INHIBITORS OF HSRA FOR TREATING HELICOBACTER PYLORI INFECTION

Desarrollado por: Fundación Instituto de Investigación Sanitaria Aragón

Descripción

Helicobacter pylori is considered the most prevalent human pathogen since nearly half of the world's population is infected by this bacterium. Persistent colonization of human stomach by H. pylori results in gastric inflammation and highly contributes to the pathogenesis of peptic ulceration, gastric adenocarcinoma, andmucosa-associated lymphoid-tissue (MALT) lymphoma. Nearly 60% of the intestinal type gastric cancers and 98% of MALT lymphomas are associated with H. pylori infections. In addition, the presence of H. pylori in the host increases the risk of developing other lymphomas, such as diffuse large B cell lymphoma and ocular adnexal lymphoma.
The standard triple therapy containing a proton-pump inhibitor (PPI) and a combination of two antibiotics (clarithromycin and amoxicillin/metronidazole) is considered the first-line regimen for treatment of H. pylori. However, this PPI-based triple therapy has been reported to be losing its efficacy for H. pylori, with eradication
rates as low as 50% to 70%, mainly due to high levels of antibiotic resistance, high rates of antibiotic-associated side effects and low compliance.
The compounds of the invention have high bactericidal activity even on metronidazole and clarithromycin-resistant H. pylori strains through a novel molecular mechanism of antimicrobial action of these compounds on H. pylori: the inhibition of the essential response regulator HsrA.

Aplicaciones

The compounds of the invention are high effective as antibiotics against H. pylori.
These novel antimicrobials are FDA-approved low-molecular-weight drugs prescribed for other therapeutic uses which will considerably reduce the effort required for its implementation.
These compounds are not affected by the molecular mechanisms of metronidazole and clarithromycin resistance evolved by H. pylori.

Estado de protección

Spanish patent application (2018) and international patent application (PCT, 2019) with extension possibilities.

Cooperación que se desea

  • Further research or development
  • Exclusive/non-exclusive licence agreement
Estado:
Transferible
Tecnología sanitaria:
Medicamentos - Farma