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Pharmacology

Human Pharmacokinetics and Safety Profile of Finafloxacin, a New Fluoroquinolone Antibiotic, in Healthy Volunteers

Heena Patel, Arne Andresen, Andreas Vente, Hans-Dietrich Heilmann, Will Stubbings, Michael Seiberling, Luis Lopez-Lazaro, Rolf Pokorny, Harald Labischinski
Heena Patel
1MerLion Pharmaceuticals GmbH, Robert-Rössle Strasse 10, Berlin, Germany
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Arne Andresen
1MerLion Pharmaceuticals GmbH, Robert-Rössle Strasse 10, Berlin, Germany
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Andreas Vente
1MerLion Pharmaceuticals GmbH, Robert-Rössle Strasse 10, Berlin, Germany
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Hans-Dietrich Heilmann
1MerLion Pharmaceuticals GmbH, Robert-Rössle Strasse 10, Berlin, Germany
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  • For correspondence: heilmann@merlionpharma.de
Will Stubbings
1MerLion Pharmaceuticals GmbH, Robert-Rössle Strasse 10, Berlin, Germany
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Michael Seiberling
2Covance Clinical Research Unit AG, Lettenweg 118, Allschwil (Basel), Switzerland
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Luis Lopez-Lazaro
2Covance Clinical Research Unit AG, Lettenweg 118, Allschwil (Basel), Switzerland
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Rolf Pokorny
2Covance Clinical Research Unit AG, Lettenweg 118, Allschwil (Basel), Switzerland
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Harald Labischinski
1MerLion Pharmaceuticals GmbH, Robert-Rössle Strasse 10, Berlin, Germany
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DOI: 10.1128/AAC.00832-10
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  • Fig. 1.
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    Fig. 1.

    Dose proportionality of Cmax after single-dose administration of finafloxacin.

  • Fig. 2.
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    Fig. 2.

    Dose proportionality of AUC∞ after single-dose administration of finafloxacin.

  • Fig. 3.
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    Fig. 3.

    Arithmetic mean plus standard deviation of plasma finafloxacin concentration-versus-time profile on a logarithmic concentration scale in part A subjects.

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    Fig. 4.

    Arithmetic mean plus standard deviation of serum finafloxacin concentration-versus-time profile on a logarithmic concentration scale in part B subjects.

Tables

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  • Table 1.

    Demographic data

    Subject group, dose regimen, and dose (mg)Total no. of subjectsNo. of male subjectsNo. of female subjectsMean body weight (kg)Mean BMI (kg/m2)Mean age (yr)
    Part A, single dose
        2532176.423.841.7
        5066072.723.539.3
        10065176.424.238.3
        20065174.124.436.7
        40065176.325.137.8
        80065173.323.737.0
        Placebo, single dose107372.123.944.4
    Part B, 7 days q.d.
        15065170.023.544.0
        30065178.424.446.8
        60066079.124.343.7
        80066081.224.844.8
        Placebo, multiple dose87179.625.742.3
    Part C, 7 days q.d.
        60020202075.724.341.6
  • Table 2.

    Plasma pharmacokinetics of finafloxacin in healthy volunteers after single-dose administration (part A)a

    Dose (mg)No. of subjectsCmax (mg/liter)Cmax,norm [(mg/liter)/mg]AUC∞ (h · mg/liter)AUC∞,norm [(h · mg/liter)/mg]tmax (h)t1/2 (h)CL/F (liters/h)Vz/F (liters)
    2530.240.00960.420.0171.001.2859.0109
    5060.44 ± 0.160.00881.26 ± 0.480.0250.883.8 ± 2.745.0 ± 17.1220 ± 127
    10061.32 ± 0.620.0132.80 ± 0.720.0280.507.2 ± 3.237.2 ± 7.5389 ± 202
    20061.90 ± 0.730.00954.08 ± 1.050.0200.754.6 ± 1.951.5 ± 11.7348 ± 194
    40065.06 ± 2.090.01314.2 ± 4.440.0361.0010.0 ± 4.430.8 ± 10.4487 ± 363
    800611.1 ± 2.960.01429.2 ± 7.500.0360.8810.5 ± 2.229.0 ± 7.7435 ± 130
    • ↵a Where indicated, values are means ± standard deviations. Cmax, peak plasma concentration; AUC, area under the concentration-time curve; tmax, time to reach Cmax (for this parameter median values are reported); t1/2 terminal half life; CL/F, total body clearance; Vz/F, distribution volume based on the terminal phase; norm, values normalized by the administered dose per kg of body weight; AUC∞, AUC extrapolated to infinite time.

  • Table 3.

    Plasma pharmacokinetics of finafloxacin in six healthy volunteers per dose after multiple-dose administration (part B)a

    Dose (mg)Day no.Cmax (mg/liter)Cmax,norm [(mg/liter)/mg]AUC24h (h · mg/liter)AUC24h,norm [(h · mg/liter)/mg]tmax (h)t1/2 (h)CL/F (liters/h)Vz/F (liters)
    15011.69 ± 0.380.0113.76 ± 0.820.0250.50
    15071.50 ± 0.520.0104.01 ± 0.640.0270.505.3 ± 0.637.4 ± 5.8282 ± 25
    30012.96 ± 0.880.00998.75 ± 3.500.0291.50
    30074.15 ± 2.110.0149.09 ± 3.830.0300.636.5 ± 2.537.4 ± 17.5337 ± 155
    60017.67 ± 3.420.01318.7 ± 7.630.0310.75
    60076.76 ± 2.200.01119.2 ± 6.400.0320.888.8 ± 3.132.5 ± 10.2409 ± 175
    80018.68 ± 1.960.01120.8 ± 7.420.0260.75
    80078.95 ± 3.110.01126.1 ± 8.600.0330.8814.0 ± 5.531.6 ± 10.6659 ± 467
    • ↵a Where indicated, values are means ± standard deviations. AUC24h, area under the plasma concentration-time curve to 24 h after dosing. For the explanation of other symbols, see the footnote to Table 2.

  • Table 4.

    Finafloxacin concentrations in urine (part A)

    Collection period (h)Median finafloxacin concn (mg/liter [range]) at a dose of:
    100 mg200 mg400 mg800 mg
    0–236.4 (16.5–101)52.2 (30.6–159)85.5 (50.8–134.0)89.8 (38.0–242.0)
    2–443.8 (19.3–61.9)48.4 (34.9–166)83.2 (44.7–328)112.5 (62.6–193.0)
    4–814.2 (6.3–36.5)22.4 (11.9–91.7)80.4 (29.4–207)137.6 (43.9–257.0)
    8–124.9 (1.1–6.9)10.5 (2.0–31.5)26.6 (9.3–63.9)22.2 (12.1–87.1)
    12–242.1 (0.7–4.8)2.3 (0.9–13.0)8.6 (5.0–11.3)11.4 (7.5–54.0)
    24–480.8 (0.1–1.1)0.7 (0.5–1.6)2.1 (1.4–7.5)1.9 (0.7–73.8)
  • Table 5.

    Urine pharmacokinetic parameters of finafloxacin after single-dose administration (part A)

    Dose (mg)No. of subjectsRecovery in urine (% of dose [range])CLR (liters/h)a
    25327.8 (27.0–29.2)17.0 (10.5–19.2)
    50631.9 (25.8–38.1)14.2 (10.8–17.5)
    100635.5 (26.8–44.1)13.3 (10.1–16.5)
    200632.1 (19.3–44.9)15.8 (12.8–18.8)
    400628.5 (20.0–37.0)8.6 (4.9–12.2)
    800633.5 (26.1–40.8)9.6 (7.5–11.6)
    • ↵a Median (minimum-maximum) values are reported for the 25-mg dose; mean values (95% confidence limits) are reported for the other dose levels. CLR, renal clearance.

  • Table 6.

    AEs observed in the study parts

    Subject group and dose (mg)No. of subjectsNo. (%) of subjects with AETotal no. of AEsNo. of AEs per subjectNo. of AEs by typea
    GINSRTIOther
    Part A, single dose
        2531 (33)30.331101
        5060 (0)000000
        10062 (33)30.50102
        20065 (83)71.171402
        40061 (33)20.331100
        80065 (83)111.832108
        Placebo, single dose103 (33)50.50302
    Part B, 7 days q.d.
        15064 (67)132.171318
        30060 (0)000000
        60063 (50)50.833101
        80065 (83)101.671117
        Placebo, multiple dose85 (63)121.51326
    Part C
        Fasting subjects1411 (79)161.148215
        Fed subjects64 (67)101.675203
        Total group, 7 days q.d., 600 mg2015 (75)261.3013418
            Nonflatulence AE subjects11 (55)201.07418
    • ↵a GI, gastrointestinal; NS, nervous system; RTI, respiratory tract infections; Other, cardiovascular, musculoskeletal, eye, skin, local reaction at puncture site, and/or general.

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Human Pharmacokinetics and Safety Profile of Finafloxacin, a New Fluoroquinolone Antibiotic, in Healthy Volunteers
Heena Patel, Arne Andresen, Andreas Vente, Hans-Dietrich Heilmann, Will Stubbings, Michael Seiberling, Luis Lopez-Lazaro, Rolf Pokorny, Harald Labischinski
Antimicrobial Agents and Chemotherapy Aug 2011, 55 (9) 4386-4393; DOI: 10.1128/AAC.00832-10

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Human Pharmacokinetics and Safety Profile of Finafloxacin, a New Fluoroquinolone Antibiotic, in Healthy Volunteers
Heena Patel, Arne Andresen, Andreas Vente, Hans-Dietrich Heilmann, Will Stubbings, Michael Seiberling, Luis Lopez-Lazaro, Rolf Pokorny, Harald Labischinski
Antimicrobial Agents and Chemotherapy Aug 2011, 55 (9) 4386-4393; DOI: 10.1128/AAC.00832-10
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