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25 May 2016

Macrolide Pharmaceuticals Scientific Founder publishes new findings on groundbreaking technology for novel macrolide antibiotics

The paper describes a innovative synthetic chemistry platform that enables access to novel macrolide antibiotics.

Macrolide Pharmaceuticals has announced that a research team led by Macrolide’s scientific founder has published new findings in Nature describing a groundbreaking synthetic chemistry platform that enables access to novel macrolide antibiotics. The paper, entitled “A platform for the discovery of new macrolide antibiotics,” appeared in the May 19 edition of Nature based on research by Ian B. Seiple, PhD, Ziyang Zhang, and other members of Prof. Andrew Myers group at Harvard University.

The fully synthetic macrolide technology discovered by Prof. Myers and his team forms the basis of Macrolide Pharmaceuticals’ unique platform through a licensing agreement from Harvard University. Together with the Myers lab, Macrolide Pharmaceuticals has synthesized more than 600 novel macrolides, and is continuing to make macrolide derivatives that not only address drug-resistant Gram-negative pathogens, but also bacterial resistance mechanisms that limit the efficacy of commercial macrolides.

Notable scientists have reviewed the Nature paper and have applauded the impact of Myers’ technology platform. Ming Yan and Phil S. Baran, PhD, of The Scripps Research Institute comment in Nature: “[Myers and colleagues have developed] a highly modular and versatile chemical-synthesis approach that provides access to a rich array of antibiotics possessing different molecular topologies and functionalities.”

Current macrolide antibiotics, such as clarithromycin and azithromycin, are made by semi-synthesis, wherein the core structure is isolated by a fermentation process and then chemical modifications are made in the laboratory. But this approach has technical limitations.

A number of commentators have grasped the implications of the new approach to macrolide antibiotics, such as Derek Lowe, PhD, in his influential Science Translational Medicine blog, In the Pipeline (“Antibiotics from Scratch” on May 19, 2016, http://blogs.sciencemag.org/pipeline/): “There are more [compounds] to make – the same approach could produce thousands more compounds. It’s still a lot of work, but just getting into the “lot of work” category (and out of the “totally implausible” one) is a big accomplishment.”

“The team at Macrolide Pharmaceuticals has been making good progress, and has identified macrolide scaffolds that have significantly better activity against clinically relevant Gram-negative organisms than any macrolide molecules that have been published to date,” said Larry Miller, CEO of Macrolide Pharmaceuticals. “We are indeed fortunate to have gained an exclusive license to the technology developed by Andy Myers and colleagues, and our initial efforts show encouraging results. We’re confident that we can use this breakthrough to discover new antibiotics to treat the huge unmet clinical need of serious bacterial infections.”

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