Abstract |
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).
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Authors | K S Lam, D S Alberts, Y M Peng, F Brodar, B Matias, M Modiano, R Tuttle, V Sol Lucas, W Wargin |
Journal | Anti-cancer drugs
(Anticancer Drugs)
Vol. 3
Issue 3
Pg. 219-24
(Jun 1992)
ISSN: 0959-4973 [Print] England |
PMID | 1525401
(Publication Type: Journal Article)
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Chemical References |
- Anthracenes
- Antineoplastic Agents
- Intercalating Agents
- 502U83
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Topics |
- 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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