Delving into the Latest Updates on GraR inhibitors(Compound F12) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

GraR

Action

inhibitors

Mechanism

GraR inhibitors(Bacteria Response regulator protein inhibitors)

Therapeutic Areas

Infectious Diseases

Active Indication-

Inactive Indication

MRSA - Methicillin resistant Staphylococcus aureus infection

Originator Organization

Case Western Reserve University School of MedicineQ2 Pharma Ltd.

Active Organization-

Inactive Organization

Case Western Reserve University School of MedicineQ2 Pharma Ltd.

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

AbstractSmall-molecule antivirulence agents represent a promising alternative or adjuvant to antibiotics. These compounds disarm pathogens of disease-causing toxins without killing them, thereby diminishing survival pressure to develop resistance. Here we show that the small-molecule antivirulence agents F12 and F19 block staphylococcal transcription factor AgrA from binding to its promoter. Consequently, toxin expression is inhibited, thus preventing host cell damage by Gram-positive pathogens. Broad spectrum efficacy against Gram-positive pathogens is due to the existence of AgrA homologs in many Gram-positive bacteria. F12 is more efficacious in vitro and F19 works better in vivo. In a murine MRSA bacteremia/sepsis model, F19 treatment alone resulted in 100% survival while untreated animals had 70% mortality. Furthermore, F19 enhances antibiotic efficacy in vivo. Notably, in a murine MRSA wound infection model, combination of F19 with antibiotics resulted in bacterial load reduction. Thus, F19 could be used alone or in combination with antibiotics to prevent and treat infections of Gram-positive pathogens.

100 Deals associated with GraR inhibitors(Compound F12)

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
MRSA - Methicillin resistant Staphylococcus aureus infection	Preclinical	United States	Case Western Reserve University School of Medicine	01 Oct 2018
MRSA - Methicillin resistant Staphylococcus aureus infection	Preclinical	Israel	Q2 Pharma Ltd.	01 Oct 2018