Phase I and pharmacokinetic study of 502U83 (an arylmethylaminopropanediol) in cancer patients.

502U83, a novel arylmethylaminopropanediol, has proven active in vivo against a panel of murine leukemia and solid tumors as well as in a tumor clonogenic assay against a variety of fresh human cancers. A total of 35 previously treated cancer patients were enrolled in a phase I study of this compound. The maximally tolerated dose (MTD) appears to be 12,800 mg/m2/72 h by continuous intravenous infusion with severe granulocytopenia occurring in three of five patients. There were no objective clinical responses. Serum pharmacokinetic parameters were as follows: plasma terminal phase half-life (t1/2 beta) = 3.84 h; total body clearance (CLB) = 53.1 l/h/m2; volume of distribution at steady state (Vdss) = 127.9 l/m2; maximum plasma concentration (Cmax) = 3.7 micrograms/ml (at 12,800 mg/m2/72 h dose).
AuthorsK S Lam, D S Alberts, Y M Peng, F Brodar, B Matias, M Modiano, R Tuttle, V Sol Lucas, W Wargin
JournalAnti-cancer drugs (Anticancer Drugs) Vol. 3 Issue 3 Pg. 219-24 (Jun 1992) ISSN: 0959-4973 [Print] ENGLAND
PMID1525401 (Publication Type: Journal Article)
Chemical References
  • Anthracenes
  • Antineoplastic Agents
  • Intercalating Agents
  • 502U83
  • Anthracenes (adverse effects, pharmacokinetics, therapeutic use)
  • Antineoplastic Agents (adverse effects, pharmacokinetics, therapeutic use)
  • Chromatography, High Pressure Liquid
  • Drug Evaluation
  • Female
  • Half-Life
  • Humans
  • Intercalating Agents (adverse effects, pharmacokinetics, therapeutic use)
  • Male
  • Neoplasms (drug therapy, metabolism)

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