GLYCOPEPTIDE ANTIBIOTICS: from Old Mississipi mud to new derivatives -- a critical appraisal

Table of Contents

GLYCOPEPTIDE ANTIBIOTICS from Old Mississipi mud …  … to new derivatives:   a critical appraisal

Glycopeptide story: from natural to semi-synthetic derivatives

Glycopeptide story: from natural to semi-synthetic derivatives

Peptidoglycan synthesis

Glycopeptide mechanism of action

But resistance came in ...

Resistance in enterococci

Resistance in enterococci

Resistance in enterococci

Resistance in enterococci

Resistance in staphylococci (GISA)

Resistance in staphylococci (GISA)

Resistance in staphylococci (GRSA)

Glycopeptides: what can we improve ?

Glycopeptide updated mechanism of action

Glycopeptide updated mechanism of action in VRE

Glycopeptides: how can we improve ?

Glycopeptides: how can we improve ?

Glycopeptides: how can we improve ?

Glycopeptides: how can we improve ?

Molecules in clinical development:DESIGN

From vancomycin to oritavancin

From vancomycin to oritavancin

From vancomycin to oritavancin

From vancomycin to oritavancin

From teicoplanin to dalbavancin

From teicoplanin to dalbavancin

From teicoplanin to dalbavancin

From teicoplanin to dalbavancin

Molecules in clinical development:IN VITRO DATAmicrobiologypharmacodynamics

Spectrum of activity

Pharmacodynamic properties of oritavancin

PK/PD properties of oritavancinin a model of S.aureus infected macrophages

Molecules in clinical development:IN VIVO DATApharmacokineticspharmacodynamics

Pharmacokinetic properties

PK/PD profile

Safety profile

Molecules in clinical development:IN VIVO DATAclinical studies

Clinical experience

Clinical experience

In which indications could they be useful ?

Research is still active …

Research is still active …

We are looking forward these new antibiotics …

Email: tulkens@facm.ucl.ac.be

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