Clinical pharmacology of UCN-01: Initial observations and comparison to preclinical models

Edward A. Sausville*, Richard D. Lush, Donna Headlee, Adaline C. Smith, William D. Figg, Susan G. Arbuck, Adrian M. Senderowicz, Eiichi Fuse, Hiromi Tanii, Takashi Kuwabara, Satoshi Kobayashi

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

82 Scopus citations


UCN-01 (7-hydroxystaurosporine; NSC 638850) is a protein kinase antagonist selected for clinical trial based in part on evidence of efficacy in a preclinical renal carcinoma xenograft model. Schedule studies and in vitro studies suggested that a 72-h continuous infusion would be appropriate. In rats and dogs, maximum tolerated doses produced peak plasma concentrations of approximately 0.2-0.3 μM. However, concentrations 10-fold greater are well tolerated in humans, and the compound has a markedly prolonged T( 1/4 ). Specific binding to human α1-acidic glycoprotein has been demonstrated. These findings reinforce the need to consider actual clinical pharmacology data in 'real time' with phase I studies.

Original languageEnglish
Pages (from-to)S54-S59
JournalCancer Chemotherapy and Pharmacology, Supplement
StatePublished - Aug 1998
Externally publishedYes


  • Protein kinase antagonist
  • Staurosporine, 7-hydroxy
  • α-Acidic glycoprotein


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