Pharmacokinetics and Toxicology of the Neuroprotective e,e,e -Methanofullerene(60)-63-tris Malonic Acid  [C 3 ] in Mice and Primates

ConclusionsThe plasma half-life ofC3 was 8.2 ± 0.2 h, and there was wide tissue distribution, including uptake into brain. The compound was cleared by both hepatic and renal excretion. C3 was quite stable, with minimal metabolism of the compound even after 7  days of treatment. The LD50 in mice was 80  mg/kg for a single intraperitoneal injection, and was>  30 mg/kg/day for sustained administration; therapeutic doses are 1–5 mg/kg/day. For primates, no evidence of renal, hepatic, electrolyte, or hematologic abnormalities were noted, and serial ECGs demonstrated no alteration in cardiac electrical activity. Thus, doses ofC3 that have therapeutic efficacy appear to be well tolerated after 2  years (mice) or 2 months (non-human primates) of treatment.
Source: European Journal of Drug Metabolism and Pharmacokinetics - Category: Drugs & Pharmacology Source Type: research