Affinium presents data from lead program, potential new class of antibacterial agents
Dr. Henry W. Pauls, Executive Director, Medicinal Chemistry, describes structure guided design, synthesis and characterization of novel inhibitors
Toronto, Ontario, September 1, 2005 — Affinium Pharmaceuticals, a structure guided pharmaceutical company focused on the discovery, development and commercialization of novel anti-infective medicines, said Dr. Pauls will present studies of potent antibacterial agents at the 230th American Chemical Society National Meeting in Washington, D.C. on September 1, 2005. These inhibitors of bacterial fatty acid biosynthesis are amongst the most potent known agents for treating Staphylococcal infections, including MRSA, and represent a novel class of antibiotics that operate via a biochemical pathway not previously targeted.
The presentation highlights the integrated drug discovery methods developed at Affinium to maximize medicinal chemistry outputs via integration of input from molecular modeling, structural biology, microbiology, biochemistry, and preclinical analysis. Computational chemistry was instrumental in guiding medicinal chemistry in optimizing the drug like properties of these inhibitors. Affinium’s design hypotheses were validated by high resolution X-ray structures of representative inhibitors in complex with S. aureus enoyl-ACP reductase. The inhibitors display submicromolar enzyme inhibitory activity, potent MICs and oral activity in animal models of staphylococcal infection.
Dr. Judd Berman, Affinium's Senior Vice President for Research & Development, said, "Dr. Pauls’ presentation illustrates the strength and versatility of Affinium’s scientists and our structure guided drug discovery capabilities. Such encouraging data support the utility of structure guided techniques for the discovery of novel antibiotics.”
About Affinium Pharmaceuticals
Affinium Pharmaceuticals is a specialty pharmaceutical company focused on the discovery, development and commercialization of novel anti-infective medicines. AFN-1252 utilizes a unique mechanism of action by directly inhibiting the function of the bacterial fatty acid synthesis (FAS) II pathway. Affinium's FASII antibacterial programs constitute a new antibiotic franchise with the potential for multiple products targeting the FASII pathway. These programs include a broad base of long-term intellectual property: issued and pending composition of matter patents on potent orally available small molecule inhibitors of a new class of antibiotics with a unique mechanism of action, targeting an underexploited pathway.
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