新経口用Cephem T-2588: その抗菌力, β-lactamaseに対する安定性, 作用点PBPへの結合親和性, および血清補体とマクロファージとの協力的殺菌作用

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タイトル別名
  • A NEW ORAL PRODRUG OF 3 RD GENERATION CEPHEM, T-2588: ITS ANTIBACTERIAL ACTIVITY, AFFINITY TO β-LACTAMASES AND PBPS, AND SYNERGY WITH THE COMPLEMENT AND MACROPHAGES

説明

T-2588 is a novel oral prodrug of T-2525 that is a cephem antibiotic with broad spectrum. T-2588 is converted into an active form, T-2525, after being absorbed from the intestine.<BR>The antibacterial activity of T-2525 was compared with that of other oral β-lactam antibiotics, i. e. ampicillin, cephalexin, and cefaclor.<BR>MIC80μg/mps of T-2525 to 22 to 59 clinical isolates of S. aureus, S. epidermidis, β-streptococci, E. coli (R+), K. pneumoniae, P. mirabilis, P.vulgaris, M. morganii, P. rettgeri, C. freundii, E. cloacae, S. marcescens, A. calcoaceticus, H. influenzae, and B. fragilis were 6.25, 50, 0.025, 0.39, 0.39, 0.1, 0.78, 1.56, 6.25, 3. 13, 50, 6, 25, 50, 0.05, and 6.25μg/ml, respectively.<BR>T-2525 is stable against PCase type β-lactamases. Although the antibiotic is also stable to the type la β-lactamase, it is hydrolyzed by the type Ic β-lactamase in some extent.<BR>T-2525 binds to PBPs of S. aureus at the same level as cefaclor. This antibiotic, however, manifests much stronger binding affinity to PBPs of E. coli, S. marcescens and A. calcoaceticus than cefaclor.<BR>Addition of the complement and serum results in enhancement of bactericidal effect of T-2525. Filamentous cells of E. coli induced by sub MICs of T-2525 are phagocytized well and easily digested by mouse cultured macrophages.<BR>T-2525 would be a useful antibiotic if its safety and pharmacokinetic are satisfactory.

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