A 2'guanidyl derivative of gentamicin (S86451) with reduced nephrotoxicity studies at low and medium dose levels in the rat.

Maldague P, Laurent G, Carlier MB, Tulkens P

The nephrotoxic potential of S86451 (2'guanidyl, 2'deamino gentamicin C1) has been investigated in Sprague-Dawley rats at 10 and 25 mg/kg, in comparison with gentamicin at 4 and 10 mg/kg. The criteria were (i) the severity of the lysosomal phospholipidosis, as assessed by both biochemical and morphological investigations; (ii) the degree of tubular regeneration, a consequence of the aminoglycoside-induced focal necrosis measured by 3H-thymidine incorporation into kidney cortex DNA. S86451 was found at least 2-5 times less toxic than gentamicin. Thus, this compound should be a safer antibiotic than gentamicin in combating organisms with a similar sensitivity to either drug.

PMID: 6596014, UI: 85096288