First ever non-hydroxamate inhibitor of LpxC to demonstrate efficacy in preclinical models of Gram-negative bacteria infection
San Diego, Calif., June 14, 2016 – Forge Therapeutics, Inc. today announced a scientific presentation at the American Society of Microbiology titled, “Non-hydroxamic Acid LpxC Inhibitors: In Vitro and In Vivo Antimicrobial Activities.” Forge has developed a novel platform technology for developing inhibitors of metalloenzymes and is currently focused on LpxC, a zinc metalloenzyme that is responsible for the outer membrane of Gram-negative bacteria. Proof-of-principle has been established through antimicrobial activity against highly resistant superbugs as well as animal models of infection.
“Forge embarked on the difficult, but essential, challenge of developing a novel antibiotic for serious infections where no or limited options exist to treat patients. Using a combination of metalloenzyme and medicinal chemistry, they have successfully discovered a promising lead compound with potency and drug-like properties ready to advance to the next stage of drug development,” said Dr. Michael Barbachyn, Ph.D., Professor, Brummel Chair in Organic Chemistry, Calvin College, former Director Infection Discovery Astra Zeneca, former Director Antibacterial Chemistry Pfizer, and inventor of the antibiotic linezolid (ZYVOX).
LpxC is highly conserved across Gram-negative bacteria and not found in Gram-positive bacteria or human cells. 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. Forge, using its innovative chemistry platform, has developed novel inhibitors of LpxC that are safe and effective in an animal model of Gram-negative infection and are able to kill Gram-negative superbugs where other antibiotics are ineffective.
“Our goal is to develop an antibiotic using novel chemistry and a unique mechanism of action that is able to fill the gaps in spectrum for Gram-negative infections, including superbugs that are resistant to all known antibiotics”, said Zachary A. Zimmerman, Ph.D., CEO of Forge Therapeutics. “Our novel chemistry approach for targeting metalloenzymes has resulted in the first non-hydroxamate inhibitor of LpxC that is effective in vitro and in vivo models of infection.”
Forge Therapeutics poster presentation at ASM Microbe 2016:
Poster #LB-056: “Non-hydroxamic Acid LpxC Inhibitors: In Vitro and In Vivo Antimicrobial Activities.”
Authors: Min Teng, Ph.D., Konstantin Taganov, Ph.D, Baskar Nammalwar, Ph.D., and David Puerta, Ph.D.
Date: Saturday, June 18, 2016
Time: 12:45pm – 2:45pm
Location: Boston Convention and Exhibition Center, Boston, MA
About Forge Therapeutics, Inc.
Forge Therapeutics, Inc. (“Forge”) is a biotechnology start-up that leverages its novel chemistry platform to develop small molecule inhibitors to target metalloproteins. Metalloproteins are proteins that require metal ions for their biological function and make up over 1/3 of the proteins in the human body. Forge uses a proprietary approach comprised of molecular modeling for rational drug design along with fundamental knowledge and expertise in bioinorganic chemistry to target metalloproteins. The name Forge Therapeutics comes from two definitions for forge: to manipulate (inhibit) a metal object (metalloprotein) and to move forward steadily with a purpose (the Forge team). Forge Therapeutics, Inc., maintains its headquarters in San Diego, California. To learn more please visit www.ForgeTherapeutics.com.