Skip to main content
SpringerLink
Log in

Neue Antibiotika auf dem Markt und in Entwicklung

New antibacterial agents on the market and in the pipeline

  • Schwerpunkt
  • Published:
Der Internist Aims and scope Submit manuscript

Zusammenfassung

Nach Jahren der Stagnation sind inzwischen wieder zahlreiche Neuentwicklungen im Bereich der antibakteriellen Substanzen zu verzeichnen. Überwiegend handelt es sich dabei jedoch um Weiterentwicklungen bestehender Klassen. Unter den β-Laktamen sind dies Cephalosporine mit Wirksamkeit bei methicillinresistentem Staphylococcus aureus (Ceftarolin und Ceftobiprol) und neue Kombinationen von β-Laktamen mit β-Laktamase-Inhibitoren (Ceftolozan/Tazobactam, Ceftazidim/Avibactam, Imipenem/Relebactam, Meropenem/RPX7009). Weiterentwicklungen gibt es auch bei anderen Substanzklassen, z. B. bei den Oxazolidinonen (Tedizolid, Radezolid, Cadazolid, MRX-I), Makroliden und Ketoliden (Modithromycin, Solithromycin), Aminoglykosiden (Plazomicin), Chinolonen (Nemonoxacin, Delafloxacin, Avarofloxacin), Tetrazyklinen (Omadacyclin, Eravacyclin) und bei den Glyko- und Lipopeptidantibiotika (Oritavancin, Telavancin, Dalbavancin, Surotomycin). Neu, aber noch sehr früh in der Entwicklung sind FabI-Inhibitoren, Endolysine, Peptidomimetika, Lipid-A-Inhibitoren, Methionyl-tRNA-Synthetase-Inhibitoren und Teixobactin.

Abstract

After some years of stagnation there have been several new successful developments in the field of antibacterial agents. Most of these new developments have been in conventional antibacterial classes. New drugs among the beta-lactam agents are methicillin-resistant Staphylococcus aureus (MRSA) active cephalosporins (ceftaroline and ceftobiprole) and new combinations of beta-lactam with beta-lactamase inhibitors (ceftolozane/tazobactam, ceftazidime/avibactam, imipenem/relebactam and meropenem/RPX7009). New developments can also be observed among oxazolidinones (tedizolid, radezolid, cadazolid and MRX-I), macrolides/ketolides (modithromycin and solithromycin), aminoglycosides (plazomicin), quinolones (nemonoxacin, delafloxacin and avarofloxacin), tetracyclines (omadacycline and eravacycline) as well as among glycopeptides and lipopeptides (oritavancin, telavancin, dalbavancin and surotomycin). New agents in a very early developmental phase are FabI inhibitors, endolysines, peptidomimetics, lipid A inhibitors, methionyl-tRNA synthetase inhibitors and teixobactin.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Abb. 1
Abb. 2

Literatur

  1. Almaghrabi R, Clancy CJ, Doi Y et al (2014) Carbapenem-resistant Klebsiella pneumoniae strains exhibit diversity in aminoglycoside-modifying enzymes, which exert differing effects on plazomicin and other agents. Antimicrob Agents Chemother 58:4443–4451

    Article  PubMed Central  PubMed  Google Scholar 

  2. Awad SS, Rodriguez AH, Chuang YC et al (2014) A phase 3 randomized double-blind comparison of ceftobiprole medocaril versus ceftazidime plus linezolid for the treatment of hospital-acquired pneumonia. Clin Infect Dis 59:51–61

    Article  PubMed Central  CAS  PubMed  Google Scholar 

  3. Chan LC, Basuino L, Dip EC, Chambers HF (2015) Comparative efficacies of tedizolid phosphate, vancomycin, and daptomycin in a rabbit model of methicillin-resistant Staphylococcus aureus endocarditis. Antimicrob Agents Chemother 59(6):3252–3256

    Article  CAS  PubMed  Google Scholar 

  4. Drawz SM, Papp-Wallace KM, Bonomo RA (2014) New β-lactamase inhibitors: a therapeutic renaissance in an MDR world. Antimicrob Agents Chemother 58:1835–1846

    Article  PubMed Central  PubMed  Google Scholar 

  5. Dryden M, Wilson D, Iaconis J, Gonzalez J (2015) A phase III trial of ceftaroline fosamil 600 mg q8 h versus vancomycin plus aztreonam in patients with cSSTI with systemic inflammatory response or underlying comorbidities. 25th ECCMID, Kopenhagen. Abstract O193

  6. Henson KE, Levine MT, Wong EA, Levine DP (2015) Glycopeptide antibiotics: evolving resistance, pharmacology and adverse event profile. Expert Rev Anti Infect Ther 13:1265–1278

    Article  PubMed  Google Scholar 

  7. Hook EW 3rd, Golden M, Jamieson BD et al (2015) A phase 2 trial of oral solithromycin 1200 mg or 1000 mg as single-dose oral therapy for uncomplicated gonorrhea. Clin Infect Dis 61:1043–1048

    Article  PubMed  Google Scholar 

  8. Ivarsson ME, Leroux JC, Castagner B (2015) Investigational new treatments for Clostridium difficile infection. Drug Discov Today 20(5):602–608

    Article  CAS  PubMed  Google Scholar 

  9. Jacobsson S, Golparian D, Phan LT et al (2015) In vitro activities of the novel bicyclolides modithromycin (EDP-420, EP-013420, S-013420) and EDP-322 against MDR clinical Neisseria gonorrhoeae isolates and international reference strains. J Antimicrob Chemother 70:173–177

  10. Kiang TK, Wilby KJ, Ensom MH (2015) A critical review on the clinical pharmacokinetics, pharmacodynamics, and clinical trials of ceftaroline. Clin Pharmacokinet 54:915–931

    Article  CAS  PubMed  Google Scholar 

  11. Lee CR, Lee JH, Jeong BC, Lee SH (2013) Lipid A biosynthesis of multidrug-resistant pathogens – a novel drug target. Curr Pharm Des 19(36):6534–6350

    Article  CAS  PubMed  Google Scholar 

  12. Ling LL, Schneider T, Peoples AJ et al (2015) A new antibiotic kills pathogens without detectable resistance. Nature 517:455–459

    Article  CAS  PubMed  Google Scholar 

  13. Louie T, Nord CE, Talbot GH et al (2015) A multicenter, double-blind, randomized, phase 2 study evaluating the novel antibiotic, cadazolid, in patients with Clostridium difficile infection. Antimicrob Agents Chemother 59:6266–6273

    Article  PubMed Central  PubMed  Google Scholar 

  14. Macone AB, Caruso BK, Leahy RG et al (2014) In vitro and in vivo antibacterial activities of omadacycline, a novel aminomethylcycline. Antimicrob Agents Chemother 58:1127–1135

    Article  PubMed Central  CAS  PubMed  Google Scholar 

  15. Mazuski JE, Gasink L, Armstrong J (2015) Efficacy and safety of ceftazidime-avibactam plus metronidazole versus meropenem in the treatment of complicated intra-abdominal infection – results from a phase III programme. 25th ECCMID, Kopenhagen. Abstract O191

  16. Mensa B, Howell GL, Scott R, DeGrado WF (2014) Comparative mechanistic studies of brilacidin, daptomycin, and the antimicrobial peptide LL16. Antimicrob Agents Chemother 58:5136–5145

    Article  PubMed Central  PubMed  Google Scholar 

  17. Morata L, Mensa J, Soriano A (2015) New antibiotics against gram-positives: present and future indications. Curr Opin Pharmacol 24:45–45

    Article  CAS  PubMed  Google Scholar 

  18. Nathan C, Cars O (2014) Antibiotic resistance – problems, progress, and prospects. N Engl J Med 371:1761–1763

  19. Oldach D, Barrera C, Mykietiuk A et al (2015) SOLITAIRE-oral: results of a global phase 3 trial comparing oral solithromycin versus oral moxifloxacin for treatment of community-acquired bacterial pneumonia (CABP) in adults. 25th ECCMID, Kopenhagen. Abstract LBOS0239c

  20. Page MG, Bush K (2014) Discovery and development of new antibacterial agents targeting gram-negative bacteria in the era of pandrug resistance: is the future promising? Curr Opin Pharmacol 18:91–97

    Article  CAS  PubMed  Google Scholar 

  21. Ram S, Menon K, Scott RW et al (2015) Synthetic novel host defense protein mimetics for the treatment of gram-negative bacterial infections. 25th ECCMID, Kopenhagen. Abstract O082

  22. Solomkin J, Hershberger E, Miller B et al (2015) Ceftolozane/tazobactam plus metronidazole for complicated intra-abdominal infections in an era of multidrug resistance: results from a randomized, double-blind, phase 3 trial (ASPECT-cIAI). Clin Infect Dis 60:1462–1471

    PubMed Central  PubMed  Google Scholar 

  23. Solomkin J, Slepavicius A, Evans D et al (2015) Results of IGNITE1: a phase 3 study to evaluate the efficacy and safety of eravacycline versus ertapenem in complicated intraabdominal infections. 25th ECCMID, Kopenhagen. Abstract LBOS0239d

  24. Spellberg B, Bartlett J, Wunderink R, Gilbert DN (2015) Novel approaches are needed to develop tomorrow’s antibacterial therapies. Am J Respir Crit Care Med 191:135–140

    Article  PubMed  Google Scholar 

  25. Sutcliffe JA, O’Brien W, Fyfe C, Grossman TH (2013) Antibacterial activity of eravacycline (TP-434), a novel fluorocycline, against hospital and community pathogens. Antimicrob Agents Chemother 57:5548–5558

    Article  PubMed Central  CAS  PubMed  Google Scholar 

  26. Syed YY (2014) Ceftobiprole medocaril: a review of its use in patients with hospital- or community-acquired pneumonia. Drugs 74:1523–1542

    Article  CAS  PubMed  Google Scholar 

  27. Tsai L, Marsh A, Horn P, Lloyd K (2015) Results of the lead-in study on the safety and efficacy of eravacycline versus levofloxacin in complicated urinary tract infections (cUTI). 25th ECCMID, Kopenhagen. Abstract O198

  28. Bambeke F van (2014) Renaissance of antibiotics against difficult infections: focus on oritavancin and new ketolides and quinolones. Ann Med 46:512–529

    Article  PubMed  Google Scholar 

  29. Wagenlehner FM, Umeh O, Steenbergen J et al (2015) Ceftolozane-tazobactam compared with levofloxacin in the treatment of complicated urinary-tract infections, including pyelonephritis: a randomised, double-blind, phase 3 trial (ASPECT-cUTI). Lancet 385:1949–1956

    Article  CAS  PubMed  Google Scholar 

  30. Wang Y, Lv Y, Cai J et al (2015) A novel gene, optrA, that confers transferable resistance to oxazolidinones and phenicols and its presence in Enterococcus faecalis and Enterococcus faecium of human and animal origin. J Antimicrob Chemother 70(8):2182–2190

  31. Zhong NS, Sun T, Zhuo C et al (2015) Ceftaroline fosamil versus ceftriaxone for the treatment of Asian patients with community-acquired pneumonia: a randomised, controlled, double-blind, phase 3, non-inferiority with nested superiority trial. Lancet Infect Dis 15:161–171

    Article  CAS  PubMed  Google Scholar 

  32. http://www.chemspider.com/

  33. https://pubchem.ncbi.nlm.nih.gov/

Download references

Einhaltung ethischer Richtlinien

Interessenkonflikt. W.V. Kern erhielt Forschungsbeihilfen (Drittmittel) von BMS, Boehringer, Gilead, GSK, Janssen, Pfizer und ViiV, Vortragshonorare von AstraZeneca, Infectopharm und Pfizer sowie eine Vergütung für Beratertätigkeiten von AstraZeneca, Roche, SOBI und Stiftung Warentest.

Dieser Beitrag beinhaltet keine Studien an Menschen oder Tieren.

Author information

Authors and Affiliations

  1. Abteilung Infektiologie, Klinik für Innere Medizin II, Universitätsklinikum Freiburg, Hugstetter Str. 55, 79106, Freiburg, Deutschland

    W.V. Kern

Authors
  1. W.V. Kern
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to W.V. Kern.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Kern, W. Neue Antibiotika auf dem Markt und in Entwicklung. Internist 56, 1255–1263 (2015). https://doi.org/10.1007/s00108-015-3705-0

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s00108-015-3705-0

Schlüsselwörter

Keywords

Search

Navigation