In vitro and in vivo anti-Helicobacter pylori activity of Y-904, a new fluoroquinolone

Iwao, Eiji; Yokoyama, Yoshito; Yamamoto, Kenji; Hirayama, Fumihiro; Haga, Keiichiro

doi:10.1007/s10156-003-0240-z

Cited by 9 publications

(8 citation statements)

References 24 publications

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“…The new generation fluoroquinolones may arguably offer the best alternative. In vitro studies show excellent susceptibility of H. pylori to newer quinolones [9,36] and although the prevalence of primary resistance of H. pylori to some of these newer quinolones is unclear, limited studies suggest a low rate of 8% for ciprofloxacin [37] and 4.7% to trovafloxacin [38]. Our in vitro susceptibility studies did not show any resistance to gatifloxacin in 50 H. pylori isolates.…”

Section: Discussionmentioning

confidence: 53%

Efficacy of Two Rabeprazole/Gatifloxacin‐Based Triple Therapies for Helicobacter pylori Infection

Sharara¹,

Chaar

Racoubian

et al. 2004

Helicobacter

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Section: Discussionmentioning

confidence: 53%

Efficacy of Two Rabeprazole/Gatifloxacin‐Based Triple Therapies for Helicobacter pylori Infection

Sharara¹,

Chaar

Racoubian

et al. 2004

Helicobacter

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“…In the present study, the in vitro resistance development of H. pylori for levofloxacin and sitafloxacin was examined, using a serial passage assay (14). In terms of low-resistance mutants (with a Ն8-fold MIC increase), resistance development fre- quency was significantly lower for sitafloxacin than for levofloxacin.…”

Section: Discussionmentioning

confidence: 90%

“…At 7 weeks after infection, the drugs, dissolved in 0.5% (wt/vol) hydroxypropyl methylcellulose aqueous solution (Shin-Etsu Chemical Co., Ltd., Tokyo, Japan), were orally given twice a day for a week to each group (six animals/group). Doses (3, 10, and 30 mg/kg [body weight] for levofloxacin and 0.1, 0.3, and 1, 3 mg/kg [body weight] for sitafloxacin) were chosen based on clinical doses (approximately 6 to 10 mg/kg [body weight]/ day), previous animal data (14), and the MIC data obtained in the present study. At 2 weeks after drug administration, H. pylori in the stomach was examined by culture methods.…”

Section: Methodsmentioning

confidence: 99%

“…H. pylori ATCC 43504 and seven clinical isolates (three clarithromycin-resistant strains [C1, C2, and C3] and four metronidasole-resistant strains [M1, M2, M3, and M4]) were subjected to a serial passage assay (14), using brucella broth supplemented with 10% horse serum and 96-well microplates. Serial doubling dilutions of sitafloxacin and levofloxacin were inoculated with H. pylori (10 6 CFU/ml), followed by incubation for 72 h at 37°C in a microaerophilic atmosphere.…”

Section: Methodsmentioning

confidence: 99%

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Helicobacter pylori Eradication by Sitafloxacin-Lansoprazole Combination and Sitafloxacin Pharmacokinetics in Mongolian Gerbils and ItsIn VitroActivity and Resistance Development

Yamamoto

Takano

Higuchi

et al. 2011

Antimicrob Agents Chemother

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A total of 293 strains of Helicobacter pylori, including strains resistant to levofloxacin, clarithromycin, metronidazole, or amoxicillin, were examined for in vitro susceptibility to 10 antimicrobial agents. Among these agents, sitafloxacin (a fluoroquinolone) showed the greatest activity (MIC 90 , 0.06 g/ml), with high bactericidal activity and synergy in sitafloxacin-lansoprazole (a proton pump inhibitor) combination. In a Mongolian gerbil model with a H. pylori ATCC 43504 challenge, marked eradication effects were observed at >1 mg/kg for sitafloxacin, >10 mg/kg for levofloxacin, and >10 mg/kg for lansoprazole, reflecting MIC levels for each agent (0.008, 0.25, and 2 g/ml, respectively). The therapeutic rates were 83.3% for the sitafloxacin (0.3 mg/kg)-lansoprazole (2.5 mg/kg) combination and 0% for either sitafloxacin or lansoprazole alone. The maximum serum concentration (C max ) of sitafloxacin was 0.080 ؎ 0.054 g/ml at 30 min, when orally administered at 1 mg/kg. The simultaneous administration of lansoprazole resulted in no difference. In the resistance development assay, MICs of levofloxacin increased 64-to 256-fold with gyrA mutations (Ala88Pro and Asn87Lys), while MICs of sitafloxacin only up to 16-fold with the Asn87Lys mutation. The data suggest that sitafloxacin exhibited superior anti-H. pylori activity with low rates of resistance development in vitro and that, reflecting high in vitro activities, sitafloxacin-lansoprazole combination exhibited strong therapeutic effects in Mongolian gerbils with a C max of sitafloxacin that was 10-fold higher than the MIC value at a 1-mg/kg administration.Helicobacter pylori is a spiral-shaped bacterium with one or two turns along its axis and has multiple polar flagella. Such strongly motile H. pylori colonizes the gastric mucosa of more than 50% of individuals worldwide. Children are a high-risk group for H. pylori infections, which may persist for years or be lifelong. H. pylori is closely associated with various diseases (2, 5, 13, 30), such as gastritis and peptic ulcers, mucosa-associated lymphoid tissue lymphoma, and idiopathic thrombocytopenic purpura or chronic urticaria, and is also a bacterial risk factor for gastric cancer.For the eradication of H. pylori, a combination therapy using an anti-acid agent (proton pump inhibitor [PPI] or H 2 blocker) and two anti-H. pylori agents (amoxicillin and either clarithromycin or metronidazole) has been recommended (3,11,19). Fluoroquinolones have also been selected as anti-H. pylori agents (3,11,19).Drug resistance has increasingly been reported (11,12,27). Metronidazole has a high primary rate of resistance: 60 to 100% in developing countries and 10 to 50% in developed countries. For clarithromycin, the primary rate of resistance to H. pylori in adults is relatively low, ca. 10%, with a recent increase in many countries. In addition, failure to eradicate the infection with clarithromycin treatment results in extremely high rates of resistance (36 to 85%) (27). Resistance to amoxicillin and fluoroquinolone is ...

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“…[14][15][16][17] The Mongolian gerbil model is also useful as an evaluation model for drug therapeutic effect. 18 Using this Mongolian gerbil model, we screened novel benzimidazole compounds and discovered one with strong and selective antibacterial action against H. pylori: Y-754, 2-[(3-methyl-4-{2-[2-(2,2,2-trifluoroethoxy)ethoxy]ethylthio}-2-pyridyl)methylthio]-1H-benzimidazole dihydrochloride. The present study investigated in detail the in vitro and in vivo antibacterial activity of Y-754 and examined its usefulness as an anti-H. pylori drug.…”

Section: Introductionmentioning

confidence: 99%

Potent antibacterial activity of Y-754, a novel benzimidazole compound with selective action against Helicobacter pylori

Iwao

Yamamoto²,

Yokoyama³

et al. 2004

Journal of Infection and Chemotherapy

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In vitro and in vivo anti-Helicobacter pylori activity of Y-904, a new fluoroquinolone

Cited by 9 publications

References 24 publications

Efficacy of Two Rabeprazole/Gatifloxacin‐Based Triple Therapies for Helicobacter pylori Infection

Efficacy of Two Rabeprazole/Gatifloxacin‐Based Triple Therapies for Helicobacter pylori Infection

Helicobacter pylori Eradication by Sitafloxacin-Lansoprazole Combination and Sitafloxacin Pharmacokinetics in Mongolian Gerbils and ItsIn VitroActivity and Resistance Development

Potent antibacterial activity of Y-754, a novel benzimidazole compound with selective action against Helicobacter pylori

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