ISSN:
1432-0843
Keywords:
Key words Staurosporine
;
7-hydroxy
;
Protein kinase antagonist
;
α1-Acidic glycoprotein
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Abstract 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 T1/2. 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.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/s002800051080
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