Ceftaroline fosamil

Ceftaroline is a next generation cephalosporin antibiotic with broad-spectrum activity that includes contemporary resistant phenotypes such as methicillin-resistant Staphylococcus aureus (MRSA) as well as other clinically important gram-positive and gram-negative bacteria. Ceftaroline is being developed as a prodrug, ceftaroline fosamil, which is rapidly hydrolyzed in the bloodstream to active ceftaroline following intravenous administration.

Ceftaroline is currently in Phase III clinical development for complicated skin and skin structure infections (cSSSI) and community-acquired pneumonia (CAP).

NXL104

NXL104 is a non-β-lactam β-lactamase inhibitor that was in-licensed for use in combination with ceftaroline in the United States. NXL104 does not have any intrinsic antibacterial activity in its own right, but is capable of inhibiting β-lactamase enzymes that belong to molecular classes A and C. β-lactamases are enzymes that are produced by bacteria and are responsible for conferring resistance to β-lactam antibiotics by breaking open the β-lactam ring and destroying the molecule’s antibacterial properties. NXL104 is being evaluated in combination with ceftaroline. Although ceftaroline is active against many gram-negative bacteria, it is inactive against strains that produce extended-spectrum β-lactamases (ESBLs).

The ceftaroline/NXL104 combination product is currently in pre-clinical development with an IND filing anticipated in 2009.