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SGX523 is a quinoline-containing molecule that was a promising c-MET kinase inhibitor with an IC50 of 4 nmol/L and >1000-fold selectivity over other protein kinases.It is orally bioavailable and can inhibit the growth of human glioblastoma lung and gastric cancer xenografts in mice.However, in a phase Ⅰ clinical trial, the six patients received ≥80 mg daily doses all developed renal failure as confirmed by a rise in serum creatinine and blood urea nitrogen.Hydration therapy returned these levels to baseline after 1 to 4 weeks.Follow-up studies revealed that the cause of renal toxicity was drug-induced nephropathy due to a metabolite of SGX523 that was not detected in preclinical studies.Aldehyde oxidase transforms the quinoline ring into a quinolinone.