers
5.2.12 Lactamase inhibitors
5.2.13 Oxazolidinones
5.2.14 Tetracyclines
5.2.15 Natural products
5.2.16 Aminoglycosides
5.2.17 Quorum sensing
5.2.18 Rifamycins
5.2.19 ABC transporter modulator
5.2.20 Glycopeptides
5.2.21 Other technologies
5.2.22 Patent filings organisations
5.3 Discussion
6 COMBATING RESISTANCE MECHANISMS 94
6.1 Background
6.2 New Targets and Mechanisms
6.3 Multiple Activities
6.4 Circumventing Resistance
6.5 Resistance Mutations
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6.6 Virulence Page
6.7 Other Technologies
6.8 Discussion
CHAPTER 7 COMPANIES AND ORIGINATORS 107
7.1 Companies

List of Tables:

TABLES

Table 2.1 EARSS surveillance programme: countries and country codes
Table 3.1a. Fully launched antibiotics – bacterial cell wall inhibitors (ß-lactams) (Source: Company Research May 2007, Pharmaprojects May 2007)
Table 3.1b. Approved antibiotics – bacterial cell wall inhibitors (ß-lactams) (Source: Company Research May 2007, Pharmaprojects May 2007)
Table 3.2a. Approved antibiotics – Immune Stimulators/Modulators (Source: Company Research May 2007, Pharmaprojects May 2007)
Table 3.2b. Approved antibiotics – Immune Stimulators/Modulators (Source: Company Research May 2007, Pharmaprojects May 2007)
Table 3.3 Approved antibiotics – Protein 30S/50S Ribosomal Subunit Inhibitors (Source: Company Research May 2007, Pharmaprojects May 2007)
Table 3.4 Approved antibiotics – DNA topoisomerase ATP hydrolysing inhibitor (Source: Company Research May 2007, Pharmaprojects May 2007)
Table 3.5a Approved antibiotics – Other antibiotics (Source: Company Research May 2007, Pharmaprojects May 2007)
Table 3.5b Approved antibiotics – Other antibiotics (Source: Company Research May 2007, Pharmaprojects May 2007)
Table 3.5c Approved antibiotics – Other antibiotics (Source: Company Research May 2007, Pharmaprojects May 2007)
3.8 Discussion
Table 4.1 Pipeline Anti-Infectives (Source: Company Research May 2007, Pharmaprojects May 2007)
Table 4.2 Pipeline Anti-infectives (Source: Company Research May 2007, Pharmaprojects May 2007)
Table 4.3 Pipeline Anti-Infectives (Source: Company Research May 2007, Pharmaprojects May 2007)
Figure 7.1 The top 20 companies with fully launched anti-bacterials (Source: Independent Research, Pharmaprojects 2007)
Figure 7.2 The top 20 anti-bacterial development companies, representing candidates in the development pipeline (pre-clinical to Phase III/initial launch) (Source: Independent Research, Pharmaprojects 2007)
Figure 7.3 The top 20 anti-bacterial patent filing organisations of 340 patents selected for analysis in this report. (Source: Delphion)

FIGURES

Figure 2.1 Escherichia coli: Combined resistance (fluoroquinolones, third-generation cephalosporins and aminoglycosides) by country 2001–2005. Only countries that reported 20 isolates or more per year for at least 3 years were included. The arrows indicate significant trends (Source: EARSS).
Figure 2.2 Streptococcus pneumoniae: Dual resistance to penicillin and erythromycin by country, 1999–2005. Only countries that reported 20 isolates or more per year for at least 3 years were included. The arrows indicate significant trends (Source: EARSS).
Figure 2.3 Staphylococcus aureus: Resistance to methicillin by country, 1999–2005. Only countries that reported 20 isolates or more per year for at least 3 years were included. The arrows indicate significant trends (Source: EARSS).
Figure 2.4 Staphylococcus aureus: MRSA levels in England and Wales, 1992–2005. (Source UK Health Protection Agency, Trends in Antimicrobiol Resistance in England and Wales, 2004–2005).
Figure 2.5 Enterococcus faecalis: Trends in high aminoglycoside resistance by country 2001–2005. Only countries that reported 20 isolates or more per year for at least 3 years were included. The arrows indicate significant trends (Source: EARSS).
Figure 2.6 Klebsiella pneumoniae: Trends in high aminoglycoside resistance by country in 2002 and 2005. Only countries that reported 20 isolates or more per year for at least 3 years were included (Source: EARSS).
Figure 2.7 Pseudomonas aeruginosa: Trends in high aminoglycoside resistance by country in 2002 and 2005. Only countries that reported 20 isolates or more per year for at least 3 years were included (Source: EARSS).
Figure 2.8 Antibiotic resistance of gram-positive cocci in England and Wales, 2004–2005 (Source: UK Health Protection Agency, Trends in Antimicrobiol Resistance in England and Wales, 2004–2005.
Figure 2.9 Antibiotic resistance of gram-negative bacilli in England and Wales, 2004–2005 (Source: UK Health Protection Agency, Trends in Antimicrobiol Resistance in England and Wales, 2004–2005.
Figure 2.10 Antibiotic resistance of other bacteria in England and Wales, 2004–2005 (Source: UK Health Protection Agency, Trends in Antimicrobiol Resistance in England and Wales, 2004–2005).
Figure 2.11 Antibiotic resistance of Staphylococcus, Streptococcus, Escherichia coli and Enterococcus in the US, Egypt and Tunisia (Source: Frimodt-Møller et al., Danish Medical Bulletin Vol. 54, May 2007)
Figure 3.1 Current, fully launched anti-infectives (Independent Research, Pharmaprojects 2007)
Figure 3.2 Categories of fully approved anti-bacterial therapeutics (Independent Research, Pharmaprojects 2007)