Ceftobiprole medocaril (BAL5788) sodium is the parenteral prodrug of Ceftobiprole . Ceftobiprole is a parenteral pyrrolidinone cephalosporin. Ceftobiprole is a broad-spectrum cephalosporin with high levels of in vitro activity against methicillin- (MRSA) and vancomycin-resistant staphylococci (VRSA) and penicillin-resistant streptococci. Ceftobiprole also inhibits gram-positive and gram-negative pathogens[1][2].
Ceftobiprole medocaril (s.c.; 3 × q12h; total daily doses of BAL9141 equivalents, 2.1, 4.2, or 8.4 mg/kg) causes ten-day cumulative survival rates ranged from 57 to 100% for female Swiss albino mice (body weight, 20 to 22 g) infected Penr Cros Ctxs strain P-15986[1].
Ceftobiprole medocaril (10, 40, 160 mg/kg; single dose; sc) has T1/2s from 20 min to 31 min, as the dose rose from 40 mg/kg to 160 mg/kg. The AUC/dose values for the escalating single doses ranges from 0.585 to 1.33, and the Cmax/dose values decreases from 1.08 to 0.90 in neutropenic thigh-infected mice[2].
[1]. E Azoulay-Dupuis, et al. Efficacy of BAL5788, a prodrug of cephalosporin BAL9141, in a mouse model of acute pneumococcal pneumonia. Antimicrob Agents Chemother. 2004 Apr;48(4):1105-11.
[2]. W A Craig, et al. In vivo pharmacodynamics of ceftobiprole against multiple bacterial pathogens in murine thigh and lung infection models. Antimicrob Agents Chemother. 2008 Oct;52(10):3492-6.