Grepafloxacin  (Synonyms: OPC-17116; dl-Grepafloxacin)

Grepafloxacin (OPC-17116) is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin has high tissue penetration and a promising pharmacodynamic profile^[1][2][3].

Grepafloxacin (OPC-17116; 0-1 mg/L; 14-21 d) has antibiotic activity with a MIC value of ≤ 0.006 mg/L for E. coli strain^[1].
Grepafloxacin (0-1 mg/L; 3 h) has antimicrobial activity against mycobacteria in macrophages with a MIC value of 0.5 mg/L for M. avium^[1].
Grepafloxacin 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Grepafloxacin (OPC-17116; 200 mg/kg; p.o.; Balb/c mice) 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) has modest activities in both intranasal (IN) infection and intravenous (IV) Mycobacterium avium infection models^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

359.39

C₁₉H₂₂FN₃O₃

119914-60-2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Vacher S, et, al. Comparative antimycobacterial activities of ofloxacin, ciprofloxacin and grepafloxacin. J Antimicrob Chemother. 1999 Nov;44(5):647-52.  [Content Brief]

  [2]. Owen K. Comparative grepafloxacin phototoxicity in mouse skin. J Antimicrob Chemother. 1998 Aug;42(2):261-4.  [Content Brief]

  [3]. Cynamon MH, et, al. The activity of grepafloxacin in two murine models of Mycobacterium avium infection. J Infect Chemother. 2004 Jun;10(3):185-8.  [Content Brief]

  [4]. Miyamoto H, et al. Synthesis and biological properties of substituted 1,4-dihydro-5-methyl-4-oxo-3-quinolinecarboxylic acids. Bioorg Med Chem. 1995;3(12):1699-1706.  [Content Brief]