Grepafloxacin (hydrochloride)

Grepafloxacin (OPC-17116) hydrochloride is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin hydrochloride has high tissue penetration and a promising pharmacodynamic profile^[1][2][3][4]. In Vitro:Grepafloxacin (OPC-17116; 0-1 mg/L; 14-21 d) hydrochloride has antibiotic activity with a MIC value of ≤ 0.006 mg/L for E. coli strain^[1].
Grepafloxacin (0-1 mg/L; 3 h) hydrochloride has antimicrobial activity against mycobacteria in macrophages with a MIC value of 0.5 mg/L for M. avium^[1].
Grepafloxacin hydrochloride exhibits potent in vitro antibacterial activity against Gram-positive bacteria such as Streptococcus pneumoniae and high in vivo efficacy on the experimental systemic infections caused by the Gram-positive and -negative bacteria tested^[4].
In Vivo:Grepafloxacin (OPC-17116; 200 mg/kg; p.o.; Balb/c mice) hydrochloride displays good safety profile in terms of phototoxicity^[2].
Grepafloxacin (25-200 mg/kg; p.o.; 5 days/week for 4 weeks; female C57BL6/J-Lyst bg-J/ mice/beige mice) hydrochloride has modest activities in both intranasal (IN) infection and intravenous (IV) Mycobacterium avium infection models^[3].