The pharmacokinetics of an antimicrobial drug in human plasma and in vitro susceptibility testing of an antimicrobial drug do not necessarily predict its efficacy in vivo. Therefore, the combined activity of an antimicrobial drug and blood-derived polymorphonuclear leukocytes (PMN) against Staphylococcus aureus were investigated in vitro. In addition, a pharmacological model allowing analysis of the bactericidal activity of a drug-containing exudate against S. aureus ex vivo was developed. For this purpose, a phagocytic-bactericidal assay was miniaturized to a volume of 100 microliters in order to test the bactericidal activities of an antimicrobial drug with blood PMN in vitro and with skin blister fluid (CBF) ex vivo. Ro 40-6890, the active metabolite of the ester prodrug Ro 41-3399, was used as the test drug. Killing of S. aureus was clearly enhanced when Ro 41-6890 was combined in vitro with a suboptimal number of blood-derived PMN. In eight healthy volunteers, skin blisters were provoked by plasters containing cantharidin. Following a single oral dose of Ro 41-3399, CBF containing PMN was sampled at regular intervals and incubated ex vivo with S. aureus (5 x 10(5) CFU/ml) for 2, 4, 6, and 24 h at 37 degrees C. Concentrations of Ro 40-6890 were measured in CBF (CCBF) and plasma. Ro 40-6890 distributed well from plasma into CBF. When CCBF was below the MIC, an enhanced effect of Ro 40-6890 and host defense factors present in CBF against S. aureus was observed. In conclusion, the present model can provide additional information on human plasma drug concentrations and MICs established in vitro.

01 Apr 1993·Antimicrobial Agents and ChemotherapyQ2 · MEDICINE

Antimicrobial activity and disk diffusion susceptibility testing of Ro 40-6890, the active metabolite of the new cephalosporin ester, Ro 41-3399

Q2 · MEDICINE

Article

Author: Pfaller, M A ; Fuchs, P C ; Barry, A L

Ro 40-6890, the active metabolite of Ro 41-3399, was tested against 391 gram-negative and gram-positive clinical isolates. Ro 40-6890 was active against members of the family Enterobacteriaceae, Moraxella catarrhalis, pneumococci, other Streptococcus spp., and methicillin-susceptible staphylococci. Preliminary disk diffusion interpretive zone criteria were calculated for 5-, 10-, and 30-micrograms Ro 40-6890 disks and several possible MIC susceptibility breakpoints. We recommend the use of the 5-micrograms disk and suggest that the following zone diameters be used as breakpoints in clinical trials: susceptible, > or = 21 mm (MIC, < or = 1 microgram/ml); intermediate, 18 to 20 mm (MIC, 2 micrograms/ml); and resistant, < or = 17 mm (MIC, > or = 4 micrograms/ml).

01 Dec 1992·Antimicrobial Agents and ChemotherapyQ2 · MEDICINE

In vitro activities of Ro 40-6890 against 164 predominantly intestinal members of the families Enterobacteriaceae and Vibrionaceae

Q2 · MEDICINE

Article

Author: Zollinger-Iten, J ; Hohl, P ; von Graevenitz, A

The in vitro activities of Ro 40-6890, the active metabolite of a novel orally absorbable cephalosporin ester, Ro 41-3399, against 164 nonfastidious aerobic gram-negative rods of predominantly intestinal origin from patients with diarrhea were evaluated by the agar dilution method recommended by the National Committee for Clinical Laboratory Standards. Ro 40-6890 was inhibitory (MIC for 90% of isolates [MIC90], 0.12 micrograms/ml) against the majority of intestinal members of the families Enterobacteriaceae and Vibrionaceae (Vibrio spp., Aeromonas spp., and Plesiomonas shigelloides). The potency of Ro 40-6890 was very similar to that of cefotaxime (MIC90, 0.12 micrograms/ml) and distinctly higher than those of cefadroxil (MIC90, > or = 128 micrograms/ml) and amoxicillin-clavulanic acid (MIC90, 32 micrograms/ml-2 micrograms/ml).

100 Deals associated with Ceftrazonal bopentil

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Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	Phase 1	-	F. Hoffmann-La Roche Ltd.	-
Bacterial Infections	Phase 1	DE	-	-
Bacterial Infections	Phase 1	US	-	-
Bacterial Infections	Phase 1	CH	Roche Holding AG	-

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