AFN–1252 Anti-Staphylococcal Program
AFN-1252 was selected from the Affinium staphylococcal FabI program as the lead clinical candidate, and it is currently in oral Phase 1 trials. AFN-1252 has completed two single ascending dose oral Phase 1 trials that showed excellent tolerability and attainment of target pharmacokinetic levels. Additional single and multiple ascending dose Phase 1 trials with an improved oral formulation are ongoing in 2010. Development of an intravenous formulation is continuing.
AFN-1252 is a highly potent, specific-spectrum agent that is active mainly against staphylococci, with little to no activity against other common bacterial species and gut flora. AFN-1252 shows a consistent MIC90 of 0.016 μg/ml against >3000 strains of S. aureus including MSSA, MRSA, CA-MRSA, HA-MRSA, VISA, VRSA, and all other drug resistant mechanisms tested. AFN-1252 has a very low propensity for resistance development, in both single step and multiple passage selection experiments. AFN-1252 has shown excellent oral efficacy in multiple mouse models of infection including thigh abscess, skin abscess, pneumonia and peritonitis / septicemia models.
By specifically targeting staphylococci, and not disrupting the human microbiome, AFN-1252 has a potentially significant safety advantage, and its use is expected to result in much reduced selection pressure for overgrowth of antibiotic resistant organisms, including C. difficile and VRE, and in much reduced antibiotic associated adverse events such as diarrhea, colitis, and candidiasis.
Affinium is interested in worldwide, out-licensing of AFN-1252. For further information please contact Leisa Dennehy at ldennehy@afnm.com
 AFN-1252 co-crystallized in the S. aureus FabI enzyme |
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