Product Pipeline

Calixa's first compound (CXA-101) had been advanced into clinical study. Additional promising drug candidates are the combination CXA-101 with a β-lactamase inhibitor (CXA-201) for parenteral use and CXA-301, an inhaled formulation of CXA-101 for use in cystic fibrosis patients. CXA-201 is slated to start Phase 1 study in 2009.

CXA-101

CXA-101 (FR264205) is a novel parenteral cephalosporin with excellent in vitro activity against Pseudomonas aeruginosa. Cephalosporin antibiotics are highly trusted and widely used because of their potent bactericidal activity, broad antibacterial spectrum, and well-established safety profile. CXA-101 is highly active in vitro against common gram-negative and some gram-positive organisms, including pathogens causing respiratory and various other community-acquired and nosocomial infections. In general, the anti-gram-positive and -negative profile of CXA-101 is similar to that of ceftazidime, but its antipseudomonal activity is the most potent among all currently available β-lactam antimicrobial agents, including the cephalosporins and carbapenems. Most importantly, CXA-101 is active against the majority of P. aeruginosa isolates that are resistant to carbapenems, cephalosporins, fluoroquinolones and aminoglycosides. CXA-101 is a bactericidal agent that exhibits time-dependent killing activity against various gram-negative organisms, including P. aeruginosa. CXA-101 has proven to be highly effective in various models of animal infection caused by both gram-positive and gram-negative bacteria, including multi-drug-resistant strains of P. aeruginosa.

Extensive nonclinical safety studies demonstrate that CXA-101 has an excellent safety profile in animals and that the pharmacokinetic profile is similar to other widely used cephalosporins.

In summary, CXA-101 is a novel cephalosporin antibiotic with broad-spectrum antibacterial activity that includes multi-drug-resistant P. aeruginosa. Both in vitro and in vivo efficacy and safety data fully support its clinical development as a potential human therapeutic agent for the treatment of severe bacterial infections caused by P. aeruginosa and other susceptible organisms.