Table 6.

Protective effects of OPC-20011 and reference compounds against experimental systemic infection models in mice

Organism (% of mucin used)CompoundMIC (μg/ml)Challenge dose (cells/ mouse)ED50 (mg/kg)Confidence limit (mg/kg)
S. aureusSmith OPC-200110.21.32 × 107 0.220.11–0.37
 (5)CTM0.390.610.006–1.56
CAZ12.512.126.54–19.66
FMOX0.390.530.17–0.87
CPR0.391.721.29–2.40
VCM0.783.742.58–5.12
MRSA 5120 OPC-200116.257.6 × 107 1.000.60–1.57
 (5)CTM100>100
CAZ100>100
FMOX258.524.41–17.3
CPR5027.712.92–105
VCM0.7811.57.12–17.2
MRSA 5143OPC-200116.251.31 × 107 6.634.48–10.8
 (5)CTM>100>200
CAZ>100>200
FMOX5074.537.9–230
CPR100>200
VCM0.784.663.30–6.36
E. faecalis C0063 (2.5)OPC-200110.787.0 × 107 5.233.88–7.31
CTM100>200
CAZ>100>200
FMOX100>200
CPR12.5>100
ABPC1.565.23.86–7.00
S. pneumoniae Type IIIOPC-20011<0.00154.2 × 102 5.543.56–11.9
CTM0.12717.94–56.3
 (none)CAZ0.2172122–341
FMOX0.211.25.26–41.4
CPR0.01326.7219.5–42.1
ABPC0.02513.28.36–25.3
S. pneumoniae C0096OPC-200110.0062.0 × 104 0.560.31–0.90
CTM6.2529.517.4–49.5
 (none)CAZ3.1318.111.8–33.5
FMOX6.2518.610.1–63.7
CPR0.21.681.08–2.55
ABPC3.138.235.47–12.8
E. coli 29 (2.5)OPC-200110.391.35 × 106 0.150.12–0.19
CTM0.101.100.78–1.53
CAZ0.390.170.12–0.22
FMOX0.100.430.31–0.57
CPR0.0250.640.46–0.86
E. coliT0020OPC-200110.0136.8 × 105 0.060.039–0.090
 (2.5)CTM0.050.0520.036–0.072
CAZ0.050.210.126–0.298
FMOX0.0250.590.435–0.775
CPR0.0130.650.486–0.871
K. pneumoniae T0011 (2.5)OPC-200110.25.3 × 102 8.425.93–12.4
CTM0.110.78.14–14.3
CAZ0.050.870.24–1.45
FMOX0.112.79.80–16.4
CPR0.0130.670.45–0.91
S. marcescens T0004 (2.5)OPC-200110.781.6 × 106 1.410.622–2.30
CTM3.1326.78.34–56.2
CAZ0.20.140.065–0.300
FMOX0.782.341.20–3.79
CPR0.10.110.0063–0.209
P. mirabilis T0003 (2.5)OPC-200110.22.5 × 106 3.381.51–6.59
CTM0.3910.65.73–26.6
CAZ0.051.428.92–59.3
FMOX0.3922.60.686–2.53
P. aeruginosa T0017 (2.5)OPC-200116.254.8 × 104 13095.7–171
CTM>100>200
CAZ0.7811.35.44–22.9
FMOX>100>200
AZT3.1378.650.3–133