Mecillinam (FL 1060), a 6β-Amidinopenicillanic Acid Derivative: In Vitro Evaluation

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Abstract
Mecillinam (formerly called FL 1060), a novel 6β-amidinopenicillanic acid derivative, showed markedly higher activity than ampicillin against clinical isolates of Enterobacteriaceae . The mode of action of mecillinam is different from that of ampicillin and consequently no intrinsic cross-resistance between the two antibiotics was observed. Mecillinam is inactivated by β-lactamases but is generally more stable than ampicillin; thus an apparent cross-resistance exists for strong β-lactamase producers. The protein binding was low and the activity was relatively independent of pH between 5.5 and 8.0. Slow-growing, insensitive variants of Escherichia coli could be selected but these were not stable. The frequency of insensitive variants was affected by the sodium chloride concentration in the medium.

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