BACKGROUND: Exatecan mesylate (DX-8951f) is a water soluble analogue of @entity9800 that inhibits topoisomerase I. This multi-centre phase II study evaluated the activity of single agent exatecan in previously untreated @entity1 with advanced @entity1149 ( @entity1149 ). @entity1 AND METHODS: @entity1 with histologically or cytologically proven stage IIIb or IV @entity1149 were treated with exatecan 0.5 mg/m(2) per day by 30 min intra-venous (i.v.) infusion for 5 days every 3 weeks to a maximum of six cycles. Measurable disease was documented prior to study entry and @entity1 were re-staged every two cycles. Pharmacokinetic (PK) sampling was performed during cycle one. RESULTS: 39 @entity1 (32 @entity1 ECOG performance status 0 or 1; 29 male and ten female; mean age 63 years) were entered into the study. Thirty-three completed at least two cycles of exatecan and 11 completed six cycles. Two @entity1 (5.1%, 95% C.I. 0.3-21.3%) had a partial response, 7 (18.0%) minor response and 8 (20.5%) stable disease. Median time @entity5 ( @entity5 ) was 88 days and median overall survival 262 days. The main @entity137 was reversible @entity1398 . PK analysis of exatecan demonstrated a mean clearance of 2.28 l/h per m(2), volume of distribution 18.2 l/m(2) and mean elimination half-life of 7.9 h. CONCLUSIONS: Exatecan mesylate has limited activity in advanced @entity1149 and is not recommended for further evaluation as a single agent in this @entity5 type. PK data from this trial supports results established in phase I studies.

Phase II study of exatecan mesylate (DX-8951f) as first line therapy for advanced XXXX .

@entity1 :: ('9606', 'Species') :: ['Patients', 'patients', 'PATIENTS'] @entity137 :: ('MESH:D064420', 'Disease') :: ['toxicity'] @entity5 :: ('MESH:D009369', 'Disease') :: ['to tumour progression', 'TTP', 'tumour'] @entity1149 :: ('MESH:D002289', 'Disease') :: ['NSCLC', 'non-small cell lung cancer'] @entity1398 :: ('MESH:D009503', 'Disease') :: ['neutropenia'] @entity9800 :: ('MESH:D002166', 'Chemical') :: ['camptothecin']
@entity1149 :: (MESH:D002289,Disease) :: ['non-small cell lung cancer']
