SAN DIEGO, March 19, 2024 /PRNewswire/ -- Blacksmith Medicines, Inc. (Blacksmith), a leading biopharma dedicated to discovering and developing medicines targeting metalloenzymes, announced today that it will present a talk and poster highlighting its novel chemistry technology platform for metalloenzyme inhibitors of LpxC for the treatment of infections caused by multidrug-resistant Gram-negative bacteria at the New Antibacterial Discovery and Development Gordon Research Conference (GRC): Innovative Approaches in Antibacterial Research and Development to Fight the Antibiotic Resistance Crisis being held March 17-22, 2024, in Ventura, CA.
"We are looking forward to attending the GRC and presenting an overview of Blacksmith's discovery platform along with a progress update on our novel class small-molecule antibacterial targeting LpxC," said Andrew Tomaras, Ph.D., Senior Vice President of Blacksmith. "Our lead candidate, currently undergoing IND-enabling studies, has demonstrated activity against susceptible and multidrug-resistant Gram-negative organisms included on the WHO and CDC bacterial threat lists, and is currently being pursued using both IV and oral routes of administration for indications such as UTI."
Talk Presentation Details:
Title: "Anti-Infective Candidates with Novel Targets Using the Blacksmith Discovery Platform"
Category: Discovery Pipelines, Hits, Leads and Candidates
Date and Time: Tuesday, March 19 at 11:05am – 11:25am Pacific
Poster Presentation Details:
Title: "Advanced preclinical in vitro and in vivo characterization of a novel, non-hydroxamate-based LpxC inhibitor for the intravenous and oral treatment of multidrug-resistant Enterobacterales"
Date and Time: Thursday, March 21 at 4:00pm – 6:00pm Pacific
Poster Board Number: 13
More information can be found on the meeting website at 2024 New Antibacterial Discovery and Development GRC and, following the presentation, a version of the poster will be made available on the Blacksmith Medicines website www.BlacksmithMedicines.com
About LpxC
LpxC, a zinc hydrolase, is an attractive and highly sought-after antibiotic target – it is conserved across Gram-negative bacteria and not found in Gram-positive bacteria or human cells. Inhibiting LpxC results in potent killing of Gram-negative bacteria with the benefit of sparing Gram-positive bacteria such as those residing in the protective microbiome of the gut which help to deter opportunistic C. difficile infections.
Other LpxC inhibitors have been evaluated by biopharma in the past but chemistry limitations (e.g. hydroxamic acid) have yielded ineffective compounds that suffer from poor drug-like properties. Thus, there are no approved therapeutics targeting LpxC. Blacksmith, using its proprietary chemistry platform, has developed novel non-hydroxamate inhibitors of LpxC that are safe and effective in animal models of Gram-negative infection and are able to kill Gram-negative 'superbugs' where other antibiotics are ineffective.
About metalloenzymes and the Blacksmith platform
Metalloenzymes utilize a metal ion cofactor in the enzyme active site to perform essential biological functions. This diverse class of targets has historically been difficult to drug due to small molecule chemistry limitations that have plagued the industry. The Blacksmith metalloenzyme platform has solved this problem by leveraging the following:
- A large proprietary fragment library of metal-binding pharmacophores (MBPs);
- A comprehensive database containing a full characterization of the metalloenzyme genome including functions, metal cofactors, and associations to disease;
- A first-of-its-kind metallo-CRISPR library of custom single guide RNAs;
- An industry-leading metalloenzyme computational toolkit for docking, modeling and structure-based drug design; and
- A robust and blocking intellectual property estate covering bioinorganic, medicinal, and computational chemistry approaches for metalloenzyme-targeted medicines.
About Blacksmith Medicines
At Blacksmith Medicines, we are developing medicines targeting metal-dependent enzymes. Over 30% of known enzymes are metalloenzymes, covering all major enzyme classes: oxidoreductases, transferases, hydrolases, lyases, isomerases, and ligases. Metal ions, including magnesium, zinc, iron, manganese and copper, are the essential ingredient in these metalloenzymes. We recognized a large unmet need for new chemical matter and innovative approaches to drug this important class of enzymes. Our purpose-built platform for metalloenzyme-targeted medicines combines, for the first time in industry, a focused library of metal-binding pharmacophores with proprietary computational modeling approaches to rapidly and rationally design small molecule inhibitors that interact with key metal ions in the enzyme's active site. Our comprehensive knowledge of the metal environment and key active site interactions enables Blacksmith to rapidly build potent and selective inhibitors in a stepwise and predictable manner.
Blacksmith has executed strategic drug discovery collaborations with Basilea Pharmaceutica International Ltd., Cyteir Therapeutics Inc., Eli Lilly and Company (Lilly), Hoffmann-La Roche Ltd., and Zoetis LLC., and has been awarded non-dilutive Federal funding agreements with CARB-X and NIH/NIAID. Blacksmith investors include Lilly, Evotec A.G., MP Healthcare Partners, MagnaSci Ventures, and Alexandria Venture Investments.
For further information, please visit the company's website www.BlacksmithMedicines.com and LinkedIn.
Media Contact:
Amy Conrad
Juniper Point
[email protected]
858-366-3243
SOURCE Blacksmith Medicines
![](https://rt.prnewswire.com/rt.gif?NewsItemId=LA58900&Transmission_Id=202403191000PR_NEWS_USPR_____LA58900&DateId=20240319)
Share this article