title: UCN-01 Kyowa Hakko Kogyo Co.
abstract: Kyowa Hakko Kogyo is developing UCN-01, a selective but non-specific inhibitor of kinases with good activity against protein kinase C (PKC) and the cyclin-dependent kinases (CDKs). This hydroxylated derivative of staurosporine has potential for the treatmentfor cancer [154087], [311028], and may be useful in the treatment of chronic lymphocytic leukemia [312089]. It is in phase I clinical trials [321641], [326004], [326256]. At the 11th NCI-EORTC-AACR Symposium (Amsterdam, November 2000), a presentation was made on UCN-01. In the initial clinical trial, in which UCN-01 was administered by continuous infusion for 72 h, a prolonged half-life of 600 h was observed. The MTD was 42.5 mg/m2/day x 3. One patient with refractory melanoma achieved a partial response, another patient with refractory anaplastic large cell lymphoma had no evaluable diseasefor more than three years [391376].
authors.affiliation: University of Leeds, Molecular Medicine Unit, St James's University Hospital, UK. medkg@leeds.ac.uk
authors.forename: K
authors.initials: K
authors.lastname: Grosios
mesh_terms: D000470:Alkaloids / Q000009:adverse effects / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D000075202:Contraindications; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D019311:Staurosporine / Q000031:analogs & derivatives; D013329:Structure-Activity Relationship
chemical_list: D000470:Alkaloids; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; C054852:7-hydroxystaurosporine; D011493:Protein Kinase C; D019311:Staurosporine