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Summary: We report the first hepatic adverse effect of tosufloxacin tosylate in a muscle invasive bladder cancer patient with normal liver functions and with scheduling to undergo a surgical operation for a neobladder. Tosufloxacin tosylate 150 mg was administered to a 57-year-old man who maintained transurethral resection of bladder tumor (TUR-BT) postoperative multiple medications. His labs presented significant increases in alanine amino transferase (ALT) and aspartate amino transferase (AST) levels with 2-week compliance of 150 mg tablet three times a day. After discontinuing tosufloxacin tosylate, the levels slowly decreased and completely returned to normal ranges without any intervention in a few weeks. The Naranjo Causality Algorithm indicates a probable relationship between increased ALT and tosufloxacin. The patient was to have the second surgical operation as scheduled after getting normal range of ATL level. Therefore, tosufloxacin should be avoided in patients at risk for having liver dysfunctions or diseases if the patients have a schedule for any operation. Background: Tosufloxacin tosylate has been shown to have favorable benefits as an antibiotic. Tosufloxacin tosylate may be considered to have the adverse effects such as nauseas, vomiting, diarrhea, abdominal pain, stomatitis, tendonitis, tendon rupture, headache, dizziness, drowsiness, insomnia, weakness, agitation including hemolysis in the event of glucose-6-phosphate dehydrogenase deficiency as other fluoroquinolones. More severe adverse reactions of tosufloxacin tosylate over the above common adverse effects of fluoroquinolones were thrombocytopenia and nephritis. It also is not well known that tosufloxacin can cause hepatic problem. Here the study reports the first hepatic reaction from tosufloxacin and might arouse heath care providers' attention to appropriate drug choice for patients.