Ceftobiprole medocaril

Ceftobiprole medocaril (BAL5788) is the parenteral prodrug of Ceftobiprole (HY-112579). 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]. In Vivo: Ceftobiprole medocaril (BAL5788; 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 Pen^r Cro^s Ctx^s strain P-15986^[1].
Ceftobiprole medocaril (10, 40, 160 mg/kg; single dose; sc) has T_1/2s 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 C_max/dose values decreases from 1.08 to 0.90 in neutropenic thigh-infected mice^[2].