Antitumor activity of 2-mercaptoethanesulfonate (mesna) in vitro. Its potential use in the treatment of superficial bladder cancer.
2-Mercaptoethanesulfonate (mesna) is a nontoxic drug which upon intravenous and oral administration effectively prevents urothelial toxicity in cancer patients treated with oxazaphosphorines. Mesna is rapidly oxidized to dimesna in the blood. It is then taken up by kidney tubular cells in which it is reduced and excreted into the urine as mesna where it reacts with toxic metabolites. We have observed that mesna, but not dimesna, may inhibit growth of several human malignant cell lines in vitro. Some are extremely sensitive, whereas others are more or less resistant. It was found that 2/4 relatively resistant human bladder cancer cell lines turned sensitive upon repeated administrations of mesna and 5/5 cell lines appeared to be sensitive to mesna when grown in serum-free medium. The results seem to provide an explanation of the remarkable positive clinical effects of prolonged oral mesna treatment in patients with superficial bladder cancer.
Blomgren
H
H
Department of General Oncology, Radiumhemmet, Karolinska Hospital, Stockholm, Sweden.
Hallström
M
M
Hillgren
H
H
D002460:Cell Line; D004261:DNA Replication / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D007700:Kinetics; D015080:Mesna / Q000494:pharmacology* / Q000627:therapeutic use; D009363:Neoplasm Proteins / Q000096:biosynthesis; D011392:Proline / Q000378:metabolism; D012334:RNA, Neoplasm / Q000096:biosynthesis / Q000187:drug effects; D013936:Thymidine / Q000378:metabolism; D014529:Uridine / Q000378:metabolism; D001749:Urinary Bladder Neoplasms / Q000188:drug therapy*
D009363:Neoplasm Proteins; D012334:RNA, Neoplasm; D011392:Proline; D015080:Mesna; D013936:Thymidine; D014529:Uridine