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Brilacidin : ウィキペディア英語版
Brilacidin

Brilacidin (formerly PMX-30063〔(【引用サイトリンク】title=Fact Sheet )〕) an investigational new drug (IND), is a polymer-based antibiotic currently in human clinical trials and represents a completely new class of antibiotics called host defense protein mimetics, host defense peptide mimetics, or HDP-mimetics, which are non-peptide synthetic small-molecules modeled after host defense peptides (HDP). HDP, also called antimicrobial peptides, some of which are defensins, are part of the innate immune response and are common to most higher forms of life.〔 Accounts of Chemical Research〕 As Brilacidin is modelled after a defensin, it is also called a defensin mimetic.
Brilacidin is thus an antibiotic that works by disrupting bacterial cell membranes, mimicking defensins that play a role in innate immunity. Several mimics of antimicrobial peptides have been researched, both peptides and non peptides, but none have overcome difficulties to reach the market. Brilacidin, a non-peptide chemical mimic, is an arylamide foldamer designed to replicate the amphiphilic properties of antimicrobial peptides while solving the problems encountered by peptide-based antimicrobials.
Brilacidin, a broad-spectrum antibiotic, has potent Gram positive activity and Gram negative coverage,〔(【引用サイトリンク】 title=ECCMID poster: brilacidin, host defence peptide mimetic, on of a new class of immunomodulatory agents that can target multiple disease indications ) 〕 and is highly effective in treating the 'superbug' methicillin-resistant Staphylococcus aureus (MRSA). Brilacidin has low cytotoxicity against mammalian cells selectively targeting bacteria, directly and rapidly disrupting their membranes, resulting in the bacteria's death. Due to this unique mechanism of action (mimicking the host's natural immune response, proven to be successful in fighting off infections over millions of years of evolution), bacterial antibiotic resistance is less likely to develop.
There has not been a new drug approval from a new class of antibiotics since 1987. While six antibiotics have been approved over the last year, they are all adaptations of existing antibiotic classes. None of the recently approved novel antibiotics represent entirely new classes. Novel antibiotics are crucial as antibiotic resistance is a global health risk. The World Health Organization, warning of a "post-antibiotic era" has stated that antimicrobial resistance (AMR) is a "problem so serious that it threatens the achievements of modern medicine".
== History ==

Leveraging advanced computational bioinformatics,〔(【引用サイトリンク】title=NewWeapons for the Germ Wars )〕〔twst.com〕 Brilacidin and other defensin-mimetics〔(【引用サイトリンク】title=Chemical mimetics of host defense proteins )〕 were first developed by University of Pennsylvania-based researchers. Their efforts were consolidated, and officially incorporated, in 2002, under the company name PolyMedix. Nicholas Landekic was appointed the company's Chief Executive Officer.
Scientists who performed pre-clinical work for PolyMedix included: William DeGrado, a National Academy of Sciences member now at the University of California, San Francisco, and recipient of The American Peptide Society's 2008 Ralph F. Hirschmann Award and The Protein Society's 2015 Stein and Moore Award.;〔(【引用サイトリンク】title=American Chemical Society Awards )〕〔(【引用サイトリンク】title=The Stein And Moore Award )〕 Michael Klein, a National Academy of Sciences member now at Temple University, and current head of the Institute for Computational Molecular Science; Richard Scott, now Vice President of Research at Fox Chase Chemical Diversity Center;〔(【引用サイトリンク】title=FCCDC Leadership )〕 Gregory Tew, now Professor of Polymer Science and Engineering at the University of Massachusetts Amherst,〔(【引用サイトリンク】title=Tew Research Group )〕 and Kenichi Kuroda, now Professor of Biologic & Material Sciences at the University of Michigan.〔(【引用サイトリンク】title=Kuroda Lab )
PolyMedix conducted pre-clinical and clinical research with Brilacidin through a completed Phase 2a human clinical trial with positive results. After discontinuing a clinical trial for an unrelated compound PolyMedix filed for Chapter 7 bankruptcy protection on April 1, 2013. Cellceutix acquired the PolyMedix assets and intellectual property, including the licenses and patents for Brilacidin and the rest of the HDP-Mimetic pipeline, from bankruptcy court which on September 4, 2013 approved Cellceutix's stalking horse bid.〔(【引用サイトリンク】title=SEC Form S3 Filing: Cellceutix )

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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