Patent protection covering clinical candidate FG-2101 composition of matter and methods of use until 2042

, /PRNewswire/ -- Blacksmith Medicines, Inc. (Blacksmith), a leading biopharma dedicated to discovering and developing therapeutics targeting metalloenzymes, today announced that the United States Patent and Trademark Office (USPTO) granted U.S. Patent No. 12,187,754 titled "LpxC Inhibitors and Uses Thereof" a patent directed to composition of matter and methods of use of FG-2101. FG-2101 is a non-hydroxamate small molecule antibiotic candidate discovered at Blacksmith that is designed to selectively inhibit LpxC, a zinc-dependent metalloenzyme found only in Gram-negative bacteria. FG-2101 is being developed for intravenous and oral routes of administration to treat Gram-negative bacteria infections, including drug-resistant strains. FG-2101 has advanced through IND enabling studies and is poised to enter human trials later this year.

In addition to this granted U.S. patent, Blacksmith is pursuing patent protection for FG-2101 in Europe, China, Japan and various other countries worldwide.

"FG-2101 is being developed as a truly unique and novel antibiotic class. In preclinical studies, FG-2101 has shown potent activity against challenging Gram-negative bacteria including extended-spectrum beta-lactamases (ESBL) and carbapenem-resistant Enterobacteriaceae (CRE) as well as in vivo efficacy in multiple infection models using IV and oral formulations," said Zachary Zimmerman, Ph.D., CEO and co-founder of Blacksmith. "The recent granted patent is a significant milestone for Blacksmith as it validates the novelty of the Blacksmith technology platform and continues to fortify the strong global intellectual property portfolio that protects FG-2101." 

The FG-2101 program is currently supported under a contract with NIAID (75N93022C00060). 

About LpxC
LpxC, a zinc-dependent 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 expected benefit of sparing protective Gram-positive bacteria, such as those residing in the 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., use of hydroxamic acid-based warheads) 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:

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