Evaluation of the in-vivo activity of Sch 29482

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Abstract
Sch 29482 (SCH), a new penem antibiotic, showed high peak, and prolonged (longer than 6 h) serum levels in mice, dogs and monkeys following administration by various routes. Both the rate of elimination from serum and the nature of the dose response curves were influenced by the route of administration as well as by the dose. These facts, together with the relatively long terminal half-lives, ranging from 0.9 to 2.5 h, suggested that the pharmacokinetic behaviour of SCH was influenced by its high serum protein binding. In a series of experimental mouse infections employing 51 different strains, SCH was found to have activity against both Gram-positive and Gram-negative bacteria. SCH had equal activity against both β -lactam susceptible and resistant strains indicating good in-vivo activity against β -lactamase producing strains. Many of these strains were resistant to the five reference cephalosporins tested. PD 50 values of SCH following oral administration were about threefold higher than after subcutaneous administration, consistent with its degree of oral absorption in mice. The results in laboratory animals indicate that SCH merits clinical evaluation.

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