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Fighting gonorrhea – selective antibacterial agents against multidrug-resistant pathogenic gonococci

Abstract

This highly effective and specific antimicrobial agent is suitable for the treatment and prevention of gonococci (gonorrhea). It uses a previously unused mechanism against Neisseria gonorrhoeae and does not affect the natural microbial flora - so further development and approval as an antibiotic would be very worthwhile.

Background

According to the WHO, each year 78 million people contract gonorrhea. As with other sexually transmitted diseases, the number of gonococcal infections has increased significantly in recent years (CDC, press release, 26. Sept. 2017: ‚STDs at record high, indicating urgent need for prevention’).
Due to its growing resistance, the need for effective drugs against the pathogen Neisseria gonorrhoeae (gonococci) is regarded as particularly urgent by the WHO.

Problem

There are active substances available against the pathogen; however resistance has greatly increased worldwide, making treatment with broad-spectrum antibiotics no longer effective. So far, gonococci could not be selectively contained without damaging the healthy microflora of the intestine or vaginal tract through antibiotic treatment. Alarming reports from England and Australia show that first ‚horror gonorrhea isolates’ have been found that are resistant to all approved antibiotics. They are currently considered untreatable.

Solution

Due to its high selectivity and the fact that it spares the natural microbial flora, the new active agent could not only be suitable for effective treatment, but can probably also be used as a prophylaxis for particularly vulnerable population groups. The reason for its specificity seems to be a new mechanism of action, which uses the Achilles’ heel of the pathogen to kill multidrug-resistant gonococci.
The active substances belong to the class of 2-alkyl quinolones and their N-oxides (AQNO); in both the in vitro and the in vivo model with humanized mice, they have shown an enormous potency against gonococci, while no damage of commensal strains or mammalian cells could be detected – therefore subsequent further development and the approval as an antibiotic seem well worthwhile.

Gonococci in the crosshairs. New antibacterial agent works reliably and specifically against gonococci [acc. to T. Böttcher, University of Konstanz].

Advantages

  • Highly effective & specific AB treatment
  • Treatment and prophylaxis for pathogenic, multidrug-resistant gonococci
  • No harmful effects on naturally occurring commensal Neisseria species, commensal microbiota or eukaryotic cells
  • Avoiding resistance development
  • Significant application potential worldwide
  • Effectiveness confirmed in humanized mice

Application

The active substance is suitable both for specific treatment and for the prophylaxis of risk groups.

Exposé
Contact
Anne Böse, M.Sc.
TLB GmbH
Ettlinger Straße 25
76137 Karlsruhe | Germany
Phone +49 721-79004-0
boese(at)tlb.de | www.tlb.de
Development Status
(Mid) preclinical research / TRL4
Patent Situation
PCT WO 2019/121392A1 pending
Reference ID
17/099TLB
Service
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