Technology: Innovation in Antibiotics by Targeting MetRS

    The Bioxiness technology consists of a scaffold (“blueprint”) designed to inhibit the activity of one of 20 aminoacyl-tRNA synthetases (aaRS), the bacterial enzymes that are essential to all bacteria - Gram-positive or Gram-negative: methionyl-tRNA synthetase (MetRS, shown at right, from Serré et al. 2001)3.

    Bioxiness’ innovation engineers and integrates three ideas:

    1. Design a methionine mimic on the substrate of the natural amino acid, methionine (“analog”),
    2. Cross the bacterial cell wall/membrane by engineering known methods of illicit transport (“Trojan Horse”), then
    3. Induce cell death when intracellular mechanisms cleave the pro-drug construct, yielding an inhibitory active drug (the chemical payload that is released inside the bacterium is toxic to the cell).

    There are no marketed drugs that act on MetRS, so no drug resistance has developed yet to a new class of drugs with this Mechanism of Action.

    Product pipeline

    In industry-standard tests in vitro, Bioxiness' first-generation drug prototypes have shown a very promising pharmacological profile:

    Data Summary

    Because Bioxiness’ first-generation compounds showed anti-microbial activity against Gram-negative and Gram-positive infections in vitro, the company can potentially address a range of possible disease targets.

    Early results showed that Bioxiness may be able to develop drugs that treat Streptococcus pneumoniae. Each year in the US, there are about 4M infections due to S. pneumoniae, of which an estimated 1.2M are drug resistant. Unvaccinated groups such as elderly, children and immunocompromised individuals continue to be at greatest risk.

    In 2017, using results of tests of its next-generation drug candidates, Bioxiness will identify specific diseases where a new anti-infective medicine can make the highest impact.

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